Page last updated: 2024-12-05

vorinostat

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Description

Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5311
CHEMBL ID98
CHEBI ID45716
SCHEMBL ID9018
MeSH IDM0288128

Synonyms (147)

Synonym
AC-1923
HY-10221
VORINOSTAT,CAS:149647-78-9
zolinza; saha
AB00375377-08
AB00375377-09
nsc-701852
vorinostat
zolinza
vorinostat msd
mk-0683
suberanilohydroxamic acid
sw-064652
suberoylanilide hydroxamic acid
c14h20n2o3
zolinza (tn)
149647-78-9
vorinostat (jan/usan)
D06320
octanedioic acid hydroxyamide phenylamide
SHH ,
saha
DB02546
1ZZ1
EC-000.2057
nsc701852
n-hyrdroxy-n'-phenyloctanediamide
8-(hydroxyamino)-8-oxo-n-phenyl-octanamide
ccris 8456
mk0683
saha, suberoylanilide hydroxamic acid
win64652
ski390
zolinza (tn) (merck)
n-hydroxy-n'-phenyl-octane-1,8-diotic acid diamide
octanediamide, n-hydroxy-n'-phenyl-
NCGC00168085-02
n-hydroxy-n'-phenyloctanediamide
saha cpd
vorinostat [usan]
chembl98 ,
bdbm19149
cid_5311
n-hydroxy-n''-phenyloctanediamide
n1-hydroxy-n8-phenyloctanediamide
MLS001065855
smr000486344
BRD-K81418486-001-10-3
BRD-K81418486-001-17-8
chebi:45716 ,
nsc-748799
nsc-759852
FT-0650593
n'-hydroxy-n-phenyloctanediamide
BRD-K81418486-001-12-9
NCGC00168085-01
n1-hydroxy-n8-phenyl-octanediamide
A808935
sk1390
octanediamide, n1-hydroxy-n8-phenyl
nsc748799
BRD-K81418486-001-01-2
NCGC00168085-03
NCGC00168085-04
HMS3264D20
unii-58ifb293ji
mk 0683
nsc 701852
nsc 759852
vorinostat [usan:inn]
hsdb 7930
58ifb293ji ,
nsc 748799
SUBEROYLANILIDE HYDROXAMIC ACID (SAHA)
cas-149647-78-9
dtxsid6041133 ,
tox21_112605
tox21_113623
dtxcid4021133
nsc759852
pharmakon1600-01502267
H1388
suberoylanilidehydroxamic acid
vorinostat (saha, mk0683)
HMS2219L20
VORINOSTAT - SAHA
AKOS015966648
vorinostatum
BCPP000018
vorinostat,saha,zolinza,mk-0683
octanediamide, n1-hydroxy-n8-phenyl-
AM20030018
vorinostat [mi]
vorinostat [vandf]
vorinostat [jan]
vorinostat [mart.]
vorinostat [orange book]
vorinostat [inn]
vorinostat [who-dd]
1T69
4LXZ
CS-0589
S1047
gtpl6852
HMS3327C12
BP-30216
CCG-208659
SCHEMBL9018
NCGC00168085-05
tox21_112605_1
DG-0025
vorinostat, saha, suberoylanilide hydroxamic acid
AB00375377-07
MLS006011941
W-201327
HB1396
HMS3650D09
AB01644613_25
mfcd00945317
sr-05000000373
SR-05000000373-6
HMS3654G11
SR-05000000373-2
saha, >=98% (hplc)
HMS3715E22
NCGC00168085-13
SW199536-4
EX-A2745
vorinostat (saha) ,
n-hydroxy-n inverted exclamation mark -phenyloctanediamide
SY009383
1227736-21-1
SR-05000000373-8
suberanilohydroxaminic acid
BCP01858
Q905901
BRD-K81418486-001-13-7
BRD-K81418486-001-18-6
vorinostat (saha; mk0683)
SB17319
HMS3426G03
HMS3745M03
BP-25652
vorinostat(saha)
BV164560
EN300-120641
Z1530532755

Research Excerpts

Overview

Vorinostat is an oral histone deacetylase (HDAC) inhibitor and has been used for the treatment of T-cell lymphoma. It could attenuate its anticancer activity by activating the mTOR pathway.

ExcerptReferenceRelevance
"Vorinostat (SAHA) is an epigenetic modulator actively used in clinical oncology."( Histone Methyltransferases as a New Target for Epigenetic Action of Vorinostat.
Belitsky, G; Kirsanov, K; Maksimova, V; Makus, J; Popova, V; Prus, A; Trapeznikova, E; Usalka, O; Yakubovskaya, M; Zhidkova, E, 2023
)
1.87
"Vorinostat is a pan histone deacetylase inhibitor (HDACi) that has been investigated in MPN."( Methylation age as a correlate for allele burden, disease status, and clinical response in myeloproliferative neoplasm patients treated with vorinostat.
Andersen, C; Greenfield, G; Grinfeld, J; Hasselbalch, HC; McMullin, MF; McPherson, S; Mills, KI; Nangalia, J, 2019
)
1.44
"Vorinostat is a histone deacetylase inhibitor approved for cancer treatment, but it could attenuate its anticancer activity by activating the mTOR pathway."( Fluvastatin potentiates anticancer activity of vorinostat in renal cancer cells.
Asano, T; Isono, M; Miyai, K; Okubo, K; Sato, A, 2020
)
1.54
"Vorinostat is a drug used to treat cutaneous T cell lymphoma whose action mechanism is based on Histone Deacetylase inhibition. "( Vorinostat as potential antiparasitic drug.
Ariza-Ortega, JA; Flores-García, Y; Herrera-Martínez, M; López-Contreras, L; Montaño, S; Orozco-Samperio, E, 2020
)
3.44
"As vorinostat is an oral agent and not a P-glycoprotein substrate it may have advantages in such combination therapy."( Vorinostat and fenretinide synergize in preclinical models of T-cell lymphoid malignancies.
Chen, WH; Hindle, A; Kang, MH; Koneru, B; Makena, MR; Nguyen, TH; Reynolds, CP; Verlekar, DU, 2021
)
2.58
"Vorinostat is an oral histone deacetylase (HDAC) inhibitor and has been used for the treatment of T-cell lymphoma."( Vorinostat ameliorates IL-1α-induced reduction of type II collagen by inhibiting the expression of ELF3 in chondrocytes.
Cao, L; Miao, X; Wang, P; Wu, Y; Yu, X; Zhang, Q; Zhou, C, 2021
)
2.79
"Vorinostat is a histone deacetylase inhibitor (HDACi) that was demonstrated in our previous study to inhibit the proliferation, migration, and invasion of cervical cancer cells by regulating the PI3K/Akt signaling pathway. "( Vorinostat targets UBE2C to reverse epithelial-mesenchymal transition and control cervical cancer growth through the ubiquitination pathway.
Cai, Y; Hsiao, WLW; Liang, H; Liu, C; Luo, D; Pan, B; Peng, F; Su, J; Xia, C; Yin, S, 2021
)
3.51
"Vorinostat is a histone deacetylase inhibitor (HDACi). "( A phase 2 study of vorinostat in locally advanced, recurrent, or metastatic adenoid cystic carcinoma.
Barrett, MT; Boerner, SA; Casetta, L; Chao, J; Chen, A; Goncalves, PH; Hansen, AR; Heilbrun, LK; Kummar, S; Lenkiewicz, E; LoRusso, PM; Malasi, S; Piekarz, RL; Pilat, MJ; Siu, LL; Smith, DW; Sukari, AW, 2017
)
2.23
"Vorinostat is a histone deacetylase inhibitor that has demonstrated preclinical activity in numerous cancer models. "( Clinical pharmacology profile of vorinostat, a histone deacetylase inhibitor.
Agrawal, NG; Friedman, EJ; Iwamoto, M; Rubin, EH; Sandhu, P; Wagner, JA, 2013
)
2.11
"Vorinostat is a small molecule inhibitor of class I and II histone deacetylase enzymes which alters the expression of target genes including the cell cycle gene p21, leading to cell cycle arrest and apoptosis."( Vorinostat in combination with bortezomib in patients with advanced malignancies directly alters transcription of target genes.
Alberti, D; Bailey, HH; Espinoza-Delgado, I; Hoang, T; Holen, KD; Kim, K; Kolesar, JM; Schelman, WR; Seo, S; Traynor, AM; Wilding, G; Wright, JJ, 2013
)
3.28
"Vorinostat is an inhibitor of histone deacetylases and was shown to attenuate GVHD in preclinical models."( Vorinostat plus tacrolimus and mycophenolate to prevent graft-versus-host disease after related-donor reduced-intensity conditioning allogeneic haemopoietic stem-cell transplantation: a phase 1/2 trial.
Beumer, JH; Braun, T; Chang, L; Choi, SW; Couriel, DR; Dinarello, CA; DiPersio, JF; Ferrara, JL; Goldstein, S; Hou, G; Kitko, C; Krijanovski, OI; Lehmann, MH; Levine, JE; Magenau, JM; Mapara, MY; Paczesny, S; Pawarode, A; Reddy, P; Stockerl-Goldstein, K; Sun, Y; Tawara, I; Yanik, GA, 2014
)
2.57
"Vorinostat is a small molecule inhibitor of class I and II histone deacetylases with preclinical activity in melanoma."( Phase II trial of vorinostat in advanced melanoma.
Adams, PD; Alpaugh, RK; Haas, NB; Hotte, S; Litwin, S; Martin, LP; McBryan, T; McWhirter, E; Oza, A; Polintan, R; Quirt, I; vonMehren, M; Wang, L; Zweibel, J, 2014
)
2.18
"Vorinostat is a panHDAC inhibitor that sensitizes breast cancer cells to taxanes and trastuzumab by suppressing HDAC6 and Hsp90 client proteins."( A phase I-II study of the histone deacetylase inhibitor vorinostat plus sequential weekly paclitaxel and doxorubicin-cyclophosphamide in locally advanced breast cancer.
Alpaugh, RK; Andreopoulou, E; Bhalla, K; Fehn, K; Fineberg, S; Fiskus, W; Hershman, DL; Huang, M; Kalinsky, K; Makower, D; Montgomery, LL; Negassa, A; Pellegrino, CM; Sparano, JA; Tu, Y; Wiechmann, LS, 2014
)
1.37
"Vorinostat, which is an extensively studied inhibitor against histone deacetylase (HDAC), shows limited clinical activity to solid tumors. "( A novel small molecule hybrid of vorinostat and DACA displays anticancer activity against human hormone-refractory metastatic prostate cancer through dual inhibition of histone deacetylase and topoisomerase I.
Chao, SW; Guh, JH; Hsu, JL; Huang, WJ; Li, TK; Liu, SP; Pan, SL; Yang, YC; Yu, CC, 2014
)
2.13
"Vorinostat is an anticancer agent structurally similar to PBA."( Comparative effects of 4-phenyl-3-butenoic acid and vorinostat on cell growth and signaling.
Ali, A; Burns, TJ; Matesic, DF, 2015
)
1.39
"Vorinostat is a histone deacetylase inhibitor that has radiosensitizing properties."( Phase I Study of Vorinostat as a Radiation Sensitizer with 131I-Metaiodobenzylguanidine (131I-MIBG) for Patients with Relapsed or Refractory Neuroblastoma.
Chen, E; Cohn, SL; Courtier, J; Czarnecki, S; DuBois, SG; Geier, E; Giacomini, K; Goodarzian, F; Granger, MM; Groshen, S; Haas-Kogan, DA; Hawkins, R; Jackson, H; Marachelian, A; Matthay, KK; Park, JR; Shimada, H; Tsao-Wei, D; Villablanca, JG; Weiss, B; Yang, X; Yanik, GA, 2015
)
1.48
"Vorinostat is a histone deacetylase inhibitor that changes gene expression and protein activity. "( Vorinostat in patients with advanced malignant pleural mesothelioma who have progressed on previous chemotherapy (VANTAGE-014): a phase 3, double-blind, randomised, placebo-controlled trial.
Baas, P; Buikhuisen, WA; Calvert, H; Chu, Q; Eberhardt, WE; Fennell, D; Fukuoka, K; Gaafar, RM; Hillerdal, G; Kindler, HL; Krug, LM; Lafitte, JJ; Lubiniecki, GM; Manegold, C; Öhman, R; Plummer, R; Smith, M; Sun, X; Tsao, AS, 2015
)
3.3
"Vorinostat is an FDA-approved histone deacetylase inhibitor (HDACi) that has proven clinical success in some patients; however, it remains unclear why certain patients remain unresponsive to this agent and other HDACis. "( A genome scale RNAi screen identifies GLI1 as a novel gene regulating vorinostat sensitivity.
Falkenberg, KJ; Gould, CM; Johnstone, RW; Luu, J; Matthews, GM; Newbold, A; Simpson, KJ; Trapani, JA, 2016
)
2.11
"Vorinostat-XP is a feasible first-line chemotherapy for patients with advanced GC. "( Vorinostat in combination with capecitabine plus cisplatin as a first-line chemotherapy for patients with metastatic or unresectable gastric cancer: phase II study and biomarker analysis.
Kang, YK; Lee, CW; Na, YS; Ryoo, BY; Ryu, MH; Yoo, C, 2016
)
3.32
"Vorinostat (SAHA) is a canonical US Food and Drug Administration-approved histone deacetylase (HDAC) inhibitor for the treatment of cutaneous T-cell lymphoma."( A facile route to form self-carried redox-responsive vorinostat nanodrug for effective solid tumor therapy.
Fang, H; Han, L; Wang, T; Wu, J; Yin, X; Zhang, N,
)
1.1
"Vorinostat is a potent histone deacetylase inhibitor that blocks the catalytic site of these enzymes. "( Development of vorinostat: current applications and future perspectives for cancer therapy.
Garcia-Vargas, J; Hardwick, JS; Richon, VM, 2009
)
2.15
"Vorinostat is a small molecule inhibitor of histone deacetylase, and has shown preclinical activity in non-small cell lung cancer (NSCLC)."( Vorinostat (NSC# 701852) in patients with relapsed non-small cell lung cancer: a Wisconsin Oncology Network phase II study.
Dubey, S; Eickhoff, JC; Espinoza-Delgado, I; Groteluschen, DL; Hallahan, CM; Huie, MS; Kolesar, JM; Marcotte, SM; Schell, K; Schiller, JH; Traynor, AM; Weeks, HR; Wilding, G, 2009
)
3.24
"Vorinostat is a novel histone deacetylase (HDAC) inhibitor approved for the treatment of advanced CTCL. "( Vorinostat: A novel therapy for the treatment of cutaneous T-cell lymphoma.
Kavanaugh, SA; Kavanaugh, SM; Kolesar, JM; White, LA, 2010
)
3.25
"Vorinostat is an inhibitor of histone deacetylase 6, which acetylates tubulin and stabilizes microtubules. "( Phase I study of vorinostat (suberoylanilide hydroxamic acid, NSC 701852) in combination with docetaxel in patients with advanced and relapsed solid malignancies.
Bradley, D; Daignault, S; Dunn, R; Egorin, MJ; Hussain, M; Kalemkerian, GP; Schneider, BJ; Smith, DC, 2012
)
2.16
"Vorinostat is an epigenetic targeted drug belonging to the histone deacetylase (HDAC) inhibitors family."( Vorinostat in acute myeloid leukemia and myelodysplastic syndromes.
Prebet, T; Vey, N, 2011
)
2.53
"Oral vorinostat is a promising agent in FL and MZL, with an acceptable safety profile. "( Phase II study of vorinostat for treatment of relapsed or refractory indolent non-Hodgkin's lymphoma and mantle cell lymphoma.
Delioukina, M; Espinoza-Delgado, I; Forman, SJ; Frankel, P; Gandara, D; Kirschbaum, M; Matsuoka, D; Nademanee, A; Newman, E; Popplewell, L; Pullarkat, V; Pulone, B; Rotter, AJ; Zain, J, 2011
)
1.22
"Vorinostat is a histone deacetylase inhibitor (HDACi) that has been approved for the treatment of cutaneous T-cell lymphoma."( Vorinostat-induced apoptosis in mantle cell lymphoma is mediated by acetylation of proapoptotic BH3-only gene promoters.
Campo, E; Colomer, D; López-Guerra, M; Rosich, L; Roué, G; Saborit-Villarroya, I; Xargay-Torrent, S, 2011
)
2.53
"Vorinostat is a histone deacetylase inhibitor that effectively suppresses cancer-cell proliferation by inducing cell-cycle arrest and/or apoptosis. "( Requirement of p38 MAPK for a cell-death pathway triggered by vorinostat in MDA-MB-231 human breast cancer cells.
Kanematsu, S; Miki, H; Tsubura, A; Uehara, N; Yoshizawa, K, 2012
)
2.06
"Vorinostat is a histone deacetylase inhibitor that blocks cancer cell proliferation through the regulation of cyclin-dependent kinase inhibitors. "( Vorinostat enhances protein stability of p27 and p21 through negative regulation of Skp2 and Cks1 in human breast cancer cells.
Tsubura, A; Uehara, N; Yoshizawa, K, 2012
)
3.26
"Vorinostat is a histone deacetylase inhibitor used in the treatment of recurrent or persistent cases of cutaneous T-cell lymphoma (CTCL). "( QT interval prolongation and torsades de pointes in a patient undergoing treatment with vorinostat: a case report and review of the literature.
Lynch, DR; Newby, LK; Washam, JB, 2012
)
2.04
"Vorinostat is a potent HDAC inhibitor and has shown potential to inhibit growth of human xenograft tumors."( Vorinostat, an HDAC inhibitor attenuates epidermoid squamous cell carcinoma growth by dampening mTOR signaling pathway in a human xenograft murine model.
Athar, M; Ballestas, ME; Chaudhary, SC; Elmets, CA; Kopelovich, L; Kurundkar, D; Srivastava, RK, 2013
)
2.55
"Vorinostat is a HDACi which has produced responses in these disorders."( Vorinostat induces apoptosis and differentiation in myeloid malignancies: genetic and molecular mechanisms.
Almeida, AM; Belo, H; Cardoso, BA; Silva, G, 2013
)
2.55
"Vorinostat (Zolinza) is a histone deacetylase inhibitor that has demonstrated activity in patients with advanced solid tumors in phase I trials. "( Early phase II trial of oral vorinostat in relapsed or refractory breast, colorectal, or non-small cell lung cancer.
Chen, C; Dumez, H; Randolph, SS; Ricker, JL; Schöffski, P; Van Cutsem, E; Vansteenkiste, J, 2008
)
2.08
"Vorinostat is a histone deacetylase inhibitor that induces differentiation, growth arrest, and/or apoptosis of malignant cells both in vitro and in vivo and has shown clinical responses in approximately 30% of patients with advanced mycosis fungoides and Sézary syndrome cutaneous T-cell lymphoma (CTCL). "( Constitutive activation of signal transducers and activators of transcription predicts vorinostat resistance in cutaneous T-cell lymphoma.
Fantin, VR; Frankel, SR; Gooden, F; Harrington, EA; Hendrickson, RC; Hou, XS; Kadin, ME; Korenchuk, S; Li, L; Loboda, A; Paweletz, CP; Pierce, JW; Randolph, S; Reilly, JF; Richon, VM; Roth, JA; Ware, CM, 2008
)
2.01

Effects

Vorinostat has good therapeutic efficacy against primary cutaneous T-cell lymphoma in the refractory stage. It has been efficient in vitro and, in some cases, against parasites such as malaria, leishmaniasis, cryptosporidiosis, amoebiasis, and schistosomiasis.

ExcerptReferenceRelevance
"Vorinostat has good therapeutic efficacy against primary cutaneous T-cell lymphoma in the refractory stage. "( Vorinostat upregulates MICA via the PI3K/Akt pathway to enhance the ability of natural killer cells to kill tumor cells.
Cai, Y; He, Z; Liang, S; Xia, C, 2020
)
3.44
"Vorinostat has been efficient in vitro and, in some cases, in vivo, against parasites that cause parasitic diseases, such as malaria, leishmaniasis, cryptosporidiosis, amoebiasis, and schistosomiasis."( Vorinostat as potential antiparasitic drug.
Ariza-Ortega, JA; Flores-García, Y; Herrera-Martínez, M; López-Contreras, L; Montaño, S; Orozco-Samperio, E, 2020
)
3.44
"Vorinostat (VST) has been reported to have antioxidant and anti-inflammatory effects in bothin-vitro and in vivo models."( Protective Effects of Low Dose Vorinostat on Cisplatin-Induced Nephrotoxicity in Rats.
Ali, AS; Ali, SS; Bashraf, OMO; Eweis, HSA, 2021
)
1.63
"Vorinostat (VOR) has been reported to enhance the cytotoxic effects of doxorubicin (DOX) with fewer side effects because of the lower DOX dosage in breast cancer cells. "( Transactivation of bad by vorinostat-induced acetylated p53 enhances doxorubicin-induced cytotoxicity in cervical cancer cells.
Hoe, KL; Hwang, SO; Kim, DU; Kim, JH; Lee, SJ; Nam, JH; Nam, M; Noh, EJ, 2014
)
2.15
"Vorinostat has been shown to overcome resistance to gefitinib. "( Phase I/II study of gefitinib (Iressa(®)) and vorinostat (IVORI) in previously treated patients with advanced non-small cell lung cancer.
Han, JY; Hwang, KH; Kim, HT; Kim, JY; Lee, GK; Lee, SH; Lee, YJ; Yun, T, 2015
)
2.12
"Oral vorinostat has the remarkable curative effect on aggravated and recurrent cutaneous T-cell lymphoma (CTCL), but is accompanied by serious adverse effects. "( Preparation of a mixed-matrix hydrogel of vorinostat for topical administration on the rats as experimental model.
Dai, W; Li, Y; Sun, F; Teng, L; Wang, C; Yao, J; Yu, C, 2015
)
1.2
"Vorinostat has shown promising clinical activity against hematologic and solid tumors at doses that have been well tolerated by patients."( Development of vorinostat: current applications and future perspectives for cancer therapy.
Garcia-Vargas, J; Hardwick, JS; Richon, VM, 2009
)
1.43
"Vorinostat has demonstrated significant anticancer activity against hematologic and solid tumors at doses well tolerated by patients and has been approved for the treatment of patients with cutaneous T-cell lymphoma."( Molecular sequelae of histone deacetylase inhibition in human retinoblastoma cell lines: clinical implications.
Kotoula, V; Marks, PA; McMullan, C; Miller, JW; Mitsiades, CS; Mitsiades, N; Negri, J; Poulaki, V, 2009
)
1.07
"Vorinostat has the capacity to elicit CRT exposure, suggesting its usefulness as immunogenic antitumour agent."( The histone deacetylase inhibitor vorinostat induces calreticulin exposure in childhood brain tumour cells in vitro.
Beck, JF; Becker, S; Gressmann, S; Schmudde, M; Sonnemann, J; Wittig, S, 2010
)
2.08
"vorinostat has shown an acceptable toxicity profile with mainly gastrointestinal and constitutional side effects. "( Vorinostat in acute myeloid leukemia and myelodysplastic syndromes.
Prebet, T; Vey, N, 2011
)
3.25
"Oral vorinostat has limited single-agent activity in relapsed/refractory HL."( A phase 2 study of vorinostat for treatment of relapsed or refractory Hodgkin lymphoma: Southwest Oncology Group Study S0517.
Cook, JR; Fisher, RI; Forman, SJ; Goldman, BH; Kirschbaum, MH; Rimsza, LM; Zain, JM, 2012
)
1.16
"Vorinostat has demonstrated activity in refractory cutaneous T-cell lymphoma. "( Phase II trial of oral vorinostat (suberoylanilide hydroxamic acid) in relapsed diffuse large-B-cell lymphoma.
Cheson, BD; Coiffier, B; Crump, M; Frankel, SR; Jacobsen, ED; Randolph, SS; Ricker, JL; Sun, L; Xie, H, 2008
)
2.1

Actions

Vorinostat was found to inhibit KCs proliferation and to induce their differentiation and apoptosis. It does not enhance viral fusion with cells but rather enhances the kinetics and efficiency of postentry viral events.

ExcerptReferenceRelevance
"Vorinostat was found to inhibit KCs proliferation and to induce their differentiation and apoptosis. "( Vorinostat, a histone deacetylase inhibitor, as a potential novel treatment for psoriasis.
Bochner, R; Fuchs-Telem, D; Gilhar, A; Keren, A; Magal, L; Malovitski, K; Nousbeck, J; Sagiv, N; Samuelov, L; Sarig, O; Sprecher, E, 2022
)
3.61
"Vorinostat does not enhance viral fusion with cells but rather enhances the kinetics and efficiency of postentry viral events, including reverse transcription, nuclear import, and integration, and enhances viral production in a spreading-infection assay."( The histone deacetylase inhibitor vorinostat (SAHA) increases the susceptibility of uninfected CD4+ T cells to HIV by increasing the kinetics and efficiency of postentry viral events.
Dobrowolski, C; Haqqani, AA; Karn, J; Lucera, MB; Mao, H; Tabler, CO; Tilton, CA; Tilton, JC, 2014
)
1.4

Treatment

Vorinostat/JQ1 inhibited glycolysis/MTOR signaling, activated the clock, and upregulated the UPR and autophagy via inhibition of YAP1/NF-κB. Treatment with vorinstat ameliorates altered expression of p-Akt, NF-B, iNOS and caspase in the neuronal tissue of TBI mice.

ExcerptReferenceRelevance
"Vorinostat treatment affects the reversal of drug resistance in SK-N-Be(2)C cells and may be associated with downregulation of stemness gene expression."( Differential effect of long-term drug selection with doxorubicin and vorinostat on neuroblastoma cells with cancer stem cell characteristics.
Chu, F; Clark, S; Czurylo, M; Jafari, N; Jie, C; Lautz, T; Madonna, MB; Naiditch, J; Qiu, Y; Zheng, X, 2013
)
1.35
"Vorinostat treatment increased the frequency of functional regulatory T-cell subsets and their transcription factors Gata3 and FoxP3 in parallel to a decrease in inflammatory dendritic cell subsets and their cytokines IL-6, IL-12, and TNF-α."( Lysine deacetylase inhibition prevents diabetes by chromatin-independent immunoregulation and β-cell protection.
Aikin, RA; Billestrup, N; Birkbak, N; Blaabjerg, L; Christensen, DP; Dahllöf, MS; Dinarello, CA; Fossati, G; Grunnet, LG; Gysemans, C; Lundh, M; Mandrup, S; Mandrup-Poulsen, T; Mascagni, P; Mathieu, C; Monzani, V; Noesgaard, D; Paraskevas, S; Piemonti, L; Schmidt, SF; Workman, CT, 2014
)
1.12
"With vorinostat treatment, the best response was partial remission in 5 patients (33%) and stabilization in 4 patients (27%)."( Vorinostat for refractory or relapsing epidermotropic T-cell lymphoma: a retrospective cohort study of 15 patients.
Brocard, A; Dréno, B; Knol, AC; Kogge, A; Peuvrel, L; Quéreux, G; Renaut, JJ; Saint-Jean, M; Volteau, C, 2015
)
2.31
"Vorinostat treatment increased histone acetylation in peripheral blood mononuclear cells (PBMCs) from treated patients, confirming target HDAC inhibition."( Histone deacetylase inhibition regulates inflammation and enhances Tregs after allogeneic hematopoietic cell transplantation in humans.
Choi, SW; Dinarello, CA; Gatza, E; Hou, G; Oravecz-Wilson, K; Reddy, P; Song, Y; Sun, Y; Tawara, I; Whitfield, J, 2015
)
1.14
"Vorinostat treatment also caused a significant increase in acetylhistone H3 and acetylhistone H4."( Role of 5'TG3'-interacting factors (TGIFs) in Vorinostat (HDAC inhibitor)-mediated Corneal Fibrosis Inhibition.
Mohan, RR; Sharma, A; Siddiqui, S; Sinha, NR, 2015
)
1.4
"Vorinostat treatment led to GRP78 acetylation, dissociation, and subsequent activation of its client protein double-stranded RNA-activated protein-like endoplasmic reticulum kinase (PERK)."( Activation of the unfolded protein response contributes toward the antitumor activity of vorinostat.
Chinnaiyan, P; Fang, B; Kahali, S; Koomen, JM; Sarcar, B; Tofilon, PJ; Williams, ES, 2010
)
1.3
"Vorinostat treatment induced CRT exposure in PFSK and DAOY cells, but not in caspase-8-deficient CADO-ES-1 cells. "( The histone deacetylase inhibitor vorinostat induces calreticulin exposure in childhood brain tumour cells in vitro.
Beck, JF; Becker, S; Gressmann, S; Schmudde, M; Sonnemann, J; Wittig, S, 2010
)
2.08
"Vorinostat-treated and control mice without tumors were also examined."( The histone deacetylase inhibitor, vorinostat, reduces tumor growth at the metastatic bone site and associated osteolysis, but promotes normal bone loss.
Akech, J; Bedard, K; Dhillon, RJ; Hussain, S; Li, X; Lian, JB; McGee-Lawrence, ME; Pratap, J; Stein, GS; Stein, JL; Szabo, G; van Wijnen, AJ; Westendorf, JJ; Wixted, JJ, 2010
)
1.36
"Vorinostat treatment had no effect on albuminuria, glomerular collagen IV concentration, or mesangiolysis in diabetic mice genetically deficient in eNOS."( Long-term administration of the histone deacetylase inhibitor vorinostat attenuates renal injury in experimental diabetes through an endothelial nitric oxide synthase-dependent mechanism.
Advani, A; Advani, SL; Connelly, KA; Gilbert, RE; Huang, Q; Kelly, DJ; Marsden, PA; Thai, K; White, KE; Yuen, DA, 2011
)
1.33
"Vorinostat treatment resulted in increased p21 levels in all glioma cells tested in a p53 independent manner."( Vorinostat modulates cell cycle regulatory proteins in glioma cells and human glioma slice cultures.
Fuller, GN; Lang, FF; Liu, Y; Prabhu, S; Puduvalli, VK; Rao, G; Sampath, D; Xu, J, 2011
)
2.53
"Vorinostat treatment also decreased the mutant allele burden in mice."( Efficacy of vorinostat in a murine model of polycythemia vera.
Akada, H; Akada, S; Bair, A; Gajra, A; Graziano, S; Hutchison, RE; Mohi, G, 2012
)
1.48
"Vorinostat treatment resulted in hyperacetylation of histones H3 and H4 in peripheral mononuclear cells."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
1.44
"Treatment with vorinostat resulted in a younger MA in PV patients and older MA in ET patients, in both cases a trend towards the normal chronological age."( Methylation age as a correlate for allele burden, disease status, and clinical response in myeloproliferative neoplasm patients treated with vorinostat.
Andersen, C; Greenfield, G; Grinfeld, J; Hasselbalch, HC; McMullin, MF; McPherson, S; Mills, KI; Nangalia, J, 2019
)
1.06
"Treatment of vorinostat upregulates PLD1 through PKCζ-Sp1 axis."( Phospholipase D1 is upregulated by vorinostat and confers resistance to vorinostat in glioblastoma.
Hwang, WC; Jang, Y; Kang, DW; Kang, Y; Kim, JA; Min, DS; Noh, YN, 2021
)
1.25
"Treatment with vorinostat reduced the IL-1α-induced production of mitochondrial reactive oxygen species (ROS) in T/C-28a2 cells."( Vorinostat ameliorates IL-1α-induced reduction of type II collagen by inhibiting the expression of ELF3 in chondrocytes.
Cao, L; Miao, X; Wang, P; Wu, Y; Yu, X; Zhang, Q; Zhou, C, 2021
)
2.4
"Treatment with Vorinostat/JQ1 inhibited glycolysis/MTOR signaling, activated the clock, and upregulated the UPR and autophagy via inhibition of YAP1/NF-κB."( YAP1 enhances NF-κB-dependent and independent effects on clock-mediated unfolded protein responses and autophagy in sarcoma.
Babichev, Y; C Brady, D; Chor, S; E Ciotti, G; E Marino, G; Egolf, S; Eisinger-Mathason, TSK; Gladdy, R; Koumenis, C; Leli, NM; Liu, Y; Mancuso, A; Pak, K; Park, PMC; Posimo, JM; Qi, J; Rivera-Reyes, A; Sostre-Colón, J; Tameire, F; Weber, K; Ye, S, 2018
)
0.82
"Also treatment with vorinostat ameliorates the altered expression of p-Akt, NF-B, iNOS and caspase by the western blot assay in the neuronal tissue of TBI mice and mRNA level of HO-1 and NQO-1 significantly enhanced in vorinostat compared to the negative control group."( Vorinostat: a histone deacetylases (HDAC) inhibitor ameliorates traumatic brain injury by inducing iNOS/Nrf2/ARE pathway.
Shi, J; Xu, J; Zhang, J; Zhang, Y, 2018
)
2.24
"Treatment with vorinostat, a histone deacetylase inhibitor (HDACi) resulted in an objective response, yet she died in less than one year from initial diagnosis."( Histone deacetylase inhibitor for NUT midline carcinoma.
Bell, D; Christensen, AM; Maher, OM; Tarek, N; Yedururi, S, 2015
)
0.76
"Treatment with vorinostat activated IGF-1R signaling in vorinostat-resistant but not vorinostat-sensitive NSCLC cells."( Activation of insulin-like growth factor receptor signaling mediates resistance to histone deacetylase inhibitors.
Choi, SP; Hyun, SY; Kim, JS; Kim, WY; Kwon, SJ; Lee, HJ; Lee, HY; Lee, SC; Min, HY; Park, KH, 2015
)
0.76
"Treatment of vorinostat-resistant cells with the GLI1 small-molecule inhibitor, GANT61, phenocopied the effect of GLI1 knockdown."( A genome scale RNAi screen identifies GLI1 as a novel gene regulating vorinostat sensitivity.
Falkenberg, KJ; Gould, CM; Johnstone, RW; Luu, J; Matthews, GM; Newbold, A; Simpson, KJ; Trapani, JA, 2016
)
1.02
"Pretreatment with vorinostat led to radiosensitisation of the intrinsically radioresistant DU 145 cells, but not the radiosensitive PC-3 and 22Rv1 cells, and was independent of hypoxia status. "( Hypoxia-independent gene expression signature associated with radiosensitisation of prostate cancer cell lines by histone deacetylase inhibition.
Clancy, T; Flatmark, K; Frikstad, KM; Jonsson, M; Julin, CH; Lyng, H; Matias-Guiu, X; Ragnum, HB; Ree, AH; Seierstad, T; Stokke, T; Yeramian, A, 2016
)
0.77
"Treatment with vorinostat induced hsp90 acetylation and inhibited its chaperone association with AKs, leading to depletion of AKs and Survivin."( Co-treatment with vorinostat synergistically enhances activity of Aurora kinase inhibitor against human breast cancer cells.
Balusu, R; Bhalla, KN; Fiskus, W; Hembruff, SL; Peiper, SC; Peth, K; Rao, R; Sharma, P; Smith, JE; Venkannagari, S, 2012
)
1.05

Toxicity

Of 14 eligible patients, three individuals experienced grade 3 gastrointestinal and related toxicities. Rat vorinostat-related adverse findings are decreased food consumption, weight loss, and hematologic changes.

ExcerptReferenceRelevance
" Rat vorinostat-related adverse findings are decreased food consumption, weight loss, and hematologic changes; a no observed adverse effects level is not established."( Nonclinical safety assessment of the histone deacetylase inhibitor vorinostat.
Andrews, PA; Armstrong, M; Galloway, S; Kerr, JS; Lagrutta, A; Miller, T; Richon, VM,
)
0.88
"In early-phase studies with targeted therapeutics and radiotherapy, it may be difficult to decide whether an adverse event should be considered a dose-limiting toxicity (DLT) of the investigational systemic agent, as acute normal tissue toxicity is frequently encountered with radiation alone."( Gastrointestinal toxicity of vorinostat: reanalysis of phase 1 study results with emphasis on dose-volume effects of pelvic radiotherapy.
Bratland, A; Dueland, S; Flatmark, K; Hollywood, D; Ree, AH, 2011
)
0.66
"Of 14 eligible patients, three individuals experienced Common Terminology Criteria of Adverse Events grade 3 gastrointestinal and related toxicities, representing a toxicity profile vorinostat has in common with radiotherapy to pelvic target volumes."( Gastrointestinal toxicity of vorinostat: reanalysis of phase 1 study results with emphasis on dose-volume effects of pelvic radiotherapy.
Bratland, A; Dueland, S; Flatmark, K; Hollywood, D; Ree, AH, 2011
)
0.85
" The most common drug-related adverse events were anorexia, nausea, fatigue, and hyperglycemia."( Evaluation of safety, pharmacokinetics, and efficacy of vorinostat, a histone deacetylase inhibitor, in the treatment of gastrointestinal (GI) cancer in a phase I clinical trial.
Chin, K; Doi, T; Hamaguchi, T; Hatake, K; Mehta, A; Noguchi, K; Ohtsu, A; Otsuki, T; Shirao, K, 2013
)
0.64
" Treatment-related adverse events (AE) included grade 1 to 2 nausea, diarrhea, fatigue, weight loss, anemia, and elevated creatinine."( Combined autophagy and HDAC inhibition: a phase I safety, tolerability, pharmacokinetic, and pharmacodynamic analysis of hydroxychloroquine in combination with the HDAC inhibitor vorinostat in patients with advanced solid tumors.
Amaravadi, RK; Carew, JS; Curiel, TJ; Davis, LE; Espitia, CM; Giles, FJ; Mahalingam, D; Mita, AC; Mita, M; Nawrocki, ST; Sarantopoulos, J; Wood, L, 2014
)
0.59
" The disease is characterized by the accumulation of toxic misfolded protein species that present as perinuclear aggregates known as aggresomes."( Tubulin hyperacetylation is adaptive in cardiac proteotoxicity by promoting autophagy.
Bhuiyan, MS; Ferguson, BS; James, J; McKinsey, TA; McLendon, PM; Osinska, H; Robbins, J, 2014
)
0.4
" In this Pelvic Radiation and Vorinostat (PRAVO) study, we investigated mechanisms of adverse effects in response to the histone deacetylase (HDAC) inhibitor vorinostat (suberoylanilide hydroxamic acid, SAHA) when administered as a potential radiosensitiser."( Induction of Apoptosis in Intestinal Toxicity to a Histone Deacetylase Inhibitor in a Phase I Study with Pelvic Radiotherapy.
Andersen, SN; Barua, IS; Dueland, S; Flatmark, K; Kalanxhi, E; Lindvall, JM; Pettersen, SJ; Redalen, KR; Ree, AH; Risberg, K; Waagene, S, 2017
)
0.74
" To the best of our knowledge, this is the first report deciphering mechanisms of normal tissue adverse effects in response to an HDAC inhibitor within a combined-modality treatment regimen."( Induction of Apoptosis in Intestinal Toxicity to a Histone Deacetylase Inhibitor in a Phase I Study with Pelvic Radiotherapy.
Andersen, SN; Barua, IS; Dueland, S; Flatmark, K; Kalanxhi, E; Lindvall, JM; Pettersen, SJ; Redalen, KR; Ree, AH; Risberg, K; Waagene, S, 2017
)
0.46
" formulations and can be suggested as a promising stable and safe nanoparticulate delivery system with prolonged release and potentiated cytotoxicity."( Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities.
Abu Hashim, II; Badria, FAE; Mohamed, EA; Shaaban, AAA; Suddek, GM; Yusif, RM, 2017
)
0.7
"We recorded a total of 31 adverse events (26 grade 1 and five grade 2) in all study participants (n = 20)."( No adverse safety or virological changes 2 years following vorinostat in HIV-infected individuals on antiretroviral therapy.
Dantanarayana, A; Elliott, JH; Hagenauer, M; Hoy, JF; Lewin, SR; McMahon, J; Mota, TM; Prince, HM; Purcell, DFJ; Rasmussen, TA; Rhodes, A; Roney, J; Spelman, T; Tennakoon, S; Wightman, F, 2017
)
0.7
" The existing side effect prediction methods mainly focus on the chemical and biological properties of drugs."( Prediction of Side Effects Using Comprehensive Similarity Measures.
Kim, MH; Lee, T; Seo, S; Yoon, Y, 2020
)
0.56
" Suberanilohydroxamic acid (SAHA) however has been proposed to prevent corneal haze without any adverse effects."( Safety and efficacy of combination of suberoylamilide hydroxyamic acid and mitomycin C in reducing pro-fibrotic changes in human corneal epithelial cells.
Dadachanji, ZV; Das, D; Ghosh, A; Khamar, P; Krishna, L; Kumar, NR; Matalia, H; Mohan, RR; Murugeswari, P; Shetty, R; Subramani, M, 2021
)
0.62
"The combination of prolonged high-dose disulfiram and vorinostat was not safe in PWH on ART and should not be pursued despite evidence of latency reversal."( Neurotoxicity with high-dose disulfiram and vorinostat used for HIV latency reversal.
Blennow, K; Bumpus, N; Burger, D; Chang, J; Dantanarayana, A; Evans, VA; Fisher, K; Gisslen, M; Hagenauer, M; Heck, CJS; Howell, BJ; Lau, JSY; Lee, S; Lewin, SR; McMahon, JH; Palmer, S; Rasmussen, TA; Solomon, A; Symons, J; Tennakoon, S; Wu, G; Zerbato, JM; Zetterberg, HH; Zuck, P, 2022
)
1.23

Pharmacokinetics

Vorinostat had a pharmacokinetic profile similar to that established in non-Japanese patients. The median C(max) of FU at each dose level increased significantly with increasing doses of vorInostat. No pharmacokinetically interactions were noted between vorinstat and FU.

ExcerptReferenceRelevance
"Patients (n = 23) received single doses of 400 mg vorinostat on day 1 (fasted) and day 5 (fed) with 48 hours of pharmacokinetic sampling on both days."( A study to determine the effects of food and multiple dosing on the pharmacokinetics of vorinostat given orally to patients with advanced cancer.
Agrawal, NG; Du, L; Frankel, SR; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Mazina, KE; Ricker, JL; Rubin, EH; Scott, P; Sun, L; Wagner, JA, 2006
)
0.81
" Vorinostat area under the concentration versus time curve and half-life increased when vorinostat was coadministered with carboplatin and paclitaxel, but vorinostat did not alter paclitaxel pharmacokinetics."( Phase I and pharmacokinetic study of vorinostat, a histone deacetylase inhibitor, in combination with carboplatin and paclitaxel for advanced solid malignancies.
Argiris, AE; Belani, CP; Egorin, MJ; Lagattuta, TF; Musguire, LA; Parise, RA; Potter, DM; Ramalingam, SS; Ramananthan, RK; Ramanathan, RK; Stoller, RG; Zwiebel, JA, 2007
)
1.52
"The aim of this work was to use phosphorus magnetic resonance spectroscopy ((31)P MRS) to investigate the pharmacodynamic effects of LAQ824, a histone deacetylase (HDAC) inhibitor."( Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of a novel histone deacetylase inhibitor, LAQ824, in human colon carcinoma cells and xenografts.
Aherne, W; Atadja, P; Beloueche-Babari, M; Chung, YL; Griffiths, JR; Jackson, LE; Judson, IR; Kristeleit, R; Leach, MO; Troy, H; Workman, P, 2008
)
0.35
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"Elimination half-life was higher than that of SAHA (5."( Pharmacokinetics and tissue distribution of Kendine 91, a novel histone deacetylase inhibitor, in mice.
Cossío, FP; Otaegui, D; Pedraz, JL; Rodríguez-Gascón, A; Zubia, A, 2009
)
0.35
"This preliminary pharmacokinetic evaluation prompts us to believe that it is worth pursuing further development of Kendine 91 as an anticancer drug."( Pharmacokinetics and tissue distribution of Kendine 91, a novel histone deacetylase inhibitor, in mice.
Cossío, FP; Otaegui, D; Pedraz, JL; Rodríguez-Gascón, A; Zubia, A, 2009
)
0.35
" The median C(max) of FU at each dose level increased significantly with increasing doses of vorinostat, suggesting a pharmacokinetic interaction between FU and vorinostat."( A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin in patients with refractory colorectal cancer.
Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Pendyala, L; Ross, ME; Rustum, YM; Toth, K; Zwiebel, JA, 2009
)
0.82
" It possesses optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, and is negative in a microbial mutagenicity (Ames) test."( Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
Fiore, F; Fonsi, M; Gonzalez Paz, O; Jones, P; Kinzel, O; Llauger-Bufi, L; Monteagudo, E; Pescatore, G; Rowley, M; Schultz-Fademrecht, C; Steinkühler, C, 2009
)
0.35
" In the 100-500 mg dose range, vorinostat area under the concentration-time curve increased in proportion to dose with a pharmacokinetic profile similar to that established in non-Japanese patients."( Phase I and pharmacokinetic study of vorinostat (suberoylanilide hydroxamic acid) in Japanese patients with solid tumors.
Fujiwara, Y; Hardwick, JS; Iwasa, T; Kanazu, S; Otsuki, T; Tamura, T; Yamada, K; Yamada, Y; Yamamoto, N, 2009
)
0.91
" No pharmacokinetic interactions were noted between vorinostat and FU."( A phase I, pharmacokinetic, and pharmacodynamic study of two schedules of vorinostat in combination with 5-fluorouracil and leucovorin in patients with refractory solid tumors.
Diasio, RB; Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Muindi, JR; Wang, K; Zwiebel, JA, 2010
)
0.84
" Pharmacokinetic studies were performed with the initial dose."( Pediatric phase I trial and pharmacokinetic study of vorinostat: a Children's Oncology Group phase I consortium report.
Adamson, PC; Ames, MM; Blaney, SM; Fouladi, M; Gilbertson, RJ; Ingle, AM; Park, JR; Reid, JM; Schaiquevich, P; Speights, R; Stewart, CF; Sun, J; Zwiebel, J, 2010
)
0.61
" Pharmacokinetic parameters were assessed for the first treatment cycle."( Evaluation of safety, pharmacokinetics, and efficacy of vorinostat, a histone deacetylase inhibitor, in the treatment of gastrointestinal (GI) cancer in a phase I clinical trial.
Chin, K; Doi, T; Hamaguchi, T; Hatake, K; Mehta, A; Noguchi, K; Ohtsu, A; Otsuki, T; Shirao, K, 2013
)
0.64
"Herein, we describe the pharmacokinetic optimization of a series of class-selective histone deacetylase (HDAC) inhibitors and the subsequent identification of candidate predictive biomarkers of hepatocellular carcinoma (HCC) tumor response for our clinical lead using patient-derived HCC tumor xenograft models."( Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Cai, J; Chen, D; Chen, J; Chen, L; Chen, T; Feng, L; Guo, L; He, Y; Ji, Y; Jin, TG; Li, S; Liang, C; Lin, X; Liu, Y; Lu, X; Mei, J; Ning, Z; Pan, D; Pan, S; Peng, Z; Ren, S; Ren, Y; Rong, Y; Shan, S; She, J; Tang, G; Wang, Z; Wong, JC; Wu, X; Xu, C; Zhang, C; Zhang, M; Zhang, N; Zhang, W; Zhang, X; Zhang, Z; Zhao, R; Zhao, W; Zhou, M, 2012
)
0.38
" The pharmacodynamic effect of an increase in acetylated histone proteins in blood was detected after both routes of administration."( Pharmacokinetics and pharmacodynamics of suberoylanilide hydroxamic acid in cats.
McDonnel, SJ; Murphy, BG; Tell, LA, 2014
)
0.4
" The cytotoxicity of the optimized formulation was evaluated in cancer cell lines (MCF-7, A549, and MDA-MB-231), and pharmacokinetic parameters were examined following oral and intravenous (IV) administration to rats."( Development of vorinostat-loaded solid lipid nanoparticles to enhance pharmacokinetics and efficacy against multidrug-resistant cancer cells.
Choi, HG; Kim, JO; Ramasamy, T; Shin, BS; Tran, TH; Truong, DH; Yong, CS, 2014
)
0.76
" Pharmacokinetic studies clearly demonstrated that VOR-SLNs markedly improved VOR plasma circulation time and decreased its elimination rate constant."( Development of vorinostat-loaded solid lipid nanoparticles to enhance pharmacokinetics and efficacy against multidrug-resistant cancer cells.
Choi, HG; Kim, JO; Ramasamy, T; Shin, BS; Tran, TH; Truong, DH; Yong, CS, 2014
)
0.76
" Furthermore, compared with SAHA, MPT0G009 exhibited longer half-life (9."( Preclinical anti-arthritic study and pharmacokinetic properties of a potent histone deacetylase inhibitor MPT0G009.
Hsieh, IN; Lai, MJ; Lee, HY; Li, YH; Liou, JP; Yang, CR, 2014
)
0.4
" This study investigated the effects of complexing iron (Fe3+) to the HDACi suberoylanilide hydroxamic acid (SAHA) and LAQ824 (LAQ) prior to their encapsulation into PEGylated liposomes, and investigated whether this technique could improve drug solubility, in vitro release and in vivo pharmacokinetic (PK) properties."( Iron complexation to histone deacetylase inhibitors SAHA and LAQ824 in PEGylated liposomes can considerably improve pharmacokinetics in rats.
Steffen, D; Tu, S; Wang, Y; Xiong, M, 2014
)
0.4
" This study examines pharmacokinetic interactions in simultaneous oral administration of SAHA and lapatinib to rats."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.66
"Statistically significant pharmacokinetic differences appeared for lapatinib levels between the lapatinib and the coadministration group."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.66
"The resulting data indicate that, when administered together, lapatinib does not influence the pharmacokinetic profile of SAHA in rats, while, in contrast, SAHA influences the pharmacokinetic profile of lapatinib."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.66
" This model may be used as a mechanistic bridge to link vorinostat exposure to molecular events and pharmacodynamic (PD) outcomes."( Cell Signaling Model Connects Vorinostat Pharmacokinetics and Tumor Growth Response in Multiple Myeloma Xenografts.
Mager, DE; Nanavati, C; Ruszaj, D, 2017
)
0.99
" In pharmacokinetics assay, 23g showed a significant improvement of pharmacokinetic profile for oral administration."( Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
He, Z; Huang, J; Jiang, J; Li, C; Wang, J; Yao, D; Zhang, J, 2020
)
0.56
" Simulations revealed that the greatest magnitude of pharmacodynamic drug interactions between bortezomib and vorinostat occurred at caspase-9, AKT, and Bcl-2."( Cluster Gauss-Newton and CellNOpt Parameter Estimation in a Small Protein Signaling Network of Vorinostat and Bortezomib Pharmacodynamics.
Chen, T; Ghasemi, M; Mager, DE; Nguyen, VA; Niu, J, 2021
)
1.05

Compound-Compound Interactions

Vorinostat in combination with temozolomide is well tolerated in patients with HGG. The primary objective of this Phase I study was to determine the maximally tolerated dose (MTD) and safety.

ExcerptReferenceRelevance
"The primary objective of this study was to determine the recommended phase II doses of the novel histone deacetylase inhibitor vorinostat when administered in combination with carboplatin and paclitaxel."( Phase I and pharmacokinetic study of vorinostat, a histone deacetylase inhibitor, in combination with carboplatin and paclitaxel for advanced solid malignancies.
Argiris, AE; Belani, CP; Egorin, MJ; Lagattuta, TF; Musguire, LA; Parise, RA; Potter, DM; Ramalingam, SS; Ramananthan, RK; Ramanathan, RK; Stoller, RG; Zwiebel, JA, 2007
)
0.82
"Both schedules of vorinostat (400 mg oral qd x 14 days or 300 mg bd x 7 days) were tolerated well in combination with carboplatin (area under the concentration versus time curve = 6 mg/mL x min) and paclitaxel (200 mg/m(2))."( Phase I and pharmacokinetic study of vorinostat, a histone deacetylase inhibitor, in combination with carboplatin and paclitaxel for advanced solid malignancies.
Argiris, AE; Belani, CP; Egorin, MJ; Lagattuta, TF; Musguire, LA; Parise, RA; Potter, DM; Ramalingam, SS; Ramananthan, RK; Ramanathan, RK; Stoller, RG; Zwiebel, JA, 2007
)
0.95
" These results demonstrate that compound 2 and its combination with SAHA are potentially useful agents that warrant further preclinical development for treatment of prostate cancer."( Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
Belosay, A; Gediya, LK; Khandelwal, A; Njar, VC; Purushottamachar, P, 2008
)
0.35
" ABT-737 was ineffective against Emu-myc/Mcl-1 and Emu-myc/A1 cells either as a single agent or in combination with HDACi."( Defining the target specificity of ABT-737 and synergistic antitumor activities in combination with histone deacetylase inhibitors.
Alsop, AE; Banks, KM; Cluse, LA; Coomans, C; Johnstone, RW; Lindemann, RK; Newbold, A; Peart, MJ; Whitecross, KF; Wiegmans, A, 2009
)
0.35
" Etoposide combined with vorinostat was additive to synergistic, and the synergism became more pronounced when etoposide was given after vorinostat."( Preclinical studies of vorinostat (suberoylanilide hydroxamic acid) combined with cytosine arabinoside and etoposide for treatment of acute leukemias.
Carlton, D; Edelman, MJ; Fang, HB; Gojo, I; Nakanishi, T; Ross, DD; Sausville, EA; Shiozawa, K; Tan, M; Wang, WC, 2009
)
0.97
"These findings using two independent methods to assess drug combination effects provide a preclinical rationale for phase I trials of the sequential combination of vorinostat followed by ara-C and etoposide in patients with advanced or refractory leukemias."( Preclinical studies of vorinostat (suberoylanilide hydroxamic acid) combined with cytosine arabinoside and etoposide for treatment of acute leukemias.
Carlton, D; Edelman, MJ; Fang, HB; Gojo, I; Nakanishi, T; Ross, DD; Sausville, EA; Shiozawa, K; Tan, M; Wang, WC, 2009
)
0.86
" Moreover, in combination with 5-fluorouracil modulated by folinic acid (5FU-FA) or with Raltitrexed (RTX), both commonly used in the treatment of this disease, it showed a clear schedule-dependent synergistic antiproliferative interaction as demonstrated by calculating combination indexes."( Modulation of thymidilate synthase and p53 expression by HDAC inhibitor vorinostat resulted in synergistic antitumor effect in combination with 5FU or raltitrexed.
Avallone, A; Bruzzese, F; Budillon, A; Delrio, P; Di Gennaro, E; Leone, A; Pepe, S; Subbarayan, PR, 2009
)
0.59
"We conducted a phase I study to determine the maximum tolerated dose of vorinostat in combination with fixed doses of 5-fluorouracil (FU), leucovorin, and oxaliplatin (FOLFOX)."( A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin in patients with refractory colorectal cancer.
Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Pendyala, L; Ross, ME; Rustum, YM; Toth, K; Zwiebel, JA, 2009
)
0.83
"The maximum tolerated dose of vorinostat in combination with FOLFOX is 300 mg orally twice daily x 1 week every 2 weeks."( A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin in patients with refractory colorectal cancer.
Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Pendyala, L; Ross, ME; Rustum, YM; Toth, K; Zwiebel, JA, 2009
)
0.89
" This phase II randomized, double-blinded, placebo-controlled study evaluated the efficacy of vorinostat in combination with carboplatin and paclitaxel in patients with advanced-stage NSCLC."( Carboplatin and Paclitaxel in combination with either vorinostat or placebo for first-line therapy of advanced non-small-cell lung cancer.
Argiris, AE; Belani, CP; Espinoza-Delgado, I; Frankel, P; Gandara, DR; Gitlitz, B; Koczywas, M; Maitland, ML; Ramalingam, SS; Thomas, S; Vokes, EE, 2010
)
0.83
" In this study, we determined if vorinostat alone or in combination with EGCG imparts anti-proliferative effects against human melanoma cells."( Anti-melanoma effects of vorinostat in combination with polyphenolic antioxidant (-)-epigallocatechin-3-gallate (EGCG).
Nihal, M; Roelke, CT; Wood, GS, 2010
)
0.95
" This phase 1 study assessed the use of vorinostat combined with pelvic palliative radiotherapy for gastrointestinal carcinoma."( Vorinostat, a histone deacetylase inhibitor, combined with pelvic palliative radiotherapy for gastrointestinal carcinoma: the Pelvic Radiation and Vorinostat (PRAVO) phase 1 study.
Abrahamsen, TW; Dueland, S; Flatmark, K; Folkvord, S; Hole, KH; Johansen, M; Ree, AH; Seierstad, T, 2010
)
2.07
" The maximum-tolerated dose of vorinostat in combination with palliative radiotherapy was thus determined to be 300 mg once daily."( Vorinostat, a histone deacetylase inhibitor, combined with pelvic palliative radiotherapy for gastrointestinal carcinoma: the Pelvic Radiation and Vorinostat (PRAVO) phase 1 study.
Abrahamsen, TW; Dueland, S; Flatmark, K; Folkvord, S; Hole, KH; Johansen, M; Ree, AH; Seierstad, T, 2010
)
2.09
"Vorinostat can be safely combined with short-term pelvic palliative radiotherapy."( Vorinostat, a histone deacetylase inhibitor, combined with pelvic palliative radiotherapy for gastrointestinal carcinoma: the Pelvic Radiation and Vorinostat (PRAVO) phase 1 study.
Abrahamsen, TW; Dueland, S; Flatmark, K; Folkvord, S; Hole, KH; Johansen, M; Ree, AH; Seierstad, T, 2010
)
3.25
" HDACi have single-agent clinical activity in haematological malignancies and have synergistic anti-leukaemia activity when combined with anthracyclines in vitro."( A phase I study of vorinostat in combination with idarubicin in relapsed or refractory leukaemia.
Egorin, MJ; Espinoza-Delgado, I; Ferrajoli, A; Garcia-Manero, G; Holleran, JL; Kadia, TM; Kantarjian, HM; Madden, TL; Maddipotti, S; Newsome, W; Ravandi, F; Sanchez-Gonzalez, B; Schroeder, C; Thomas, DA; Yang, H; Zwiebel, JA, 2010
)
0.69
"We conducted a phase I clinical trial to determine the maximum tolerated dose (MTD) of daily or twice daily vorinostat x 3 days when combined with fixed doses of 5-fluorouracil (FU) and leucovorin every 2 weeks."( A phase I, pharmacokinetic, and pharmacodynamic study of two schedules of vorinostat in combination with 5-fluorouracil and leucovorin in patients with refractory solid tumors.
Diasio, RB; Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Muindi, JR; Wang, K; Zwiebel, JA, 2010
)
0.8
"The MTD of vorinostat in combination with sLV5FU2 is 1,700 mg orally once daily x 3 or 600 mg orally twice daily x 3 days every 2 weeks."( A phase I, pharmacokinetic, and pharmacodynamic study of two schedules of vorinostat in combination with 5-fluorouracil and leucovorin in patients with refractory solid tumors.
Diasio, RB; Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Muindi, JR; Wang, K; Zwiebel, JA, 2010
)
0.98
" Vorinostat and docetaxel pharmacokinetics were comparable to previous reports in the literature, without obvious drug-drug interactions."( Phase I study of vorinostat (suberoylanilide hydroxamic acid, NSC 701852) in combination with docetaxel in patients with advanced and relapsed solid malignancies.
Bradley, D; Daignault, S; Dunn, R; Egorin, MJ; Hussain, M; Kalemkerian, GP; Schneider, BJ; Smith, DC, 2012
)
1.63
"To clarify the source of deviations of drug combination effects evaluated with different drug interaction mathematical models, the cytotoxicity of SAHA and arsenic trioxide and their combinations were observed in a series of human cancer cell lines and a normal cell line."( [Three different drug interaction mathematical models used to evaluate the cytotoxicity of SAHA and arsenic trioxide in combination].
Liu, ZJ; Lu, N; Wang, N; Yan, Z, 2010
)
0.36
" The objective of this study was to investigate the effects of 1,25(OH)(2)D(3) and the superagonistic analog CD578 in anaplastic thyroid cancer, alone or in combination with paclitaxel, a taxane, and suberoylanilide hydroxamic acid (SAHA), a potent histone deacetylase inhibitor with promising effects in undifferentiated thyroid cancer."( 1,25-dihydroxyvitamin D3 and a superagonistic analog in combination with paclitaxel or suberoylanilide hydroxamic acid have potent antiproliferative effects on anaplastic thyroid cancer.
Bouillon, R; Clinckspoor, I; Decallonne, B; Korch, C; Mathieu, C; Overbergh, L; Verlinden, L; Verstuyf, A, 2011
)
0.37
" Herein, we demonstrate that HDACi can be combined with immune-activating antibodies designed to promote the function of antigen-presenting cells (APCs) and enhance proliferation and survival of cytotoxic T cells (CTL) to stimulate a host antitumor immune response resulting in eradication of established solid tumors."( Eradication of solid tumors using histone deacetylase inhibitors combined with immune-stimulating antibodies.
Banks, KM; Christiansen, AJ; Haynes, NM; Johnstone, RW; Smyth, MJ; Teng, MW; West, A, 2011
)
0.37
" We aim to evaluate the activity of vorinostat in combination with interferon (IFN) alpha and extracorporeal photopheresis (ECP) with persistent, progressive advanced stage MF and Sezary syndrome (SS)."( The efficacy of vorinostat in combination with interferon alpha and extracorporeal photopheresis in late stage mycosis fungoides and Sezary syndrome.
Akay, BN; Akyol, A; Anadolu, R; Ozcan, M; Sanli, H; Saral, S, 2011
)
0.99
"Our experience in this case series is suggestive of the synergistic effect of vorinostat in combination with IFN and ECP and supports the efficacy of vorinostat in inducing prolonged responses in patients with progressive disease and/or stable disease in otherwise progressive and treatment refractory late stage MF/SS."( The efficacy of vorinostat in combination with interferon alpha and extracorporeal photopheresis in late stage mycosis fungoides and Sezary syndrome.
Akay, BN; Akyol, A; Anadolu, R; Ozcan, M; Sanli, H; Saral, S, 2011
)
0.94
" Mechanistically, SAHA combined with bortezomib enhanced protein ubiquitination synergistically and enhanced histone acetylation by inhibiting the expression of HDACs."( Suberoylanilide hydroxamic acid (SAHA) combined with bortezomib inhibits renal cancer growth by enhancing histone acetylation and protein ubiquitination synergistically.
Asano, T; Ito, K; Sato, A; Sumitomo, M, 2012
)
0.38
"SAHA combined with bortezomib inhibits the proliferation of renal cancer cells in vitro and in vivo, and the effectiveness of the combination is due to its synergistic enhancement of histone acetylation and protein ubiquitination."( Suberoylanilide hydroxamic acid (SAHA) combined with bortezomib inhibits renal cancer growth by enhancing histone acetylation and protein ubiquitination synergistically.
Asano, T; Ito, K; Sato, A; Sumitomo, M, 2012
)
0.38
" Vorinostat was combined with bevacizumab and CPT-11 and was escalated using a standard 3 + 3 design."( Phase I trial of vorinostat combined with bevacizumab and CPT-11 in recurrent glioblastoma.
Brem, S; Chinnaiyan, P; Chowdhary, S; Kahali, S; Murtagh, R; Pan, E; Potthast, L; Prabhu, A; Rojiani, A; Sarcar, B; Tsai, YY; Yu, HM, 2012
)
1.63
" Primary objective was to determine maximum tolerated dose (MTD) of vorinostat, a competitive inhibitor of histone deacetylase (HDAC), in combination with vinorelbine."( Unexpected high levels of vorinostat when combined with vinorelbine in patients with advanced cancer.
Arellano, C; Campone, M; Chalret du Rieu, Q; Chatelut, E; Delord, JP; Filleron, T; Gandia, P; Hennebelle, I; Lochon, I; Pierga, JY; Poublanc, M, 2011
)
0.9
"Starting dose of once daily oral vorinostat was 200 mg for 7 days every 21 days in combination with a 20-min intraveinous weekly infusion of vinorelbine 25 mg/m2, starting 4 hours after the first vorinostat dose."( Unexpected high levels of vorinostat when combined with vinorelbine in patients with advanced cancer.
Arellano, C; Campone, M; Chalret du Rieu, Q; Chatelut, E; Delord, JP; Filleron, T; Gandia, P; Hennebelle, I; Lochon, I; Pierga, JY; Poublanc, M, 2011
)
0.95
" Mean vorinostat plasma AUC was higher than reported previously at a similar dose when used as single agent or in combination with other cytotoxics."( Unexpected high levels of vorinostat when combined with vinorelbine in patients with advanced cancer.
Arellano, C; Campone, M; Chalret du Rieu, Q; Chatelut, E; Delord, JP; Filleron, T; Gandia, P; Hennebelle, I; Lochon, I; Pierga, JY; Poublanc, M, 2011
)
1.15
"MDT of the combination was 200 mg oral vorinostat for 7 days in combination with 25 mg/m2 weekly vinorelbine."( Unexpected high levels of vorinostat when combined with vinorelbine in patients with advanced cancer.
Arellano, C; Campone, M; Chalret du Rieu, Q; Chatelut, E; Delord, JP; Filleron, T; Gandia, P; Hennebelle, I; Lochon, I; Pierga, JY; Poublanc, M, 2011
)
0.94
" We therefore conducted a phase II trial to evaluate the efficacy of vorinostat in combination with the proteasome inhibitor bortezomib in patients with recurrent GBM."( Phase II trial of vorinostat in combination with bortezomib in recurrent glioblastoma: a north central cancer treatment group study.
Anderson, SK; Buckner, J; Friday, BB; Galanis, E; Geoffroy, F; Giannini, C; Gross, H; Jaeckle, K; Mazurczak, M; Pajon, E; Schwerkoske, J; Yu, C, 2012
)
0.95
"Potential radiosensitization by SAHA was assessed in MRT xenografts by analysis of tumor growth delay, necrosis (HE), apoptosis (TUNEL), proliferation (ki-67) and γH2AX expression as well as dynamic 18F-Fluorodeoxyglucose Positron Emission Tomography (18F-FDG -PET) after treatment with either SAHA alone, single-dose (10 Gy) or fractionated XRT (3 × 3Gy) solely as well as in combination with SAHA compared to controls."( In vivo efficacy of the histone deacetylase inhibitor suberoylanilide hydroxamic acid in combination with radiotherapy in a malignant rhabdoid tumor mouse model.
Battmann, C; Bischof, M; Debus, J; Ehemann, V; Haberkorn, U; Huber, PE; Kulozik, AE; Oertel, S; Perez, RL; Stenzinger, A; Thiemann, M; Weber, KJ; Weichert, W, 2012
)
0.38
"A phase I, dose-finding study of vorinostat in combination with temozolomide (TMZ) was conducted to determine the maximum tolerated dose (MTD), safety, and pharmacokinetics in patients with high-grade glioma (HGG)."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
1
" Part 1 was a dose-escalation study of vorinostat in combination with TMZ 150 mg/m(2)/day for 5 days every 28 days."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
0.99
"In part 1, the MTD of vorinostat administered on days 1 to 7 and 15 to 21 of every 28-day cycle, in combination with TMZ, was 500 mg daily."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
1.03
"Vorinostat in combination with temozolomide is well tolerated in patients with HGG."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
2.16
" We examined this drug combination in advanced relapsing and/or refractory MM patients (n = 34)."( Phase I trial of vorinostat combined with bortezomib for the treatment of relapsing and/or refractory multiple myeloma.
Graef, T; Hardwick, JS; Hussein, M; Jagannath, S; Lupinacci, L; Schiller, GJ; Sobecks, RM; Weber, DM, 2012
)
0.72
" Vorinostat combined with bortezomib has demonstrated synergistic antiproliferative and proapoptotic activity in preclinical models of MM."( Phase I trial of vorinostat combined with bortezomib for the treatment of relapsing and/or refractory multiple myeloma.
Graef, T; Hardwick, JS; Hussein, M; Jagannath, S; Lupinacci, L; Schiller, GJ; Sobecks, RM; Weber, DM, 2012
)
1.63
" In xenograft models, while gefitinib induced marked regression via apoptosis of tumors without the BIM polymorphism, its combination with vorinostat was needed to induce marked regression of tumors with the BIM polymorphism in the same manner."( EGFR-TKI resistance due to BIM polymorphism can be circumvented in combination with HDAC inhibition.
Ebi, H; Hasegawa, Y; Ishikawa, D; Nakagawa, T; Nanjo, S; Sano, T; Sato, M; Sekido, Y; Takeuchi, S; Yamada, T; Yano, S, 2013
)
0.59
"To determine the maximum-tolerated dose (MTD) of the histone deacetylase inhibitor vorinostat combined with fixed doses of cytarabine (ara-C or cytosine arabinoside) and etoposide in patients with poor-risk or advanced acute leukemia, to obtain preliminary efficacy data, describe pharmacokinetics, and in vivo pharmacodynamic effects of vorinostat in leukemia blasts."( Translational phase I trial of vorinostat (suberoylanilide hydroxamic acid) combined with cytarabine and etoposide in patients with relapsed, refractory, or high-risk acute myeloid leukemia.
Anyang, BN; Baer, MR; Beumer, JH; Carrier, F; Espinoza-Delgado, I; Fang, HB; Gojo, I; Lapidus, R; Ross, DD; Sadowska, M; Srivastava, RK; Tan, M, 2013
)
0.9
"A phase I trial of first-line vorinostat, an orally bio-available histone deacetylase inhibitor, in combination with capecitabine plus cisplatin (XP) was performed to assess recommend phase II trial dose in patients with advanced gastric cancer."( Phase I and pharmacodynamic study of vorinostat combined with capecitabine and cisplatin as first-line chemotherapy in advanced gastric cancer.
Kang, YK; Kim, SY; Koo, DH; Lee, CW; Maeng, J; Na, YS; Park, I; Ryoo, BY; Ryu, MH; Yoo, C, 2014
)
0.96
" Therefore, we studied the effect of polo-like kinase 1 (Plk1) inhibitors on prostate cancer cells as a single agent and in combination with histone deacetylase (HDAC) inhibitors valproic acid and vorinostat."( Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors.
Carducci, MA; Gonzalez, M; Hammers, H; Kachhap, SK; Kaelber, NS; Kim, E; Kortenhorst, MS; Mendonca, J; van Diest, PJ; Wissing, MD, 2013
)
0.58
"We aimed to assess efficacy and tolerability of vorinostat in combination with bortezomib for treatment of patients with relapsed or refractory multiple myeloma."( Vorinostat or placebo in combination with bortezomib in patients with multiple myeloma (VANTAGE 088): a multicentre, randomised, double-blind study.
Anderson, KC; Blacklock, H; Dimopoulos, M; Eid, JE; Facon, T; Goldschmidt, H; Graef, T; Hajek, R; Houp, J; Hungria, V; Lonial, S; Palumbo, A; Qi, J; Rosinol, L; Siegel, DS; Spencer, A; Sun, L; Vuocolo, S; Williams, C, 2013
)
2.09
" We randomly allocated patients (1:1) using an interactive voice response system to receive 21 day cycles of bortezomib (1·3 mg/m(2) intravenously on days 1, 4, 8, and 11) in combination with oral vorinostat (400 mg) or matching placebo once-daily on days 1-14."( Vorinostat or placebo in combination with bortezomib in patients with multiple myeloma (VANTAGE 088): a multicentre, randomised, double-blind study.
Anderson, KC; Blacklock, H; Dimopoulos, M; Eid, JE; Facon, T; Goldschmidt, H; Graef, T; Hajek, R; Houp, J; Hungria, V; Lonial, S; Palumbo, A; Qi, J; Rosinol, L; Siegel, DS; Spencer, A; Sun, L; Vuocolo, S; Williams, C, 2013
)
2.02
"A phase I study to assess the maximum-tolerated dose (MTD), dose-limiting toxicity (DLT), pharmacokinetics (PK) and antitumor activity of vorinostat in combination with bortezomib in patients with advanced solid tumors."( A phase I study of vorinostat in combination with bortezomib in patients with advanced malignancies.
Alberti, D; Ames, MM; Attia, S; Bailey, HH; Eickhoff, J; Espinoza-Delgado, I; Hoang, T; Holen, KD; Jiang, Z; Kolesar, JM; Marnocha, R; McGovern, RM; Reid, JM; Schelman, WR; Traynor, AM; Wilding, G; Wright, JJ, 2013
)
0.92
" We previously examined a once-daily continuous dosing schedule of vorinostat in combination with bortezomib which was well tolerated in cycles 1 and 2; however, there was concern regarding the tolerability through multiple cycles."( A Phase I study of intermittently dosed vorinostat in combination with bortezomib in patients with advanced solid tumors.
Alberti, D; Ames, MM; Bailey, HH; Deming, DA; Eickhoff, J; Espinoza-Delgado, I; Kolesar, JM; Marnocha, R; McGovern, RM; Ninan, J; Reid, JM; Schelman, WR; Wilding, G; Wright, J, 2014
)
0.91
" In conclusion, the poor results obtained with lenalidomide in combination with vorinostat and dexamethasone provide no arguments that could justify further investigation of this drug combination for the treatment of relapsed PTCL."( Lenalidomide in combination with vorinostat and dexamethasone for the treatment of relapsed/refractory peripheral T cell lymphoma (PTCL): report of a phase I/II trial.
Egle, A; Greil, R; Hopfinger, G; Lang, A; Linkesch, W; Melchardt, T; Nösslinger, T; Weiss, L, 2014
)
0.91
" Patients were treated orally with escalating doses of HCQ daily (QD) (d 2 to 21 of a 21-d cycle) in combination with 400 mg VOR QD (d one to 21)."( Combined autophagy and HDAC inhibition: a phase I safety, tolerability, pharmacokinetic, and pharmacodynamic analysis of hydroxychloroquine in combination with the HDAC inhibitor vorinostat in patients with advanced solid tumors.
Amaravadi, RK; Carew, JS; Curiel, TJ; Davis, LE; Espitia, CM; Giles, FJ; Mahalingam, D; Mita, AC; Mita, M; Nawrocki, ST; Sarantopoulos, J; Wood, L, 2014
)
0.59
" The aim of the study presented here was to analyze the effects of a pharmacological inhibition of EZH2 alone and in combination with other anticancer drugs on RTs cells in vitro."( Analysis of the antiproliferative effects of 3-deazaneoplanocin A in combination with standard anticancer agents in rhabdoid tumor cell lines.
Borchardt, C; Clemens, D; Dirksen, U; Frühwald, MC; Kool, M; Unland, R, 2015
)
0.42
" We investigated the efficacy of the histone deacetylase (HDAC) inhibitor vorinostat combined with one of several B-cell receptor (BCR) signaling inhibitors on MCL cell death and the underlying mechanisms, using MCL cell lines."( The synergistic effect of BCR signaling inhibitors combined with an HDAC inhibitor on cell death in a mantle cell lymphoma cell line.
Hagiwara, K; Iida, H; Kunishima, S; Miyata, Y; Nagai, H; Naoe, T, 2015
)
0.65
" In this study, we analysed the effects of the pan-aurora kinases inhibitor AMG 900 alone or in combination with the iHDAC SaHa (Vorinostat) on paediatric MB cell lines (UW402, UW473 and ONS-76)."( Antitumour activity of AMG 900 alone or in combination with histone deacetylase inhibitor SaHa on medulloblastoma cell lines.
Andrade, AF; Borges, KS; Geron, L; Scrideli, CA; Suazo, VK; Tone, LG, 2015
)
0.62
" Drug combination analyses were made based on Chou-Talalay method."( Antitumour activity of AMG 900 alone or in combination with histone deacetylase inhibitor SaHa on medulloblastoma cell lines.
Andrade, AF; Borges, KS; Geron, L; Scrideli, CA; Suazo, VK; Tone, LG, 2015
)
0.42
"These results indicate that AMG 900 may be a promising drug for the adjuvant treatment of MB, mainly when combined with iHDAC."( Antitumour activity of AMG 900 alone or in combination with histone deacetylase inhibitor SaHa on medulloblastoma cell lines.
Andrade, AF; Borges, KS; Geron, L; Scrideli, CA; Suazo, VK; Tone, LG, 2015
)
0.42
" We performed an open-label, multi-center, phase II study to investigate the effect and quality of life (QoL) of treatment with vorinostat in combination with fludarabine, mitoxantrone and dexamethasone (V-FND) for relapsed or refractory MCL."( Results of a phase II study of vorinostat in combination with intravenous fludarabine, mitoxantrone, and dexamethasone in patients with relapsed or refractory mantle cell lymphoma: an interim analysis.
Kim, BS; Kim, HJ; Kim, JA; Kim, SJ; Kim, WS; Kong, JH; Park, SK; Park, Y; Shin, DY; Won, JH; Yoon, DH, 2016
)
0.93
"The present global, open-label, single-arm, multicenter, phase IIb study was designed to determine the efficacy and tolerability of oral vorinostat combined with standard doses of bortezomib in patients with multiple myeloma considered refractory to novel myeloma agents."( VANTAGE 095: An International, Multicenter, Open-Label Study of Vorinostat (MK-0683) in Combination With Bortezomib in Patients With Relapsed and Refractory Multiple Myeloma.
Anderson, KC; Dimopoulos, M; Durrant, S; Eid, JE; Gause, C; Goldschmidt, H; Graef, T; Houp, J; Jagannath, S; Kaufman, JL; Leleu, X; Nagler, A; Offner, F; Siegel, DS; Vuocolo, S, 2016
)
0.88
"Vorinostat, a histone deacetylase (HDAC) inhibitor, was investigated in combination with capecitabine plus cisplatin (XP) as a first-line chemotherapy for patients with unresectable or metastatic gastric cancer (GC)."( Vorinostat in combination with capecitabine plus cisplatin as a first-line chemotherapy for patients with metastatic or unresectable gastric cancer: phase II study and biomarker analysis.
Kang, YK; Lee, CW; Na, YS; Ryoo, BY; Ryu, MH; Yoo, C, 2016
)
3.32
" Here, we report in vivo data for OTX015 in combination with the histone deacetylase inhibitor vorinostat, the Bruton's tyrosine kinase inhibitor ibrutinib, the anti-CD20 monoclonal antibody rituximab, and the mTOR inhibitor everolimus in a diffuse large B cell lymphoma model."( Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma.
Bernasconi, E; Bertoni, F; Cascione, L; Cvitkovic, E; Gaudio, E; Odore, E; Ponzoni, M; Rezai, K; Rinaldi, A; Riveiro, E; Stathis, A; Tarantelli, C; Zucca, E, 2016
)
0.65
"Clinical trials of vorinostat, a Class I/II histone deacetylase inhibitor, in combination with proteasome inhibitors and immunomodulatory agents have shown activity in relapsed/refractory multiple myeloma."( A phase IIb trial of vorinostat in combination with lenalidomide and dexamethasone in patients with multiple myeloma refractory to previous lenalidomide-containing regimens.
Anand, P; Bilotti, E; Biran, N; Ivanovski, K; McBride, L; Richter, JR; Sanchez, L; Siegel, DS; Vesole, DH, 2017
)
1.1
"In patients with HER2-positive metastatic breast cancer who had relapsed or progressed during trastuzumab therapy, we observed no DLTs with SAHA 200 mg twice daily combined with trastuzumab; however, there was insufficient statistical evidence that adding SAHA reversed trastuzumab resistance in these patients."( A Phase I/II study of suberoylanilide hydroxamic acid (SAHA) in combination with trastuzumab (Herceptin) in patients with advanced metastatic and/or local chest wall recurrent HER2-amplified breast cancer: a trial of the ECOG-ACRIN Cancer Research Group (
Bhalla, KN; Falkson, CI; Goldstein, LJ; Katherine Alpaugh, R; Klein, P; Meropol, NJ; Pellegrino, CM; Sledge, GW; Sparano, JA; Swaby, RF; Wang, M; Zhao, F, 2017
)
0.46
" Consistent additive to synergistic interactions were observed in HCT116 cells when PENT was combined with SAHA at all drug tested concentrations."( Enhanced anticancer efficacy of histone deacetyl inhibitor, suberoylanilide hydroxamic acid, in combination with a phosphodiesterase inhibitor, pentoxifylline, in human cancer cell lines and in-vivo tumor xenografts.
Chandrasekhar, KB; Karthikeyan, K; Khan, FR; Kulkarni, NM; Narayanan, S; Nidhyanandan, S; Raghul, J; Reddy, ND; Thippeswamy, BS; Vijaykanth, G, 2017
)
0.46
" This open-label, single-arm trial evaluated the maximum tolerated dose (MTD; phase I) and efficacy (phase II) of vorinostat combined with standard chemoradiation in newly diagnosed glioblastoma."( Phase I/II trial of vorinostat combined with temozolomide and radiation therapy for newly diagnosed glioblastoma: results of Alliance N0874/ABTC 02.
Ahluwalia, MS; Anderson, SK; Ballman, KV; Buckner, JC; Cerhan, J; Galanis, E; Gerstner, ER; Giannini, C; Grossman, SA; Jaeckle, K; Lee, EQ; Lesser, GJ; Ligon, KL; Loboda, A; Miller, CR; Moore, DF; Nebozhyn, M; Prados, M; Sarkaria, JN; Schiff, D; Wen, PY, 2018
)
1.01
"Vorinostat combined with standard chemoradiation had acceptable tolerability in newly diagnosed glioblastoma."( Phase I/II trial of vorinostat combined with temozolomide and radiation therapy for newly diagnosed glioblastoma: results of Alliance N0874/ABTC 02.
Ahluwalia, MS; Anderson, SK; Ballman, KV; Buckner, JC; Cerhan, J; Galanis, E; Gerstner, ER; Giannini, C; Grossman, SA; Jaeckle, K; Lee, EQ; Lesser, GJ; Ligon, KL; Loboda, A; Miller, CR; Moore, DF; Nebozhyn, M; Prados, M; Sarkaria, JN; Schiff, D; Wen, PY, 2018
)
2.25
" S0806 was a single arm phase I/II trial of vorinostat given at 400 mg po daily on days 1-9 (subsequently amended to days 1-5 due to toxicity), combined with R-CHOP given on day 3 of a 21-day cycle for 8 cycles, with primary phase II endpoint of 2-year progression free survival (PFS)."( A phase I/II trial of vorinostat (SAHA) in combination with rituximab-CHOP in patients with newly diagnosed advanced stage diffuse large B-cell lymphoma (DLBCL): SWOG S0806.
Bane, CL; Barr, PM; Fisher, RI; Friedberg, JW; LeBlanc, M; Li, H; Persky, DO; Popplewell, LL; Rimsza, LM; Smith, SM; Von Gehr, A, 2018
)
1.06
" The primary objective of this Phase I study was to determine the maximally tolerated dose (MTD) and safety of Vorinostat in combination with standard chemoradiation therapy treatment in HNSCC."( A phase 1 trial of Vorinostat in combination with concurrent chemoradiation therapy in the treatment of advanced staged head and neck squamous cell carcinoma.
Agrawal, A; Baiocchi, R; Blakaj, D; Carrau, R; Diavolitsis, V; Grecula, J; Kang, S; Kumar, B; Kumar, P; Old, MO; Ozer, E; Palettas, M; Pan, Q; Rocco, J; Savvides, P; Teknos, TN; Wei, L, 2019
)
1.05
" However, the efficacy and underlying toxicity of these hybrids in combination with other agents remain unclear."( Novel SAHA‑bendamustine hybrid NL‑101 in combination with daunorubicin synergistically suppresses acute myeloid leukemia.
Guo, W; Huang, J; Huang, S; Huang, X; Jin, J; Li, F; Li, X; Ling, Q; Pan, J; Ye, W, 2020
)
0.56
"This study was conducted to identify novel therapeutic targets that can be combined with HDACis for treating CTCL."( Kinome profiling analysis identified Src pathway as a novel therapeutic target in combination with histone deacetylase inhibitors for cutaneous T-cell lymphoma.
Fujii, K; Jimura, N; Kanekura, T; Kondo, T; Qiao, Z; Tsuchiya, R; Yoshimatsu, Y, 2021
)
0.62
" Vorinostat combined with brigatinib significantly improved EGFR-TKI sensitivity to EGFR C797S by inducing EGFR-dependent cell death and may be a promising therapy in treating C797S-resistant lung adenocarcinomas."( Vorinostat combined with brigatinib overcomes acquired resistance in EGFR-C797S-mutated lung cancer.
Chang, YH; Chang, YL; Chung, WC; Ho, CC; Huang, KY; Kao, SH; Lin, CA; Lin, CY; Lin, YC; Shih, CC; Shih, JY; Yang, PC; Yang, SC, 2021
)
2.97
" Here we explored the impact of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) on somatic hyperalgesia induced by stress or stress combined with orofacial inflammation, which mimicked the comorbidity of FMS and TMD in rats."( SAHA Inhibits Somatic Hyperalgesia Induced by Stress Combined with Orofacial Inflammation Through Targeting Different Spinal 5-HT Receptor Subtypes.
Bai, G; Cao, DY; Li, JF; Qiu, XY; Tao, ZY; Wei, SQ, 2022
)
0.72
" Platinum-based drugs have been used in multiple clinical trials as monotherapy or in combination with other chemotherapeutic agents for the treatment of CRPC."( Combination with vorinostat enhances the antitumor activity of cisplatin in castration-resistant prostate cancer by inhibiting DNA damage repair pathway and detoxification of GSH.
Chang, T; Lian, Z; Liang, Z; Liu, R; Ma, S; Ma, X; Wang, Y; Wen, X, 2023
)
1.25
" The efficacy and safety of SAHA combined with CDDP in the treatment of CRPC were further verified through animal experiments."( Combination with vorinostat enhances the antitumor activity of cisplatin in castration-resistant prostate cancer by inhibiting DNA damage repair pathway and detoxification of GSH.
Chang, T; Lian, Z; Liang, Z; Liu, R; Ma, S; Ma, X; Wang, Y; Wen, X, 2023
)
1.25
" We evaluated the potential drug combinations that interact the most with hub genes and hence have the most potential to reverse the disease process."( Drug repurposing based on differentially expressed genes suggests drug combinations with possible synergistic effects in treatment of lung adenocarcinoma.
Teimourian, S; Yesharim, L, 2023
)
0.91

Bioavailability

Vorinostat possessed high serum clearance, a short elimination half-life and low oral bioavailability in both species. No differences were noted in the pharmacokinetics of vorinstat at the 800- or 1,400-mg dose-levels, suggesting bioavailability saturation.

ExcerptReferenceRelevance
"(S)-HDAC-42 is a potent orally bioavailable inhibitor of HDAC, as well as targets regulating multiple aspects of cancer cell survival, which might have clinical value in prostate cancer chemotherapy and warrants further investigation in this regard."( Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer.
Chen, CS; Chen, CY; Kulp, SK; Wang, DS, 2006
)
0.33
" A high-fat meal increased the extent and modestly decreased the rate of absorption of vorinostat; this effect is not anticipated to be clinically meaningful."( A study to determine the effects of food and multiple dosing on the pharmacokinetics of vorinostat given orally to patients with advanced cancer.
Agrawal, NG; Du, L; Frankel, SR; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Mazina, KE; Ricker, JL; Rubin, EH; Scott, P; Sun, L; Wagner, JA, 2006
)
0.78
"In vitro liver microsomal stability, permeability, pharmacokinetics (PK) and oral bioavailability of SB639, a novel HDACi (Histone Deacetylase inhibitor), were determined."( In vitro phase I cytochrome P450 metabolism, permeability and pharmacokinetics of SB639, a novel histone deacetylase inhibitor in preclinical species.
Goh, E; Kantharaj, E; New, LS; Pasha, MK; Sangthongpitag, K; Venkatesh, PR; Xin, L; Yeo, P; Zeng, P, 2007
)
0.34
"OSU-HDAC42 is a potent, orally bioavailable inhibitor of HDAC with a broad spectrum of antitumor activity that includes targets regulating multiple aspects of cancer cell survival."( Efficacy of a novel histone deacetylase inhibitor in murine models of hepatocellular carcinoma.
Chen, CS; Chen, TJ; Cheng, AL; Hung, JH; Kashida, Y; Kulp, SK; Lin, ZZ; Lu, YS; Tang, M; Wang, D; Wang, YC, 2007
)
0.34
"The present investigation was undertaken to characterize the pharmacokinetics and oral bioavailability of Kendine 91 in mice and to compare it with other HDAC (histone deacetylases) inhibitors."( Pharmacokinetics and tissue distribution of Kendine 91, a novel histone deacetylase inhibitor, in mice.
Cossío, FP; Otaegui, D; Pedraz, JL; Rodríguez-Gascón, A; Zubia, A, 2009
)
0.35
" Absolute oral bioavailability was found to be 18%."( Pharmacokinetics and tissue distribution of Kendine 91, a novel histone deacetylase inhibitor, in mice.
Cossío, FP; Otaegui, D; Pedraz, JL; Rodríguez-Gascón, A; Zubia, A, 2009
)
0.35
" Vorinostat possessed high serum clearance, a short elimination half-life and low oral bioavailability in both species."( Disposition of vorinostat, a novel histone deacetylase inhibitor and anticancer agent, in preclinical species.
Andrews, PA; Baillie, TA; Baker, MP; Koeplinger, KA; Miller, T; Sandhu, P; Soli, ED, 2007
)
1.6
"A novel series of HDAC inhibitors demonstrating class I subtype selectivity and good oral bioavailability is described."( Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
Aherne, W; Bawden, L; Belfield, A; Bone, E; Box, G; Brotherton, D; Clark, V; Day, F; Donald, A; Eccles, S; Hardcastle, A; Moffat, D; Mortenson, P; Owen, J; Patel, S; Raynaud, F; Rowlands, M; Stimson, L; van Meurs, S; Wibawa, J, 2010
)
0.36
" This work resulted in the discovery of spirocycle 30d that shows good oral bioavailability and tumor growth inhibition in an HCT-116 murine xenograft model."( Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
Abate, A; Bigogno, C; Boggio, R; Carenzi, G; Cataudella, T; Dal Zuffo, R; Dondio, G; Fulco, MC; Mai, A; Mercurio, C; Minucci, S; Rozio, MG; Thaler, F; Varasi, M, 2011
)
0.37
" No differences were noted in the pharmacokinetics of vorinostat at the 800- or 1,400-mg dose-levels, suggesting bioavailability saturation."( A randomized phase II study of two doses of vorinostat in combination with 5-FU/LV in patients with refractory colorectal cancer.
Fakih, MG; Groman, A; McMahon, J; Muindi, JR; Wilding, G, 2012
)
0.89
" The pharmaceutical properties (LogD, solubility, liver micrsomal stability (t1/2), plasma stability (t1/2), and apparent permeability) strongly suggested that NK-HDAC-1 might be superior to SAHA in bioavailability and in vivo half-life."( Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
Fang, Q; Feng, C; Gu, G; Guo, W; Hou, J; Li, Z; Lin, J; Liu, P; Liu, R; Shen, J; Shi, YK; Tian, Y; Wang, H; Wang, PG; Yin, Z; Zhang, H, 2012
)
0.38
" pharmacokinetics and bioavailability of vorinostat, which warrants further investigation."( Vorinostat with sustained exposure and high solubility in poly(ethylene glycol)-b-poly(DL-lactic acid) micelle nanocarriers: characterization and effects on pharmacokinetics in rat serum and urine.
Borg, TM; Davies, NM; Foda, AM; Forrest, ML; Martinez, SE; Meshali, MM; Mohamed, EA; Remsberg, CM; Sayre, CL; Takemoto, JK; Zhao, Y, 2012
)
2.09
" Through a combination of conformational constraint and scaffold hopping, we lowered the in vivo clearance (CL) and significantly improved the bioavailability (F) and exposure (AUC) of our HDAC inhibitors while maintaining selectivity toward the class I HDAC family with particular potency against HDAC1, resulting in clinical lead 5 (HDAC1 IC₅₀ = 60 nM, mouse CL = 39 mL/min/kg, mouse F = 100%, mouse AUC after single oral dose at 10 mg/kg = 6316 h·ng/mL)."( Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Cai, J; Chen, D; Chen, J; Chen, L; Chen, T; Feng, L; Guo, L; He, Y; Ji, Y; Jin, TG; Li, S; Liang, C; Lin, X; Liu, Y; Lu, X; Mei, J; Ning, Z; Pan, D; Pan, S; Peng, Z; Ren, S; Ren, Y; Rong, Y; Shan, S; She, J; Tang, G; Wang, Z; Wong, JC; Wu, X; Xu, C; Zhang, C; Zhang, M; Zhang, N; Zhang, W; Zhang, X; Zhang, Z; Zhao, R; Zhao, W; Zhou, M, 2012
)
0.38
" Two representative examples exhibited a good pharmacokinetic profile with an oral bioavailability equal or higher than 35% and one of them studied in an HCT116 murine xenograft model showing a robust tumour growth inhibition."( Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
Abate, A; Bigogno, C; Boggio, R; Carenzi, G; Colombo, A; Dondio, G; Gagliardi, S; Mercurio, C; Minucci, S; Rapetti, D; Regalia, N; Resconi, A; Thaler, F; Varasi, M; Vultaggio, S; Zuffo, RD, 2013
)
0.39
"To investigate whether delivery of a histone deacetylase inhibitor, vorinostat (VOR), by using solid lipid nanoparticles (SLNs) enhanced its bioavailability and effects on multidrug-resistant cancer cells."( Development of vorinostat-loaded solid lipid nanoparticles to enhance pharmacokinetics and efficacy against multidrug-resistant cancer cells.
Choi, HG; Kim, JO; Ramasamy, T; Shin, BS; Tran, TH; Truong, DH; Yong, CS, 2014
)
0.99
" These in vivo results clearly highlighted the remarkable potential of SLNs to augment the bioavailability of VOR."( Development of vorinostat-loaded solid lipid nanoparticles to enhance pharmacokinetics and efficacy against multidrug-resistant cancer cells.
Choi, HG; Kim, JO; Ramasamy, T; Shin, BS; Tran, TH; Truong, DH; Yong, CS, 2014
)
0.76
" There are several potential mechanisms by which histone deacetylase inhibition may alter dapsone metabolism including changes in hepatic acetylation or N-glucuronidation leading to an increase in the bioavailability of dapsone's hematotoxic metabolites."( Hemolytic anemia in two patients with glioblastoma multiforme: A possible interaction between vorinostat and dapsone.
Harmon, M; Lesser, GJ; Lewis, JA; Owen, J; Peacock, JE; Petty, WJ; Pirmohamed, M; Valente, K, 2015
)
0.64
"53 h for oral administration) and higher oral bioavailability (13%) in rats."( Preclinical anti-arthritic study and pharmacokinetic properties of a potent histone deacetylase inhibitor MPT0G009.
Hsieh, IN; Lai, MJ; Lee, HY; Li, YH; Liou, JP; Yang, CR, 2014
)
0.4
" It has a good pharmacokinetic profile with oral bioavailability of 33%."( Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
Chang, CY; Chang, JY; Chen, MC; Cheng, YC; Kuo, CC; Lee, HY; Liou, JP; Liu, JF; Liu, YM; Pan, SL; Shen, PJ; Tsai, AC; Wang, JC; Yeh, TK, 2014
)
0.4
" Carfilzomib and its orally bioavailable structural analog oprozomib are second-generation, highly-selective, proteasome inhibitors."( Carfilzomib and oprozomib synergize with histone deacetylase inhibitors in head and neck squamous cell carcinoma models of acquired resistance to proteasome inhibitors.
Johnson, DE; Kirk, CJ; Zang, Y, 2014
)
0.4
"These results suggest the potential of NLCs as an oral delivery system for enhancement of cellular uptake, in vitro cytotoxicity in cancer cell lines and the oral bioavailability of VRS."( Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic.
Chu, DT; Hoang, VL; Jeong, JH; Kim, JO; Tak, JW; Tran, TH; Truong, DH; Yong, CS, 2016
)
0.43
" Notably, one of these new derivatives, (E)-N-hydroxy-3-(2-oxo-1-(quinolin-2-ylmethyl)-1,2-dihydropyridin-3-yl)acrylamide (4l), significantly restored RUNX3 in a dose-dependent manner and showed high metabolic stability, a good pharmacokinetic profile with high oral bioavailability and long half-life, and strong antitumor activity."( Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
Cho, M; Choi, S; Han, G; Jeong, JH; Kang, JS; Kim, H; Kim, HJ; Kim, JH; Lee, C; Oh, SJ; Yang, JS, 2015
)
0.42
" It indicated that a higher relative bioavailability for hydrogel was achieved compared with oral vorinostat."( Preparation of a mixed-matrix hydrogel of vorinostat for topical administration on the rats as experimental model.
Dai, W; Li, Y; Sun, F; Teng, L; Wang, C; Yao, J; Yu, C, 2015
)
0.9
" 23bb has a good pharmacokinetic profile with oral bioavailability of 47."( Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
Cao, D; Chen, L; Chen, X; Liu, Z; Long, C; Ma, L; Niu, T; Tang, M; Wang, F; Wang, T; Wang, X; Xiang, W; Yang, Z; Yi, Y; You, J, 2016
)
0.43
"To improve the bioavailability and anticancer potential of suberoylanilide hydroxamic acid (SAHA) by developing a drug-loaded polymeric nanomicellar system."( Polymeric micelles of suberoylanilide hydroxamic acid to enhance the anticancer potential in vitro and in vivo.
Biswas, S; Ghanta, P; Ghosh, B; Kiran Rompicharla, SV; Kumari, P; Trivedi, P, 2017
)
0.46
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
" What's more, 6d possessed desirable pharmacokinetic profiles with the oral bioavailability of 72% in SD rats and considerable in vivo antitumor efficacy in a human colorectal adenocarcinoma (HT-29) xenograft model."( Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
Chou, CJ; Huang, Y; Jia, Y; Li, X; Liang, X; Xu, W; Zang, J; Zhang, Y, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" In this study, a novel combination strategy was applied by combining curcumin with Suberoylanilide Hydroxamic Acid (SAHA) to increase both bioavailability of curcumin and the efficiency of SAHA, which have limited efficiency when used alone."( Synergistic Combination of Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid and Natural Flavonoid Curcumin Exhibits Anticancer and Antibacterial Activity.
Altundağ, EM; Güran, M; Kerküklü, NR; Özbilenler, C; Şanlıtürk, G; Toprak, K; Yalçın, AS; Yılmaz, AM, 2021
)
0.62
" In the present study, we hypothesize that a combination of an epigenetic modulator, vorinostat, along with rosiglitazone can impart improved gene expression of neurotrophic factors and attenuate biochemical and cellular alteration associated with AD mainly by loading these drugs in a surface modified nanocarrier system for enhanced bioavailability and enhanced therapeutic efficacy."( Neuroprotective Efficacy of Co-Encapsulated Rosiglitazone and Vorinostat Nanoparticle on Streptozotocin Induced Mice Model of Alzheimer Disease.
Chitkara, D; Dubey, SK; K C, S; Kakoty, V; Krishna, KV; Taliyan, R, 2021
)
1.09
" However, the solely clinically used SERD fulvestrant, is low orally bioavailable and requires intravenous injection, which severely limits its clinical application."( Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
Hu, Z; Huang, J; Li, C; Ning, W; Tang, C; Xin, L; Zhao, C; Zhou, HB, 2021
)
0.62

Dosage Studied

Vorinostat (VOR) has been reported to enhance the cytotoxic effects of doxorubicin (DOX) with fewer side effects because of the lower DOX dosage in breast cancer cells.

ExcerptRelevanceReference
" TSA also prevented, in a dose-response relationship, the sprouting of capillaries from rat aortic rings."( Histone deacetylases inhibitors as anti-angiogenic agents altering vascular endothelial growth factor signaling.
Blacher, S; Bonjean, K; Castronovo, V; Clausse, N; Colige, A; Deroanne, CF; Devy, L; Foidart, JM; Nusgens, BV; Servotte, S; Verdin, E, 2002
)
0.31
" Four compounds having an MTD > or = 100 mg/kg were selected for dose-response studies in the HCT116 xenograft model."( N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
Atadja, P; Bair, KW; Bontempo, J; Cesarz, D; Chandramouli, N; Chen, R; Cheung, M; Cornell-Kennon, S; Dean, K; Diamantidis, G; France, D; Green, MA; Howell, KL; Kashi, R; Kwon, P; Lassota, P; Martin, MS; Mou, Y; Perez, LB; Remiszewski, SW; Sambucetti, LC; Sharma, S; Smith, T; Sorensen, E; Taplin, F; Trogani, N; Versace, R; Walker, H; Weltchek-Engler, S; Wood, A; Wu, A, 2003
)
0.32
"To determine the safety, dosing schedules, pharmacokinetic profile, and biologic effect of orally administered histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) in patients with advanced cancer."( Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.
Chiao, JH; Chu, E; Curley, T; Heaney, M; Kelly, WK; Krug, LM; MacGregore-Cortelli, B; Marks, PA; O'Connor, OA; Olgac, S; Richardson, S; Richon, VM; Scher, H; Schwartz, L; Secrist, JP; Tong, W, 2005
)
0.33
" The maximum tolerated dose was 400 mg qd and 200 mg bid for continuous daily dosing and 300 mg bid for 3 consecutive days per week dosing."( Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.
Chiao, JH; Chu, E; Curley, T; Heaney, M; Kelly, WK; Krug, LM; MacGregore-Cortelli, B; Marks, PA; O'Connor, OA; Olgac, S; Richardson, S; Richon, VM; Scher, H; Schwartz, L; Secrist, JP; Tong, W, 2005
)
0.33
"Animals were dosed on Gestation Days 6-20 or 7-20, respectively, with litter/fetal parameters evaluated on GD 21 and 28, respectively."( Assessment of developmental toxicity of vorinostat, a histone deacetylase inhibitor, in Sprague-Dawley rats and Dutch Belted rabbits.
Kerr, JS; Turner, KJ; Wise, LD, 2007
)
0.61
" In this paper, we develop statistical methods for experimental design and data analysis of combination studies of drugs that have log-linear dose-response curves."( Experimental design and interaction analysis of combination studies of drugs with log-linear dose responses.
Fang, HB; Ross, DD; Sausville, E; Tan, M, 2008
)
0.35
" Alternative vorinostat dosing schedules may be needed for optimal down-regulation of TS expression."( A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin in patients with refractory colorectal cancer.
Egorin, MJ; Espinoza-Delgado, I; Fakih, MG; Fetterly, G; Holleran, JL; Litwin, A; Pendyala, L; Ross, ME; Rustum, YM; Toth, K; Zwiebel, JA, 2009
)
0.97
" Once-daily dosing was tested at 400 and 500 mg."( Phase I and pharmacokinetic study of vorinostat (suberoylanilide hydroxamic acid) in Japanese patients with solid tumors.
Fujiwara, Y; Hardwick, JS; Iwasa, T; Kanazu, S; Otsuki, T; Tamura, T; Yamada, K; Yamada, Y; Yamamoto, N, 2009
)
0.63
"In total, 32 patients were treated; vorinostat was dosed at 400, 600, 800, or 1000 mg day(-1) on days 1-3, followed by doxorubicin (20 mg m(-2)) on day 3 for 3 of 4 weeks."( Phase I trial of vorinostat and doxorubicin in solid tumours: histone deacetylase 2 expression as a predictive marker.
Chiappori, A; Daud, A; Egorin, M; Lee, JH; Marchion, D; Minton, S; Munster, PN; Simon, G; Springett, G; Sullivan, D; Thomas, S, 2009
)
0.97
" Vorinostat is orally dosed daily in rats (controls, 20, 50, or 150 mg/kg/d) and dogs (controls, 60, 80, or 100/125/160 mg/kg/d) for 26 weeks with a 4-week recovery."( Nonclinical safety assessment of the histone deacetylase inhibitor vorinostat.
Andrews, PA; Armstrong, M; Galloway, S; Kerr, JS; Lagrutta, A; Miller, T; Richon, VM,
)
1.28
" Daily histone deacetylase (HDAC) inhibitor infusions in the shell of the nucleus accumbens (NAc) caused an upward shift in the dose-response curve under fixed-ratio schedule and increased the break point under progressive-ratio schedule, indicating enhanced motivation for self-administered drug."( Chronic cocaine-induced H3 acetylation and transcriptional activation of CaMKIIalpha in the nucleus accumbens is critical for motivation for drug reinforcement.
Hu, Z; Hui, B; Lv, Z; Ma, L; Sheng, J; Sun, J; Wang, L, 2010
)
0.36
"Vorinostat efficiently suppressed MES-SA cell growth at a low dosage (3 microM) already after 24 hours treatment."( Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo.
Denk, H; Hrzenjak, A; Kremser, ML; Moinfar, F; Petru, E; Strohmeier, B; Zatloukal, K, 2010
)
2.09
" V concentrations higher than previously reported with oral dosing were achieved."( A phase I pharmacokinetic study of pulse-dose vorinostat with flavopiridol in solid tumors.
Ames, MM; Cane, LM; Carvajal, RD; Dials, HJ; Dickson, MA; Gonen, M; Grant, S; Lefkowitz, RA; McGovern, RM; Rathkopf, DE; Reid, JM; Roberts, JD; Schwartz, GK, 2011
)
0.63
"The pharmacology, pharmacokinetics, clinical efficacy, safety, adverse effects, dosage and administration, and role in therapy of vorinostat in the treatment of cutaneous T-cell lymphoma (CTCL) are reviewed."( Vorinostat: A novel therapy for the treatment of cutaneous T-cell lymphoma.
Kavanaugh, SA; Kavanaugh, SM; Kolesar, JM; White, LA, 2010
)
2.01
" The present results show the applicability of our novel statistical methodology for quantitatively assessing drug synergy across a wide range of doses of agents with complex dose-response profiles, a methodology with great potential for advancing the development of chemopreventive combinations."( Validation of a novel statistical model for assessing the synergy of combined-agent cancer chemoprevention.
Fujimoto, J; Hong, WK; Kong, M; Lee, JJ; Lotan, R, 2010
)
0.36
" One week later, daily vorinostat dosing was begun and continued until toxicity or disease progression occurred."( Phase I study of vorinostat in patients with advanced solid tumors and hepatic dysfunction: a National Cancer Institute Organ Dysfunction Working Group study.
Belani, CP; Beumer, JH; Egorin, MJ; Harvey, RD; Holleran, J; Ivy, SP; Kummar, S; Lin, Y; LoRusso, P; Ramalingam, SS; Sarantopoulos, J; Shibata, S; Yerk, M, 2010
)
1.01
" We demonstrated that when dose-response curves were fitted with the same method, similar evaluated results for drug combinations would be derived with different models."( [Three different drug interaction mathematical models used to evaluate the cytotoxicity of SAHA and arsenic trioxide in combination].
Liu, ZJ; Lu, N; Wang, N; Yan, Z, 2010
)
0.36
" Here we evaluated the dosage effects of HDAC inhibitors suberoylanilide hydroxamic acid (SAHA) and valproic acid (VPA) in a series of human leukaemia cell lines."( Epigenetic modulation of gene expression of human leukemia cell lines - induction of cell death and senescence.
Elknerova, K; Lacinova, Z; Marinov, I; Myslivcova, D; Stöckbauer, P; Uherkova, L, 2011
)
0.37
" However, the sequential schedule of decitabine 10 mg/m(2)/day on days 1 to 5 and vorinostat 200 mg twice a day on days 6 to 12 was more deliverable than both MTDs with fewer delays on repeated dosing and it represents the recommended phase II (RP2D) dose of this combination."( Phase I study of decitabine in combination with vorinostat in patients with advanced solid tumors and non-Hodgkin's lymphomas.
Chen, EX; Egorin, MJ; Espinoza-Delgado, I; Hirte, HW; Holleran, JL; Hotte, SJ; Laughlin, A; McGill, S; Moretto, P; Oza, AM; Siu, LL; Stathis, A; Stayner, LA; Wang, L; Webster, S; Zhang, WJ, 2011
)
0.85
" Control and streptozotocin-diabetic wild-type and eNOS(-/-) mice were treated with vorinostat by daily oral dosing for 18 weeks."( Long-term administration of the histone deacetylase inhibitor vorinostat attenuates renal injury in experimental diabetes through an endothelial nitric oxide synthase-dependent mechanism.
Advani, A; Advani, SL; Connelly, KA; Gilbert, RE; Huang, Q; Kelly, DJ; Marsden, PA; Thai, K; White, KE; Yuen, DA, 2011
)
0.83
" When orally dosed to tumor-bearing mice, 3 is enriched in tumor tissue which may contribute to its potent antitumor activity and prolonged duration of action."( Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Bonday, Z; Chang, JW; Chen, D; Deng, W; Dymock, BW; Fang, L; Goh, KC; Goh, KL; Goh, SK; Hu, C; Kantharaj, E; Khng, HH; Khoo, ML; Lee, KC; Liu, X; Lu, T; Lye, PL; Ng, MC; Poulsen, A; Sangthongpitag, K; Sun, ET; Wang, H; Wang, X; Wood, JM; Wu, X; Yeo, P; Yu, N, 2011
)
0.37
" In this study, we evaluated the safety, pharmacokinetics, and efficacy of two dosing regimens of vorinostat, an oral HDACi, in patients with GI tumors."( Evaluation of safety, pharmacokinetics, and efficacy of vorinostat, a histone deacetylase inhibitor, in the treatment of gastrointestinal (GI) cancer in a phase I clinical trial.
Chin, K; Doi, T; Hamaguchi, T; Hatake, K; Mehta, A; Noguchi, K; Ohtsu, A; Otsuki, T; Shirao, K, 2013
)
0.85
" No DLTs were encountered, but vorinostat dosing could not be escalated further due to thrombocytopenia."( Phase I study of vorinostat in combination with temozolomide in patients with high-grade gliomas: North American Brain Tumor Consortium Study 04-03.
Ames, MM; Chang, SM; Cloughesy, TF; Desideri, S; Drappatz, J; Espinoza-Delgado, I; Gilbert, MR; Kuhn, JG; Lamborn, KR; Lassman, AB; Lee, EQ; Lieberman, FS; McGovern, RM; Prados, MD; Puduvalli, VK; Reid, JM; Robins, HI; Wen, PY; Xu, J; Ye, X; Yung, WK, 2012
)
1
" Dose-response of different concentrations of bortezomib and SAHA on inhibition of cell proliferation of NPC was determined."( Bortezomib and SAHA synergistically induce ROS-driven caspase-dependent apoptosis of nasopharyngeal carcinoma and block replication of Epstein-Barr virus.
Chiang, AK; Ho, DN; Hui, KF; Lam, BH; Tsao, SW, 2013
)
0.39
" There was no clear relationship between vorinostat dosage and drug exposure over the dose range studied."( A pediatric phase 1 trial of vorinostat and temozolomide in relapsed or refractory primary brain or spinal cord tumors: a Children's Oncology Group phase 1 consortium study.
Ahern, C; Ames, MM; Blaney, SM; Fouladi, M; Gilbertson, RJ; Horton, T; Hummel, TR; Ingle, AM; McGovern, RM; Reid, JM; Wagner, L; Weigel, B, 2013
)
0.95
" Blood samples were obtained on days 1 and 9 of cycle 1 prior to dosing and 2 and 6 h post-dosing in all 60 subjects."( Vorinostat in combination with bortezomib in patients with advanced malignancies directly alters transcription of target genes.
Alberti, D; Bailey, HH; Espinoza-Delgado, I; Hoang, T; Holen, KD; Kim, K; Kolesar, JM; Schelman, WR; Seo, S; Traynor, AM; Wilding, G; Wright, JJ, 2013
)
1.83
" Bortezomib dosing was increased using a standard phase I dose-escalation schema."( A phase I study of vorinostat in combination with bortezomib in patients with advanced malignancies.
Alberti, D; Ames, MM; Attia, S; Bailey, HH; Eickhoff, J; Espinoza-Delgado, I; Hoang, T; Holen, KD; Jiang, Z; Kolesar, JM; Marnocha, R; McGovern, RM; Reid, JM; Schelman, WR; Traynor, AM; Wilding, G; Wright, JJ, 2013
)
0.72
" We previously examined a once-daily continuous dosing schedule of vorinostat in combination with bortezomib which was well tolerated in cycles 1 and 2; however, there was concern regarding the tolerability through multiple cycles."( A Phase I study of intermittently dosed vorinostat in combination with bortezomib in patients with advanced solid tumors.
Alberti, D; Ames, MM; Bailey, HH; Deming, DA; Eickhoff, J; Espinoza-Delgado, I; Kolesar, JM; Marnocha, R; McGovern, RM; Ninan, J; Reid, JM; Schelman, WR; Wilding, G; Wright, J, 2014
)
0.91
" DLTs in the intermittent dosing scheduled included thrombocytopenia and fatigue."( A Phase I study of intermittently dosed vorinostat in combination with bortezomib in patients with advanced solid tumors.
Alberti, D; Ames, MM; Bailey, HH; Deming, DA; Eickhoff, J; Espinoza-Delgado, I; Kolesar, JM; Marnocha, R; McGovern, RM; Ninan, J; Reid, JM; Schelman, WR; Wilding, G; Wright, J, 2014
)
0.67
" Tolerability was not improved with the intermittent dosing schedule of vorinostat when compared to continuous dosing."( A Phase I study of intermittently dosed vorinostat in combination with bortezomib in patients with advanced solid tumors.
Alberti, D; Ames, MM; Bailey, HH; Deming, DA; Eickhoff, J; Espinoza-Delgado, I; Kolesar, JM; Marnocha, R; McGovern, RM; Ninan, J; Reid, JM; Schelman, WR; Wilding, G; Wright, J, 2014
)
0.9
" Delayed dosing did not reduce adhesions."( Histone deacetylase inhibitors decrease intra-abdominal adhesions with one intraoperative dose by reducing peritoneal fibrin deposition pathways.
Cassidy, MR; Gainsbury, ML; Heydrick, S; Sheldon, HK; Sherburne, AC; Stucchi, AF, 2014
)
0.4
" A single, intraoperative intervention provides an ideal dosing strategy and indicates an exciting new role for HDACIs in adhesion prevention."( Histone deacetylase inhibitors decrease intra-abdominal adhesions with one intraoperative dose by reducing peritoneal fibrin deposition pathways.
Cassidy, MR; Gainsbury, ML; Heydrick, S; Sheldon, HK; Sherburne, AC; Stucchi, AF, 2014
)
0.4
"Vorinostat (VOR) has been reported to enhance the cytotoxic effects of doxorubicin (DOX) with fewer side effects because of the lower DOX dosage in breast cancer cells."( Transactivation of bad by vorinostat-induced acetylated p53 enhances doxorubicin-induced cytotoxicity in cervical cancer cells.
Hoe, KL; Hwang, SO; Kim, DU; Kim, JH; Lee, SJ; Nam, JH; Nam, M; Noh, EJ, 2014
)
2.15
" In an HCT-116 nude mice xenograft model, compound 1o displayed significant antitumor activity in both continuous and intermittent dosing schedules."( Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
Cheng, J; Guo, S; Qin, J; Qiu, H; Zhong, Y, 2014
)
0.4
"In vivo histone deacetylase (HDAC) inhibition by vorinostat under clinically acceptable dosing is limited by its poor pharmacokinetics properties."( Vorinostat-polymer conjugate nanoparticles for Acid-responsive delivery and passive tumor targeting.
Bertrand, P; Blanquart, C; Collette, F; Delatouche, R; Denis, I; El Bahhaj, F; Grégoire, M; Gueugnon, F; Héroguez, V; Pichavant, L; Pouliquen, D, 2014
)
2.1
"The recommended phase II dosage was oral pazopanib at 600 mg daily plus oral vorinostat at 300 mg daily."( Phase I study of pazopanib and vorinostat: a therapeutic approach for inhibiting mutant p53-mediated angiogenesis and facilitating mutant p53 degradation.
Araujo, D; Fu, S; Hess, K; Hong, D; Hou, MM; Hwu, P; Janku, F; Karp, D; Kee, B; Kurzrock, R; Meric-Bernstam, F; Naing, A; Piha-Paul, S; Subbiah, V; Tsimberidou, A; Wheler, J; Wolff, R; Zinner, R, 2015
)
0.93
" Busulfan dosing targeted 4000 μM-minute/day (days -8 to -5)."( Vorinostat Combined with High-Dose Gemcitabine, Busulfan, and Melphalan with Autologous Stem Cell Transplantation in Patients with Refractory Lymphomas.
Ahmed, S; Alousi, A; Anderlini, P; Andersson, BS; Bashir, Q; Champlin, R; Dabaja, B; Fanale, M; Gulbis, A; Hagemeister, F; Hosing, C; Jones, RB; Liu, Y; Nieto, Y; Oki, Y; Pinnix, C; Popat, U; Qazilbash, M; Shah, N; Shpall, EJ; Thall, PF; Valdez, BC, 2015
)
1.86
" Dosing was limited by thrombocytopenia."( Phase I study of the mTOR inhibitor ridaforolimus and the HDAC inhibitor vorinostat in advanced renal cell carcinoma and other solid tumors.
Corrigan, A; Denlinger, CS; Devarajan, K; Malizzia, L; Olszanski, AJ; Plimack, ER; Roethke, SK; Tetzlaff, CH; Wong, YN; Zibelman, M, 2015
)
0.65
" The first dose level (DL A) tested vorinostat as daily oral dosing from days 1 to 14."( Phase I study of combination of vorinostat, carboplatin, and gemcitabine in women with recurrent, platinum-sensitive epithelial ovarian, fallopian tube, or peritoneal cancer.
Berlin, S; Campos, S; Horowitz, N; Krasner, C; Lee, H; Liu, J; Matulonis, U; Obermayer, E; Penson, R; Whalen, C, 2015
)
0.98
" We hypothesized that HDACi-modulated genes would be best identified with a dose-response analysis."( Dose-responsive gene expression in suberoylanilide hydroxamic acid-treated resting CD4+ T cells.
Beliakova-Bethell, N; Margolis, DM; Reardon, B; Richman, DR; Singhania, A; Spina, CA; Woelk, CH, 2015
)
0.42
" Additional in vivo SAHA dosing studies with larger sample size are warranted."( Development of a novel in vivo corneal fibrosis model in the dog.
Bunyak, F; Giuliano, EA; Gronkiewicz, KM; Hamm, CW; Kuroki, K; Mohan, RR; Sharma, A; Teixeira, LB, 2016
)
0.43
" Dose-response curves revealed dose-dependent profiles with greater potency of HDACis over CyA (IC50 values of 82."( Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation.
Cobbold, M; Drayson, MT; Ellis, JD; Hampson, P; Inston, NG; Jenkinson, E; Neil, DA; Ready, AR; Shuttleworth, SJ, 2016
)
0.43
" The N-hydroxyl group of this motif is highly subject to sulfation/glucoronidation-based inactivation in humans; compounds containing this motif require much higher dosing in clinic to achieve therapeutic concentrations."( Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
Chou, CJ; Inks, ES; Li, J; McClure, JJ; Peterson, YK; Zhang, C, 2016
)
0.43
" Thus, genotype-directed dosing could improve pharmacotherapy by reducing the risk of toxicities or preventing suboptimal treatment."( Pharmacogenomics and histone deacetylase inhibitors.
Figg, WD; Goey, AK; Peer, CJ; Sissung, TM, 2016
)
0.43
" Triple combinations with a low dosage of cisplatin demonstrate similar therapeutic effects."( Vorinostat enhances the cisplatin-mediated anticancer effects in small cell lung cancer cells.
Chang, YF; Ko, JC; Lee, MS; Liang, MC; Liang, SK; Pan, CH; Wen, BC, 2016
)
1.88
"SAHA and TSA could inhibit total HDAC activity and placental HDAC1/2/3 expression both in Bewo and JAR, but displayed a transient induction of HDAC mRNA or protein level after being treated at low dosage or prolonged exposure to drugs."( The effect of histone deacetylase inhibition on the expression of P-glycoprotein in human placental trophoblast cell lines.
Duan, H; Hua, Y; Li, Q; Li, Y; Qiu, D; Wang, C; Wang, T; Zhang, Y; Zhou, K, 2017
)
0.46
" Increased p21 and cleaved PARP expression can potentially explain mechanisms of their enhanced effects, which require further PK/PD systems analysis to suggest an optimal dosing regimen."( Sequential Exposure of Bortezomib and Vorinostat is Synergistic in Multiple Myeloma Cells.
Mager, DE; Nanavati, C, 2017
)
0.73
" We sought to identify the optimal dosing of VOR for effective serial reversal of HIV latency."( Interval dosing with the HDAC inhibitor vorinostat effectively reverses HIV latency.
Allard, B; Archin, NM; Clutton, G; Eron, J; Gay, CL; Goonetilleke, N; Kashuba, AD; Kirchherr, JL; Kuruc, JD; Margolis, DM; Sholtis, K; Stuelke, E; Sung, JA; Xu, Y, 2017
)
0.72
"This study aimed at recommending pediatric dosages of the histone deacetylase (HDAC) inhibitor vorinostat and potentially more effective adult dosing regimens than the approved standard dosing regimen of 400 mg/day, using a comprehensive physiologically based pharmacokinetic/pharmacodynamic (PBPK/PD) modeling approach."( A physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) model of the histone deacetylase (HDAC) inhibitor vorinostat for pediatric and adult patients and its application for dose specification.
Britz, H; Burhenne, J; Egerer, G; Haefeli, WE; Lehr, T; Moj, D; Stewart, CF, 2017
)
0.88
"Thoroughly developed PBPK models enable dosage recommendations in pediatric patients and integrated PBPK/PD models, considering PD biomarkers (e."( A physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) model of the histone deacetylase (HDAC) inhibitor vorinostat for pediatric and adult patients and its application for dose specification.
Britz, H; Burhenne, J; Egerer, G; Haefeli, WE; Lehr, T; Moj, D; Stewart, CF, 2017
)
0.66
" Furthermore, SAHA dosing did not compromise corneal endothelial phenotype, density, or function in rabbit eyes, whereas MMC application did (P < ."( Efficacy and Safety Comparison Between Suberoylanilide Hydroxamic Acid and Mitomycin C in Reducing the Risk of Corneal Haze After PRK Treatment In Vivo.
Anumanthan, G; Gupta, S; Hamm, CW; Hesemann, NP; Mohan, RR; Sharma, A; Waggoner, M, 2017
)
0.46
" At the end of dosing schedule, neurobehavioral tests were conducted; followed by mechanistic evaluation through biochemical analysis, RTPCR and western blot in serum and hippocampus."( Antidepressant activity of vorinostat is associated with amelioration of oxidative stress and inflammation in a corticosterone-induced chronic stress model in mice.
Js, IC; Kv, A; Lahkar, M; Madhana, RM; Naidu, VGM; Sinha, S, 2018
)
0.78
"Inhibition of more than one pathway in a cancer cell with a single molecule could result in better therapies with less complex dosing regimens."( Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
Dymock, BW; Ohlson, S; Poulsen, A; Ramanujulu, PM; Yao, L, 2018
)
0.78
" Vorinostat was administered at the assigned dosage level (100-400 mg, three times weekly) in a standard 3 + 3 dose escalation design."( A phase 1 trial of Vorinostat in combination with concurrent chemoradiation therapy in the treatment of advanced staged head and neck squamous cell carcinoma.
Agrawal, A; Baiocchi, R; Blakaj, D; Carrau, R; Diavolitsis, V; Grecula, J; Kang, S; Kumar, B; Kumar, P; Old, MO; Ozer, E; Palettas, M; Pan, Q; Rocco, J; Savvides, P; Teknos, TN; Wei, L, 2019
)
1.75
" Behavioral tests such as Morris water maze test, novel object recognition test, and object in place test were performed at the end of the dosing schedule to assess cognition."( Cognitive Improvement by Vorinostat through Modulation of Endoplasmic Reticulum Stress in a Corticosterone-Induced Chronic Stress Model in Mice.
Bais, AK; K V, A; Kumar, P; Lahkar, M; Madhana, RM; Malik, A; Samudrala, PK; Singh, VB; Sinha, S, 2020
)
0.86
" As the VOR treatment-related adverse changes are mostly found reversible, further optimization of the therapeutic strategies with respect to dose, dosage regimen, and formulations of VOR could propel its clinical prospects."( Repurposing Vorinostat for the Treatment of Disorders Affecting Brain.
Athira, KV; Chakravarty, S; Sadanandan, P, 2021
)
1
" The model can be potentially applied to evaluate their combination regimens and explore in vivo dosing regimens."( Network-Based Systems Analysis Explains Sequence-Dependent Synergism of Bortezomib and Vorinostat in Multiple Myeloma.
Mager, DE; Nanavati, C, 2021
)
0.84
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 3.5.1.98 (histone deacetylase) inhibitorAn EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98).
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
hydroxamic acidA compound, RkE(=O)lNHOH, derived from an oxoacid RkE(=O)l(OH) (l =/= 0) by replacing -OH with -NHOH, and derivatives thereof. Specific examples of hydroxamic acids are preferably named as N-hydroxy amides.
dicarboxylic acid diamide
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (136)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nrf2Homo sapiens (human)Potency3.38890.09208.222223.1093AID624171; AID651593
RAR-related orphan receptor gammaMus musculus (house mouse)Potency1.29090.006038.004119,952.5996AID1159521; AID1159523
PPM1D proteinHomo sapiens (human)Potency1.47400.00529.466132.9993AID1347411
TDP1 proteinHomo sapiens (human)Potency0.50870.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency0.12390.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency2.06690.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743040; AID743042; AID743053; AID743054; AID743063
Smad3Homo sapiens (human)Potency3.16230.00527.809829.0929AID588855
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency4.21630.013326.981070.7614AID1346978
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency5.62780.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency3.61900.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency0.94390.000417.946075.1148AID1346795
EWS/FLI fusion proteinHomo sapiens (human)Potency2.65250.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.90030.000214.376460.0339AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency1.05760.003041.611522,387.1992AID1159552; AID1159553; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency1.09510.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency2.11300.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency7.49780.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency4.75480.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency4.89750.00108.379861.1304AID1645840
caspase-3Homo sapiens (human)Potency4.21630.013326.981070.7614AID1346978
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency6.72670.001723.839378.1014AID743083
Caspase-7Cricetulus griseus (Chinese hamster)Potency14.96010.006723.496068.5896AID1346980
caspase-3Cricetulus griseus (Chinese hamster)Potency14.96010.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency2.31770.000323.4451159.6830AID743065; AID743067
histone deacetylase 9 isoform 3Homo sapiens (human)Potency0.32610.037617.082361.1927AID1259364; AID1259388
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency5.21340.000627.21521,122.0200AID743202; AID743219
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency0.89130.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency0.06310.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency0.06310.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency0.06310.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency6.52130.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency1.62760.005612.367736.1254AID624032; AID624044
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency7.07950.025911.239831.6228AID602313
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency3.34910.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency2.15340.00339.158239.8107AID1347407; AID1347411
Cellular tumor antigen p53Homo sapiens (human)Potency0.75420.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency3.34910.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency1.99380.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency1.89590.011912.222168.7989AID651632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188IC50 (µMol)0.95000.95000.95000.9500AID977608
Chain A, Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188IC50 (µMol)0.95000.95000.95000.9500AID977608
Histone deacetylase 8Schistosoma mansoniIC50 (µMol)1.31470.30341.33503.6200AID1296346; AID1446915; AID1784185
Histone deacetylase Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Lysine-specific demethylase 4EHomo sapiens (human)IC50 (µMol)277.00000.20001.95696.3096AID1798635; AID1885254; AID604081; AID604082
Gli1Mus musculus (house mouse)IC50 (µMol)2.23000.02704.293911.4000AID602464
nuclear receptor subfamily 0 group B member 1Homo sapiens (human)IC50 (µMol)45.34370.13430.86462.1450AID588797; AID687017
cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC50 (µMol)1.55000.140016.625050.0000AID1224863
steroidogenic factor 1Homo sapiens (human)IC50 (µMol)67.47401.87302.92953.9860AID687018
protein Wnt-3a precursorMus musculus (house mouse)IC50 (µMol)50.00000.44104.995214.8000AID651570
Histone deacetylase 1Mus musculus (house mouse)IC50 (µMol)0.11200.00140.72308.1000AID273173; AID316880; AID90675; AID90680; AID90681
Histone deacetylase 1Mus musculus (house mouse)Ki0.06760.00110.03430.0676AID90677
Histone deacetylase 3Homo sapiens (human)IC50 (µMol)1.59440.00040.619610.0000AID1061953; AID1063058; AID1063059; AID1065634; AID1126958; AID1126961; AID1127324; AID1128556; AID1129005; AID1139706; AID1141243; AID1141761; AID1164026; AID1164782; AID1164908; AID1166497; AID1173501; AID1174680; AID1174694; AID1177044; AID1178597; AID1201642; AID1205625; AID1206764; AID1225983; AID1227031; AID1234889; AID1239049; AID1246509; AID1250642; AID1256443; AID1263144; AID1266094; AID1266808; AID1273866; AID1273871; AID1274873; AID1275076; AID1275247; AID1275592; AID1275632; AID1275636; AID1280307; AID1281848; AID1282239; AID1293553; AID1293565; AID1303686; AID1308511; AID1312867; AID1321702; AID1339569; AID1340594; AID1341595; AID1341621; AID1341623; AID1348917; AID1349715; AID1361633; AID1380938; AID1384208; AID1390009; AID1390012; AID1390020; AID1394888; AID1398800; AID1399543; AID1401341; AID1401374; AID1403153; AID1409640; AID1409641; AID1409642; AID1415637; AID1418667; AID1439349; AID1449216; AID1451831; AID1482099; AID1487001; AID1487094; AID1493593; AID1511130; AID1525779; AID1541444; AID1541452; AID1541453; AID1541563; AID1541565; AID1542181; AID1543943; AID1545756; AID1545761; AID1547269; AID1548247; AID1548256; AID1548728; AID1549163; AID1550094; AID1563942; AID1566039; AID1566804; AID1578147; AID1578156; AID1578475; AID1578887; AID1587865; AID1597974; AID1600657; AID1600732; AID1600735; AID1614128; AID1622907; AID1622908; AID1622913; AID1622931; AID1622954; AID1622962; AID1622977; AID1623525; AID1639362; AID1650413; AID1650415; AID1655789; AID1659646; AID1659649; AID1677516; AID1688025; AID1690106; AID1690833; AID1690844; AID1697196; AID1702062; AID1720096; AID1722282; AID1727740; AID1742179; AID1753839; AID1754753; AID1758467; AID1759720; AID1759721; AID1759727; AID1759728; AID1762488; AID1762497; AID1764247; AID1764248; AID1764288; AID1764292; AID1765326; AID1771467; AID1775547; AID1775565; AID1784987; AID1785334; AID1798419; AID1798524; AID1798526; AID1800141; AID1801572; AID1802356; AID1802398; AID1808546; AID1812439; AID1812444; AID1816187; AID1819502; AID1821272; AID1821957; AID1821959; AID1825925; AID1832670; AID1832687; AID1832805; AID1846147; AID1848558; AID1848559; AID1848585; AID1861251; AID1861259; AID1861655; AID1863173; AID1863435; AID1864216; AID1864240; AID1865258; AID1865263; AID1873383; AID1873409; AID1873410; AID1873411; AID1873412; AID1873413; AID1876341; AID1882466; AID1886185; AID1888420; AID1890310; AID1890512; AID1893824; AID1899585; AID1901148; AID1901153; AID1901761; AID1915571; AID1915585; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID313731; AID316872; AID316875; AID316877; AID316878; AID316931; AID324949; AID328795; AID331898; AID331899; AID343689; AID343690; AID348798; AID350715; AID352517; AID352748; AID353356; AID366642; AID373073; AID373076; AID374818; AID382342; AID408882; AID420326; AID456795; AID459821; AID461250; AID463865; AID465151; AID473030; AID473175; AID487873; AID488238; AID488275; AID499799; AID511065; AID525002; AID527317; AID539709; AID541646; AID545854; AID546545; AID546549; AID591330; AID593548; AID594123; AID603542; AID605298; AID605394; AID608776; AID609506; AID615998; AID622254; AID622256; AID626565; AID628440; AID631668; AID652747; AID652762; AID663331; AID669756; AID670514; AID670971; AID673992; AID675299; AID708770; AID717824; AID717827; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID725668; AID729522; AID732145; AID732875; AID732878; AID744378; AID748112; AID748985; AID749389; AID749705; AID750109; AID753149; AID753167; AID755627; AID760510; AID761584; AID764219; AID764647; AID772639; AID780575; AID780587; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 3Homo sapiens (human)Ki0.32180.00020.42378.1900AID1170742; AID1740130; AID331899; AID447579; AID482943; AID496803; AID619048; AID765391
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00100.00040.21474.0000AID348801; AID348802
Lysine-specific histone demethylase 1AHomo sapiens (human)IC50 (µMol)100.00000.00312.16029.6000AID1502982; AID1816685
Tyrosine-protein kinase JAK2Homo sapiens (human)IC50 (µMol)10.00000.00010.372210.0000AID1201644
Bromodomain-containing protein 4Homo sapiens (human)IC50 (µMol)4.15860.00040.40329.0500AID1454051; AID1462230; AID1727731; AID1727732; AID1845320
Nuclear receptor corepressor 1Homo sapiens (human)IC50 (µMol)0.03820.00980.07410.2340AID1349715; AID1451831; AID1742179
Nuclear receptor corepressor 1Homo sapiens (human)Ki0.01200.00020.01240.0250AID765391
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Tyrosine-protein kinase ABL1Homo sapiens (human)IC50 (µMol)100.00000.00010.712810.0000AID414721
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)0.45600.00000.536910.0000AID1720112; AID1915572
Tubulin alpha-1A chainSus scrofa (pig)IC50 (µMol)1.50000.00672.160310.0000AID711157
Tubulin beta chainSus scrofa (pig)IC50 (µMol)1.50000.00672.137410.0000AID711157
AlbuminHomo sapiens (human)IC50 (µMol)0.10720.00131.62173.5000AID373082
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC50 (µMol)10.00000.00000.79498.9000AID737918
Amyloid-beta precursor proteinHomo sapiens (human)IC50 (µMol)20.00000.00053.889510.0000AID1690839
Heat shock protein HSP 90-alphaHomo sapiens (human)IC50 (µMol)167.33330.00040.695010.0000AID1394887; AID1578157; AID1690105
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)11.00000.00011.753610.0000AID274013; AID609494
Leukotriene A-4 hydrolaseHomo sapiens (human)IC50 (µMol)4.66000.00051.28547.6500AID1441630; AID1441631
Cytochrome P450 2C8Homo sapiens (human)IC50 (µMol)0.09030.00081.88487.9000AID1067347; AID1437239
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.01100.00002.015110.0000AID1437239
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.24000.00002.800510.0000AID1200971
Aminopeptidase NSus scrofa (pig)IC50 (µMol)100.00000.00053.53548.9000AID1802060
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)0.15820.00101.979414.1600AID1166497
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.80000.00021.874210.0000AID759303
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.05300.00031.38338.4000AID764219
Cannabinoid receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00020.660910.0000AID1200971; AID1200972
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)100.00000.00002.37899.7700AID1502983
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.80000.00021.270410.0000AID759303
Leukotriene A-4 hydrolaseMus musculus (house mouse)IC50 (µMol)6.15000.79003.47006.1500AID1441702
DNA (cytosine-5)-methyltransferase 1Homo sapiens (human)IC50 (µMol)10.00000.01861.64886.0000AID1775568
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)100.00000.00001.89149.5700AID1502984
Phosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)IC50 (µMol)10.00000.00000.683210.0000AID1312848
Proteasome subunit beta type-5Homo sapiens (human)IC50 (µMol)25.00000.00050.939410.0000AID1363797; AID1363798; AID1363799
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.04200.00002.398310.0000AID1200972; AID1401904
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.13000.00010.995010.0000AID1067347
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)10.00000.00000.48308.8000AID1256442; AID1275245; AID1915578
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC50 (µMol)10.00000.00010.32759.5480AID1201643
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)7.20000.00020.75218.0140AID80353
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC50 (µMol)10.00000.00000.734010.0000AID1312848
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.80000.00001.819410.0000AID759303
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)7.20000.00402.15557.2000AID80353
Histone deacetylase 4Homo sapiens (human)IC50 (µMol)7.11290.00061.052610.0000AID1063059; AID1065630; AID1065631; AID1065638; AID1126958; AID1127325; AID1128557; AID1129006; AID1139706; AID1141243; AID1141761; AID1164186; AID1164909; AID1174680; AID1178599; AID1181304; AID1201642; AID1205625; AID1206765; AID1246514; AID1250644; AID1256443; AID1266808; AID1273866; AID1275076; AID1275247; AID1275632; AID1275638; AID1281849; AID1282240; AID1293553; AID1293564; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1348919; AID1349725; AID1352482; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1451832; AID1466062; AID1482101; AID1511134; AID1541452; AID1541453; AID1541456; AID1542182; AID1545761; AID1547268; AID1548248; AID1549163; AID1550094; AID1566806; AID1578147; AID1578156; AID1597974; AID1600732; AID1600735; AID1614133; AID1622907; AID1622908; AID1622932; AID1622954; AID1622973; AID1623527; AID1639362; AID1650413; AID1650415; AID1652191; AID1655790; AID1659646; AID1677516; AID1690106; AID1690835; AID1697196; AID1720096; AID1727741; AID1742181; AID1754754; AID1762488; AID1762489; AID1764247; AID1764248; AID1764252; AID1764288; AID1764292; AID1771467; AID1785335; AID1794854; AID1798524; AID1798526; AID1801045; AID1801572; AID1802239; AID1802356; AID1802398; AID1811364; AID1812439; AID1816189; AID1819502; AID1821957; AID1832670; AID1832688; AID1846147; AID1848558; AID1848559; AID1848587; AID1861251; AID1861260; AID1863436; AID1864216; AID1864226; AID1864240; AID1865258; AID1873384; AID1888420; AID1893824; AID1901148; AID1901156; AID1915571; AID1915596; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID313732; AID316872; AID316875; AID316877; AID316878; AID324950; AID328796; AID328797; AID331898; AID343689; AID343690; AID348800; AID350715; AID352749; AID353356; AID373073; AID373077; AID382342; AID420326; AID440821; AID456795; AID459821; AID461250; AID463865; AID473175; AID487873; AID492804; AID499799; AID525000; AID527317; AID539709; AID541648; AID545854; AID546545; AID591330; AID593549; AID603542; AID605298; AID608776; AID615998; AID616004; AID622254; AID626565; AID663331; AID669756; AID670514; AID675299; AID708770; AID711156; AID717827; AID723464; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID732153; AID732878; AID748111; AID749705; AID750109; AID753167; AID755627; AID760509; AID761584; AID764219; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 4Homo sapiens (human)Ki12.50100.00021.62559.1242AID1439780; AID1600730; AID1650411; AID447579; AID482944; AID619049
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.08600.00061.525710.0000AID1279124; AID1279125
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Ki20.00000.00090.19811.2400AID1361628
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)22.58050.00091.901410.0000AID1464879; AID1742739; AID609493; AID613341
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC50 (µMol)0.10000.00000.38373.9000AID1293554
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)1.44810.00010.55439.9000AID1061955; AID1063056; AID1063059; AID1065629; AID1065971; AID1067347; AID1126958; AID1126959; AID1127323; AID1128544; AID1128978; AID1139706; AID1141243; AID1141761; AID1141786; AID1162484; AID1164024; AID1164185; AID1164780; AID1164906; AID1166496; AID1168913; AID1173499; AID1174680; AID1174692; AID1177042; AID1178595; AID1181303; AID1200971; AID1201642; AID1202583; AID1203889; AID1205625; AID1206736; AID1206762; AID1225985; AID1227029; AID1231807; AID1233250; AID1234887; AID1234888; AID1235108; AID1235256; AID1239048; AID1240548; AID1246507; AID1248356; AID1250640; AID1251316; AID1256443; AID1260653; AID1266092; AID1266808; AID1266818; AID1273866; AID1274871; AID1275076; AID1275077; AID1275247; AID1275590; AID1275632; AID1275633; AID1276240; AID1279124; AID1280259; AID1280306; AID1281847; AID1282229; AID1293553; AID1293563; AID1296348; AID1303685; AID1308511; AID1312847; AID1312867; AID1321619; AID1321700; AID1326509; AID1330926; AID1337195; AID1339567; AID1340594; AID1341595; AID1341621; AID1341623; AID1348915; AID1349719; AID1352480; AID1355688; AID1361627; AID1365022; AID1379287; AID1380938; AID1383985; AID1384206; AID1384210; AID1384215; AID1390009; AID1390010; AID1390020; AID1390962; AID1393285; AID1394888; AID1396985; AID1399542; AID1401341; AID1401372; AID1401902; AID1403152; AID1409640; AID1409641; AID1409642; AID1410323; AID1415637; AID1421602; AID1421911; AID1437240; AID1437552; AID1439348; AID1449214; AID1449326; AID1451821; AID1452273; AID1459953; AID1462221; AID1464870; AID1466061; AID1469380; AID1476119; AID1478590; AID1478591; AID1482097; AID1486293; AID1486677; AID1486999; AID1487092; AID1493590; AID1502986; AID1503840; AID1511132; AID1511967; AID1514595; AID1515840; AID1518781; AID1525777; AID1535339; AID1537554; AID1541446; AID1541452; AID1541453; AID1541563; AID1541565; AID1542179; AID1543929; AID1545755; AID1545761; AID1547270; AID1548244; AID1548245; AID1548256; AID1548726; AID1549163; AID1549164; AID1550094; AID1558002; AID1563940; AID1566037; AID1566802; AID1572341; AID1576449; AID1578147; AID1578149; AID1578156; AID1578886; AID1587863; AID1589336; AID1591715; AID1597931; AID1597974; AID1600659; AID1600732; AID1600735; AID1614126; AID1622904; AID1622905; AID1622907; AID1622908; AID1622909; AID1622912; AID1622929; AID1622954; AID1622960; AID1622972; AID1622975; AID1623523; AID1633653; AID1639362; AID1650413; AID1650415; AID1652190; AID1655787; AID1658889; AID1659234; AID1659646; AID1659647; AID1667066; AID1677512; AID1677516; AID1688023; AID1690106; AID1690833; AID1690842; AID1697196; AID1698862; AID1699972; AID1702055; AID1702060; AID1704066; AID1707507; AID1720096; AID1722281; AID1723742; AID1727729; AID1730857; AID1731759; AID1737133; AID1742177; AID1751984; AID1752936; AID1753636; AID1753835; AID1754751; AID1758461; AID1759721; AID1759727; AID1759728; AID1762488; AID1762495; AID1764247; AID1764248; AID1764288; AID1764292; AID1764800; AID1764815; AID1765324; AID1769648; AID1771467; AID1775545; AID1775563; AID1777021; AID1783108; AID1784189; AID1784985; AID1785332; AID1794854; AID1797826; AID1798419; AID1798524; AID1798526; AID1798784; AID1800141; AID1801045; AID1801572; AID1802239; AID1802356; AID1802398; AID1802920; AID1808545; AID1810051; AID1811363; AID1812439; AID1812442; AID1816186; AID1816687; AID1819502; AID1819503; AID1821270; AID1821957; AID1821958; AID1825923; AID1826595; AID1832670; AID1832671; AID1832801; AID1845307; AID1845459; AID1846130; AID1846147; AID1847777; AID1848558; AID1848559; AID1848582; AID1849157; AID1855242; AID1855243; AID1856988; AID1861251; AID1861653; AID1863172; AID1863433; AID1864216; AID1864224; AID1864240; AID1865258; AID1865261; AID1873381; AID1873399; AID1873400; AID1873401; AID1873402; AID1873403; AID1876461; AID1882089; AID1882456; AID1886183; AID1888420; AID1888466; AID1888581; AID1890307; AID1890510; AID1893824; AID1897365; AID1897805; AID1899585; AID1901054; AID1901148; AID1901152; AID1907399; AID1915523; AID1915537; AID1915562; AID1915571; AID1915574; AID1917530; AID240505; AID240810; AID258011; AID269668; AID274015; AID274062; AID274110; AID288446; AID292436; AID294382; AID297470; AID297471; AID300832; AID303347; AID303348; AID304373; AID308049; AID310180; AID313729; AID316872; AID316875; AID316877; AID316878; AID316892; AID316896; AID324948; AID328793; AID331898; AID343687; AID343689; AID343690; AID344920; AID347808; AID348792; AID350715; AID350716; AID352516; AID353356; AID366640; AID373073; AID373074; AID374811; AID382342; AID392398; AID392406; AID395022; AID408880; AID411253; AID414717; AID420324; AID420326; AID438216; AID440819; AID449260; AID456795; AID459821; AID461250; AID463865; AID465149; AID473029; AID473175; AID482939; AID482940; AID487873; AID488273; AID492803; AID499799; AID511063; AID525003; AID527317; AID538408; AID539709; AID541644; AID545854; AID546545; AID546547; AID591330; AID593547; AID603542; AID605298; AID605392; AID608776; AID609489; AID609505; AID615998; AID616002; AID619041; AID621737; AID622254; AID622255; AID623020; AID626565; AID628437; AID631666; AID655470; AID655476; AID659492; AID659493; AID663331; AID669756; AID669761; AID670013; AID670514; AID670970; AID672021; AID672022; AID673990; AID675299; AID683274; AID708770; AID711159; AID717826; AID717827; AID723466; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID725670; AID729522; AID732146; AID732877; AID732878; AID734736; AID737917; AID744378; AID747252; AID748114; AID748983; AID749390; AID749704; AID749705; AID750109; AID753167; AID755627; AID759305; AID760512; AID761583; AID761584; AID764219; AID764647; AID772655; AID780575; AID780588; AID781051; AID80353; AID90195; AID90211; AID90212; AID90214; AID90340; AID90342; AID90347; AID90350; AID90351; AID90352; AID90353; AID90529; AID90663; AID90665
Histone deacetylase 1Homo sapiens (human)Ki0.36520.00000.49888.1900AID1170740; AID1389960; AID1399812; AID1740129; AID1798196; AID385229; AID447579; AID482939; AID496801; AID619046; AID765393
Histone deacetylase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.34513.5120AID90522
Histone deacetylase Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC50 (µMol)0.07000.00202.123310.0000AID1063058
ReninMacaca fascicularis (crab-eating macaque)IC50 (µMol)0.06700.06700.76851.4700AID748985
Histone deacetylase 3Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188IC50 (µMol)1.00001.00001.10001.2000AID420318
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188Ki1.15000.70003.05009.2000AID420317; AID420320
Histone deacetylase Plasmodium falciparum 3D7IC50 (µMol)0.10000.10000.10000.1000AID544400
Histone deacetylase 7Homo sapiens (human)IC50 (µMol)6.58890.00071.02609.9000AID1063059; AID1065636; AID1126958; AID1127328; AID1128560; AID1129009; AID1139706; AID1141243; AID1141761; AID1164030; AID1164912; AID1174680; AID1201642; AID1205625; AID1246516; AID1250646; AID1256443; AID1266808; AID1273866; AID1275076; AID1275247; AID1275632; AID1282242; AID1293553; AID1293568; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1348921; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1511136; AID1541452; AID1541453; AID1542185; AID1545761; AID1547271; AID1549163; AID1550094; AID1566808; AID1578147; AID1578156; AID1597974; AID1600732; AID1600735; AID1614135; AID1622907; AID1622908; AID1622935; AID1622954; AID1623529; AID1639362; AID1650413; AID1650415; AID1659646; AID1659651; AID1677516; AID1690106; AID1690834; AID1697196; AID1720096; AID1731758; AID1742183; AID1754756; AID1762488; AID1762490; AID1764247; AID1764248; AID1764288; AID1764292; AID1771467; AID1785338; AID1798524; AID1801572; AID1802356; AID1802398; AID1812439; AID1816190; AID1819502; AID1821957; AID1832670; AID1832691; AID1846147; AID1848558; AID1848559; AID1861251; AID1863168; AID1864216; AID1864240; AID1865258; AID1865266; AID1873387; AID1888420; AID1893824; AID1901148; AID1915571; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID313735; AID316872; AID316875; AID316877; AID316878; AID328800; AID331898; AID343689; AID343690; AID348802; AID350715; AID353356; AID373073; AID373080; AID374821; AID382342; AID420326; AID440823; AID456795; AID459821; AID461250; AID463865; AID473175; AID487873; AID499799; AID524997; AID527317; AID539709; AID541650; AID545854; AID546545; AID591330; AID593552; AID603542; AID605298; AID608776; AID615998; AID622254; AID626565; AID652751; AID663331; AID669756; AID670514; AID675299; AID708770; AID717827; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID732143; AID732878; AID747268; AID748108; AID749705; AID750109; AID753167; AID755627; AID760506; AID761584; AID764219; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 7Homo sapiens (human)Ki1.29950.00022.00059.5000AID447579; AID619052
Histone deacetylase 2Homo sapiens (human)IC50 (µMol)1.99980.00010.72219.9700AID1055355; AID1061954; AID1063057; AID1063059; AID1065628; AID1067347; AID1126958; AID1126960; AID1127318; AID1128555; AID1129004; AID1139706; AID1141243; AID1141761; AID1141787; AID1164025; AID1164781; AID1164907; AID1168913; AID1173500; AID1174680; AID1174693; AID1177043; AID1178596; AID1201642; AID1203890; AID1205625; AID1206736; AID1206763; AID1225984; AID1227030; AID1231808; AID1234887; AID1235108; AID1235256; AID1240548; AID1246508; AID1248356; AID1250641; AID1251315; AID1256443; AID1266093; AID1266808; AID1273866; AID1273870; AID1274872; AID1275076; AID1275247; AID1275591; AID1275632; AID1275635; AID1276240; AID1279124; AID1279125; AID1282238; AID1293553; AID1293554; AID1308511; AID1312867; AID1321619; AID1321701; AID1326520; AID1339568; AID1340594; AID1341595; AID1341621; AID1341623; AID1348916; AID1349724; AID1352481; AID1361632; AID1365023; AID1380938; AID1380953; AID1383985; AID1383986; AID1384207; AID1390009; AID1390011; AID1390020; AID1393286; AID1394888; AID1401341; AID1401373; AID1401903; AID1409640; AID1409641; AID1409642; AID1415637; AID1449217; AID1451829; AID1459954; AID1466055; AID1478590; AID1482098; AID1486678; AID1487000; AID1487093; AID1493592; AID1502987; AID1511131; AID1525778; AID1541445; AID1541452; AID1541453; AID1541563; AID1541565; AID1542180; AID1545761; AID1547273; AID1548244; AID1548246; AID1548256; AID1548727; AID1549163; AID1550094; AID1550100; AID1563941; AID1566038; AID1566803; AID1578147; AID1578156; AID1587864; AID1597974; AID1600658; AID1600732; AID1600735; AID1614127; AID1622907; AID1622908; AID1622912; AID1622930; AID1622954; AID1622961; AID1622976; AID1622984; AID1623524; AID1639362; AID1650413; AID1650415; AID1655788; AID1659646; AID1659648; AID1677511; AID1677516; AID1688024; AID1690106; AID1690833; AID1690843; AID1697196; AID1697200; AID1702061; AID1720096; AID1730854; AID1737134; AID1742178; AID1753838; AID1754752; AID1758466; AID1759721; AID1759727; AID1759728; AID1762488; AID1762496; AID1764247; AID1764248; AID1764251; AID1764288; AID1764292; AID1765325; AID1769649; AID1771467; AID1775546; AID1775564; AID1783109; AID1784986; AID1785333; AID1798419; AID1798524; AID1800141; AID1801572; AID1802356; AID1802398; AID1802589; AID1802920; AID1808547; AID1812439; AID1812443; AID1816710; AID1819502; AID1819504; AID1821271; AID1821957; AID1825921; AID1832670; AID1832686; AID1832804; AID1846147; AID1848558; AID1848559; AID1848583; AID1855242; AID1861251; AID1861258; AID1861654; AID1863434; AID1864216; AID1864240; AID1865258; AID1865262; AID1873382; AID1873404; AID1873405; AID1873406; AID1873407; AID1873408; AID1882457; AID1886184; AID1888420; AID1890309; AID1890511; AID1893824; AID1897373; AID1899585; AID1901055; AID1901148; AID1915563; AID1915571; AID1915594; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310123; AID310180; AID313730; AID316872; AID316875; AID316877; AID316878; AID328794; AID331898; AID343689; AID343690; AID348797; AID350715; AID350717; AID352519; AID352747; AID353356; AID366641; AID373073; AID373075; AID374817; AID382342; AID408881; AID411253; AID420326; AID420502; AID438216; AID440820; AID449260; AID456795; AID459821; AID461250; AID463865; AID465150; AID473175; AID480067; AID480068; AID487873; AID488237; AID488274; AID499799; AID511064; AID525001; AID527317; AID539709; AID541645; AID545854; AID546545; AID591330; AID593546; AID594124; AID603542; AID605298; AID605393; AID608776; AID615998; AID622254; AID626565; AID628436; AID631667; AID655477; AID659492; AID663331; AID669756; AID669762; AID670514; AID672023; AID672025; AID673991; AID675299; AID708770; AID711158; AID717827; AID723465; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID725669; AID732154; AID732876; AID732878; AID737916; AID748113; AID748984; AID749705; AID750109; AID753148; AID753167; AID755627; AID760511; AID761584; AID764219; AID775843; AID780575; AID781051; AID80353; AID90195; AID90211; AID90212; AID90214; AID90340; AID90342; AID90347; AID90350; AID90351; AID90352; AID90353; AID90529; AID90685
Histone deacetylase 2Homo sapiens (human)Ki0.34470.00000.47098.1900AID1170741; AID1600731; AID1650412; AID447579; AID482942; AID496802; AID619047; AID765392
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
HD2 type histone deacetylase HDA106 Zea maysIC50 (µMol)0.22270.00300.17372.0000AID241474; AID255813; AID273166; AID90197; AID90359; AID90682; AID90687; AID90689; AID90690; AID90691; AID90696
HD2 type histone deacetylase HDA106 Zea maysKi0.13180.00440.06810.1318AID90199; AID90693
Polyamine deacetylase HDAC10Homo sapiens (human)IC50 (µMol)1.57710.00050.72459.9000AID1061951; AID1063036; AID1063059; AID1126958; AID1127331; AID1128562; AID1129012; AID1139706; AID1141243; AID1141761; AID1164033; AID1164785; AID1164915; AID1173506; AID1174680; AID1177047; AID1201642; AID1205625; AID1246512; AID1250649; AID1256443; AID1266808; AID1273866; AID1274880; AID1275076; AID1275247; AID1275632; AID1282244; AID1293553; AID1293571; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1482104; AID1511139; AID1541452; AID1541453; AID1542188; AID1545761; AID1547264; AID1549163; AID1550094; AID1566811; AID1578147; AID1578156; AID1587859; AID1587860; AID1597974; AID1600732; AID1600735; AID1614131; AID1622907; AID1622908; AID1622938; AID1622954; AID1622964; AID1623532; AID1639362; AID1650413; AID1650415; AID1659646; AID1677516; AID1690106; AID1697196; AID1702069; AID1720096; AID1742185; AID1758470; AID1762488; AID1764247; AID1764248; AID1764288; AID1764292; AID1771467; AID1798419; AID1802398; AID1812439; AID1816191; AID1819502; AID1821957; AID1832670; AID1846147; AID1848558; AID1848559; AID1861251; AID1864216; AID1864240; AID1865258; AID1865268; AID1873390; AID1888420; AID1893824; AID1901148; AID1915571; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID316872; AID316875; AID316877; AID316878; AID331898; AID343689; AID343690; AID350715; AID352520; AID353356; AID366645; AID373073; AID382342; AID420326; AID456795; AID459821; AID461250; AID463865; AID465153; AID473175; AID487873; AID499799; AID511067; AID524995; AID527317; AID539709; AID541653; AID545854; AID546545; AID591330; AID593555; AID603542; AID605298; AID608776; AID615998; AID622254; AID626565; AID652754; AID663331; AID669756; AID670514; AID675299; AID708770; AID717827; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID732878; AID749705; AID750109; AID753167; AID755627; AID760503; AID761584; AID764219; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Polyamine deacetylase HDAC10Homo sapiens (human)Ki0.65500.00000.76878.1900AID1170745; AID447579; AID482949; AID619055
Histone deacetylase 11 Homo sapiens (human)IC50 (µMol)3.38670.00030.92989.9000AID1061949; AID1063035; AID1063059; AID1126958; AID1127332; AID1128563; AID1129013; AID1139706; AID1141243; AID1141761; AID1164034; AID1164786; AID1164916; AID1174680; AID1177048; AID1201642; AID1205625; AID1206768; AID1246513; AID1250650; AID1256443; AID1266808; AID1273866; AID1275076; AID1275247; AID1275632; AID1275639; AID1282245; AID1293553; AID1293572; AID1294805; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1467234; AID1482105; AID1511140; AID1541452; AID1541453; AID1542189; AID1545761; AID1547263; AID1549163; AID1550094; AID1566812; AID1578147; AID1578156; AID1578478; AID1597974; AID1600732; AID1600735; AID1614137; AID1622907; AID1622908; AID1622939; AID1622954; AID1623533; AID1639362; AID1650413; AID1650415; AID1659646; AID1677516; AID1690106; AID1697196; AID1720096; AID1727743; AID1742186; AID1751997; AID1762488; AID1764247; AID1764248; AID1764288; AID1764292; AID1771467; AID1785341; AID1794854; AID1802239; AID1808542; AID1812439; AID1816712; AID1819502; AID1821957; AID1832670; AID1846147; AID1848558; AID1848559; AID1861251; AID1864216; AID1864240; AID1865239; AID1865258; AID1873391; AID1876344; AID1888420; AID1893824; AID1901148; AID1901764; AID1915571; AID1915597; AID1917542; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID316872; AID316875; AID316877; AID316878; AID331898; AID343689; AID343690; AID350715; AID353356; AID373073; AID382342; AID420326; AID456795; AID459821; AID461250; AID463865; AID473175; AID487873; AID499799; AID527317; AID539709; AID541654; AID545854; AID546545; AID591330; AID593556; AID603542; AID605298; AID608776; AID615998; AID622254; AID626565; AID652755; AID663331; AID669756; AID670514; AID675299; AID708770; AID717827; AID723460; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID732878; AID749705; AID750109; AID753167; AID755627; AID760502; AID761584; AID764219; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 11 Homo sapiens (human)Ki0.51260.00011.21478.1900AID1170746; AID447579; AID482950; AID619056; AID765383
Carboxypeptidase B2Homo sapiens (human)IC50 (µMol)0.36200.00150.54291.8000AID1129013
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC50 (µMol)10.00000.00251.14809.2000AID1775567
Histone deacetylase 7Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Histone deacetylase 6 Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Histone deacetylase 4Rattus norvegicus (Norway rat)IC50 (µMol)0.16500.00280.35173.5120AID90522
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)2.23480.00070.99479.9000AID1061950; AID1063055; AID1063059; AID1065632; AID1065967; AID1126958; AID1127329; AID1128561; AID1129010; AID1139706; AID1141243; AID1141761; AID1164027; AID1164784; AID1164913; AID1173505; AID1174680; AID1177046; AID1178598; AID1200973; AID1201642; AID1202585; AID1203891; AID1205625; AID1206767; AID1225981; AID1227033; AID1231809; AID1246510; AID1250643; AID1256443; AID1266808; AID1266820; AID1273866; AID1274878; AID1275076; AID1275247; AID1275632; AID1275637; AID1279129; AID1280261; AID1280309; AID1282231; AID1293553; AID1293569; AID1296347; AID1308511; AID1312867; AID1322159; AID1326522; AID1339571; AID1340594; AID1341595; AID1341621; AID1341623; AID1348918; AID1349726; AID1361635; AID1380938; AID1380956; AID1383988; AID1390009; AID1390014; AID1390020; AID1394888; AID1401341; AID1401376; AID1403155; AID1409640; AID1409641; AID1409642; AID1415637; AID1449218; AID1449328; AID1451833; AID1464872; AID1466064; AID1478593; AID1482100; AID1487003; AID1487095; AID1511137; AID1525780; AID1533327; AID1541452; AID1541453; AID1541457; AID1541563; AID1541565; AID1543945; AID1545761; AID1547266; AID1548250; AID1548256; AID1549163; AID1550094; AID1550102; AID1563944; AID1566041; AID1566805; AID1572344; AID1578147; AID1578156; AID1578477; AID1578889; AID1587866; AID1597927; AID1597974; AID1600732; AID1600735; AID1614129; AID1622907; AID1622908; AID1622936; AID1622954; AID1622963; AID1622974; AID1622978; AID1622986; AID1631200; AID1639362; AID1649884; AID1650413; AID1650415; AID1652193; AID1655793; AID1659646; AID1659652; AID1667068; AID1677510; AID1677516; AID1690106; AID1690833; AID1697196; AID1699974; AID1720096; AID1727742; AID1737135; AID1742180; AID1751996; AID1753840; AID1758469; AID1759721; AID1759727; AID1759728; AID1762488; AID1763821; AID1764247; AID1764248; AID1764254; AID1764288; AID1764292; AID1764801; AID1765328; AID1771467; AID1783110; AID1784187; AID1784988; AID1785339; AID1794854; AID1794865; AID1798419; AID1798524; AID1798784; AID1801572; AID1802059; AID1802239; AID1802356; AID1802398; AID1812439; AID1816188; AID1816711; AID1819502; AID1819506; AID1821274; AID1821957; AID1821961; AID1825927; AID1832670; AID1832692; AID1846147; AID1848558; AID1848559; AID1848586; AID1855245; AID1861251; AID1861262; AID1861657; AID1863440; AID1864216; AID1864225; AID1864240; AID1865258; AID1865264; AID1873388; AID1876343; AID1882467; AID1886187; AID1888420; AID1890311; AID1890514; AID1893824; AID1897374; AID1899585; AID1901148; AID1901154; AID1901763; AID1915571; AID1915595; AID1917541; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID313736; AID316872; AID316875; AID316877; AID316878; AID316893; AID316910; AID328801; AID331898; AID343689; AID343690; AID348803; AID350715; AID350718; AID352751; AID353356; AID366643; AID373073; AID373081; AID374822; AID382342; AID408883; AID411254; AID420326; AID438217; AID441872; AID456795; AID459821; AID461250; AID462789; AID463865; AID465152; AID473175; AID482941; AID487873; AID488277; AID489911; AID499799; AID499800; AID524996; AID527317; AID539709; AID541647; AID545854; AID546545; AID546550; AID591330; AID593553; AID594125; AID603542; AID605298; AID608776; AID615998; AID616003; AID622254; AID623021; AID626565; AID628439; AID652752; AID652764; AID659495; AID663331; AID669756; AID670514; AID675299; AID689653; AID704015; AID708770; AID711157; AID717827; AID723461; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID729522; AID732151; AID732878; AID734738; AID744378; AID748106; AID748978; AID749702; AID749705; AID750109; AID753167; AID755627; AID759303; AID760505; AID761584; AID764219; AID764647; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529; AID90839
Histone deacetylase 8Homo sapiens (human)Ki2.08450.00020.75258.1900AID1170743; AID1503585; AID1600728; AID1650409; AID1798196; AID441872; AID447579; AID482941; AID496808; AID619053; AID760388; AID765390
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC50 (µMol)100.00000.10003.38006.6000AID699752
REST corepressor 3Homo sapiens (human)Ki0.00300.00300.00300.0030AID1389960
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)1.28670.00000.53769.9000AID1055353; AID1061952; AID1063037; AID1063059; AID1065633; AID1065968; AID1126958; AID1126962; AID1127327; AID1128559; AID1129008; AID1139706; AID1141243; AID1141761; AID1141788; AID1164032; AID1164187; AID1164783; AID1164911; AID1165117; AID1166498; AID1173495; AID1174680; AID1174695; AID1177045; AID1178601; AID1181305; AID1200972; AID1201642; AID1202584; AID1205625; AID1206766; AID1225982; AID1227032; AID1233269; AID1234890; AID1239050; AID1246511; AID1250648; AID1251317; AID1256443; AID1263145; AID1266095; AID1266808; AID1266819; AID1273866; AID1273872; AID1274876; AID1275076; AID1275078; AID1275247; AID1275632; AID1275634; AID1280260; AID1280308; AID1281850; AID1282230; AID1293553; AID1293567; AID1296349; AID1308511; AID1312867; AID1321703; AID1326521; AID1330927; AID1337196; AID1339570; AID1340594; AID1341595; AID1341621; AID1341623; AID1348923; AID1349716; AID1352483; AID1361634; AID1365024; AID1373246; AID1380938; AID1380955; AID1383987; AID1384209; AID1390009; AID1390013; AID1390020; AID1390963; AID1394888; AID1396986; AID1398799; AID1399544; AID1401341; AID1401375; AID1401904; AID1403154; AID1409640; AID1409641; AID1409642; AID1415637; AID1418666; AID1421603; AID1421912; AID1437239; AID1439350; AID1449215; AID1449327; AID1451830; AID1452274; AID1459955; AID1464871; AID1466063; AID1476121; AID1478592; AID1486294; AID1487002; AID1487096; AID1493591; AID1503841; AID1511133; AID1511968; AID1518780; AID1525776; AID1533326; AID1535340; AID1537555; AID1541443; AID1541452; AID1541453; AID1543944; AID1545761; AID1547272; AID1548249; AID1548729; AID1549163; AID1549165; AID1550094; AID1550101; AID1558003; AID1563943; AID1566040; AID1566810; AID1572342; AID1578147; AID1578156; AID1578476; AID1578888; AID1591716; AID1597932; AID1597974; AID1600656; AID1600732; AID1600735; AID1614130; AID1622906; AID1622907; AID1622908; AID1622910; AID1622914; AID1622934; AID1622954; AID1622965; AID1622985; AID1623531; AID1633654; AID1639362; AID1650413; AID1650415; AID1652192; AID1655792; AID1658891; AID1659236; AID1659646; AID1659650; AID1667067; AID1677516; AID1688026; AID1690106; AID1690838; AID1697196; AID1697202; AID1699973; AID1702065; AID1707508; AID1720096; AID1722283; AID1723743; AID1727730; AID1742175; AID1751995; AID1752944; AID1753635; AID1753834; AID1758468; AID1762488; AID1762492; AID1763822; AID1764247; AID1764248; AID1764253; AID1764288; AID1764292; AID1764799; AID1764816; AID1765327; AID1769650; AID1771467; AID1775548; AID1775566; AID1777022; AID1783107; AID1784193; AID1784989; AID1785337; AID1794854; AID1798419; AID1798524; AID1798526; AID1800141; AID1801572; AID1802239; AID1802356; AID1802398; AID1810052; AID1811362; AID1812439; AID1812445; AID1816184; AID1816689; AID1819502; AID1819505; AID1819859; AID1821273; AID1821957; AID1821960; AID1825926; AID1832670; AID1832690; AID1832800; AID1845460; AID1846147; AID1847778; AID1848280; AID1848558; AID1848559; AID1848584; AID1849158; AID1855244; AID1856989; AID1861251; AID1861261; AID1861656; AID1863169; AID1863438; AID1864216; AID1864227; AID1864240; AID1865258; AID1865267; AID1873386; AID1876342; AID1876462; AID1882462; AID1886186; AID1888420; AID1888582; AID1890308; AID1890513; AID1893824; AID1895827; AID1897366; AID1897806; AID1901057; AID1901148; AID1901155; AID1901762; AID1915524; AID1915538; AID1915564; AID1915571; AID1917529; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID303349; AID304373; AID310180; AID313734; AID316872; AID316875; AID316877; AID316878; AID316899; AID324956; AID328799; AID331898; AID331900; AID343688; AID343689; AID343690; AID348799; AID350715; AID350719; AID352518; AID352750; AID353356; AID366644; AID373073; AID373079; AID374820; AID382342; AID392399; AID408885; AID411256; AID414718; AID420326; AID438219; AID456795; AID459821; AID461250; AID463865; AID465154; AID473175; AID487873; AID488239; AID488276; AID499799; AID499802; AID511066; AID524999; AID527317; AID538409; AID539709; AID541652; AID545854; AID546545; AID546548; AID591330; AID593551; AID603542; AID603543; AID605298; AID605396; AID608776; AID609507; AID615998; AID616005; AID622254; AID622257; AID626565; AID631669; AID652750; AID652763; AID659494; AID663331; AID669756; AID669763; AID670012; AID670514; AID670972; AID673993; AID675299; AID708770; AID711155; AID717825; AID717827; AID723462; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID732152; AID732874; AID732878; AID734740; AID737915; AID748109; AID748981; AID749388; AID749703; AID749705; AID750109; AID753146; AID753167; AID755627; AID759304; AID760507; AID761582; AID761584; AID764219; AID780575; AID780586; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529; AID90702
Histone deacetylase 6Homo sapiens (human)Ki0.30470.00010.41568.1900AID1170744; AID1578479; AID1600729; AID1650410; AID1798196; AID1802011; AID331900; AID385230; AID447579; AID482946; AID482947; AID496806; AID619051; AID765385
Histone deacetylase 9Homo sapiens (human)IC50 (µMol)6.16910.00050.94139.9000AID1063059; AID1065635; AID1126958; AID1127330; AID1129011; AID1139706; AID1141243; AID1141761; AID1164031; AID1164914; AID1174680; AID1178600; AID1201642; AID1205625; AID1246517; AID1250647; AID1256443; AID1266808; AID1273866; AID1275076; AID1275247; AID1275632; AID1282243; AID1293553; AID1293570; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1348922; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1482103; AID1511138; AID1541452; AID1541453; AID1545761; AID1547265; AID1549163; AID1550094; AID1566809; AID1578147; AID1578156; AID1597974; AID1600732; AID1600735; AID1614136; AID1622907; AID1622908; AID1622937; AID1622954; AID1623530; AID1639362; AID1650413; AID1650415; AID1659646; AID1677516; AID1690106; AID1690837; AID1697196; AID1720096; AID1742184; AID1754757; AID1762488; AID1762491; AID1764247; AID1764248; AID1764288; AID1764292; AID1771467; AID1785340; AID1801572; AID1802398; AID1812439; AID1819502; AID1821957; AID1832670; AID1832693; AID1846147; AID1848558; AID1848559; AID1861251; AID1863441; AID1864216; AID1864240; AID1865258; AID1873389; AID1888420; AID1893824; AID1901148; AID1915571; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID316872; AID316875; AID316877; AID316878; AID331898; AID343689; AID343690; AID350715; AID353356; AID373073; AID373082; AID382342; AID420326; AID456795; AID459821; AID461250; AID463865; AID473175; AID487873; AID499799; AID524994; AID527317; AID539709; AID541651; AID545854; AID546545; AID591330; AID593554; AID603542; AID605298; AID608776; AID615998; AID622254; AID626565; AID663331; AID669756; AID670514; AID675299; AID708770; AID717827; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID725667; AID732142; AID732878; AID748107; AID749705; AID750109; AID753167; AID755627; AID760504; AID761584; AID764219; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 9Homo sapiens (human)Ki1.14600.00021.85209.0000AID385231; AID447579; AID482948; AID619054
Histone deacetylase 5Homo sapiens (human)IC50 (µMol)4.09410.00070.961010.0000AID1063059; AID1065637; AID1126958; AID1127326; AID1128558; AID1129007; AID1139706; AID1141243; AID1141761; AID1164029; AID1164910; AID1174680; AID1201642; AID1205625; AID1246515; AID1250645; AID1256443; AID1266808; AID1273866; AID1274875; AID1275076; AID1275247; AID1275632; AID1282241; AID1293553; AID1293566; AID1308511; AID1312867; AID1340594; AID1341595; AID1341621; AID1341623; AID1348920; AID1380938; AID1390009; AID1390020; AID1394888; AID1401341; AID1409640; AID1409641; AID1409642; AID1415637; AID1482102; AID1511135; AID1541452; AID1541453; AID1545761; AID1547267; AID1549163; AID1550094; AID1566807; AID1578147; AID1578156; AID1597974; AID1600732; AID1600735; AID1614134; AID1622907; AID1622908; AID1622933; AID1622954; AID1623528; AID1639362; AID1650413; AID1650415; AID1655791; AID1659646; AID1677516; AID1690106; AID1690836; AID1697196; AID1720096; AID1742182; AID1754755; AID1762488; AID1764247; AID1764248; AID1764288; AID1764292; AID1771467; AID1785336; AID1798524; AID1801572; AID1802356; AID1802398; AID1812439; AID1819502; AID1821957; AID1832670; AID1832689; AID1846147; AID1848558; AID1848559; AID1861251; AID1864216; AID1864240; AID1865258; AID1865265; AID1873385; AID1888420; AID1893824; AID1901148; AID1915571; AID1915598; AID240505; AID240810; AID258011; AID269668; AID288446; AID292436; AID294382; AID297470; AID300832; AID303347; AID304373; AID310180; AID313733; AID316872; AID316875; AID316877; AID316878; AID331898; AID343689; AID343690; AID348801; AID350715; AID353356; AID373073; AID373078; AID374819; AID382342; AID420326; AID440822; AID456795; AID459821; AID461250; AID463865; AID473175; AID487873; AID499799; AID524998; AID527317; AID539709; AID541649; AID545854; AID546545; AID591330; AID593550; AID603542; AID605298; AID605395; AID608776; AID615998; AID622254; AID626565; AID652749; AID663331; AID669756; AID670514; AID675299; AID708770; AID717827; AID723463; AID723467; AID723468; AID723469; AID723470; AID723471; AID723472; AID723479; AID723726; AID729522; AID732144; AID732878; AID744378; AID748110; AID749705; AID750109; AID753167; AID755627; AID760508; AID761584; AID764219; AID764647; AID780575; AID781051; AID80353; AID90195; AID90211; AID90340; AID90342; AID90350; AID90351; AID90352; AID90353; AID90529
Histone deacetylase 5Homo sapiens (human)Ki3.62780.00021.29939.5000AID1439781; AID447579; AID482945; AID496805; AID619050
Histone deacetylase Plasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)0.09450.00060.16880.9400AID414980; AID499814
Nuclear receptor corepressor 2Homo sapiens (human)IC50 (µMol)0.09050.00170.59528.0000AID1061953; AID1128556; AID1129005; AID1225983; AID1293565; AID1348917; AID1390012; AID1398800; AID1449216; AID1541444; AID1548728; AID1566039; AID1566804; AID1587865; AID1600657; AID1622931; AID1622977; AID1688025; AID1690844; AID1702062; AID1754753; AID1775565; AID1785334; AID1808546; AID1832687; AID331899; AID594123; AID628440; AID652747; AID652762; AID673992
Nuclear receptor corepressor 2Homo sapiens (human)Ki0.00200.00030.33253.2000AID331899
Histone deacetylase 6Mus musculus (house mouse)IC50 (µMol)0.37420.00060.20660.7870AID1797826; AID1801045
Histone deacetylase Zea maysIC50 (µMol)0.02900.00040.01330.0300AID273168; AID384316
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 3Homo sapiens (human)EC50 (µMol)2.81970.03001.85126.7000AID1312869; AID1404339; AID1599722; AID1664945; AID297472; AID343694; AID371221; AID414719
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)30.30000.00203.519610.0000AID1215086; AID1215094
Protein TatHIV-1 M:B_HXB2REC50 (µMol)2.30000.13003.51008.1000AID1598103
Histone deacetylase 4Homo sapiens (human)EC50 (µMol)3.43000.03002.35236.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 1Homo sapiens (human)EC50 (µMol)2.81970.03001.98776.7000AID1312869; AID1404339; AID1599722; AID1664945; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 1Homo sapiens (human)Kd0.12830.01210.10490.2820AID1802399; AID637888
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188Kd0.30000.30000.30000.3000AID637887
Histone deacetylase 7Homo sapiens (human)EC50 (µMol)3.43000.03002.32116.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 2Homo sapiens (human)EC50 (µMol)2.81970.03001.85756.7000AID1312869; AID1404339; AID1599722; AID1664945; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 2Homo sapiens (human)Kd0.17250.01210.11300.2820AID1802399
Polyamine deacetylase HDAC10Homo sapiens (human)EC50 (µMol)3.43000.03002.54656.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 11 Homo sapiens (human)EC50 (µMol)3.43000.03002.54656.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 8Homo sapiens (human)EC50 (µMol)3.16860.03002.27346.7000AID1404339; AID1599722; AID1664945; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 8Homo sapiens (human)Kd2.87000.00312.59269.1600AID1260656; AID1800408; AID1800409; AID637891
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC50 (µMol)2.50000.01004.139410.0000AID1215090
Histone deacetylase 6Homo sapiens (human)EC50 (µMol)2.13280.00521.59986.7000AID1164902; AID1200970; AID1266100; AID1312868; AID1404339; AID1599722; AID1702141; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 6Homo sapiens (human)Kd0.30000.30000.30000.3000AID637889
Histone deacetylase 9Homo sapiens (human)EC50 (µMol)3.43000.03002.32666.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
Histone deacetylase 5Homo sapiens (human)EC50 (µMol)3.43000.03002.54656.7000AID1404339; AID1599722; AID297472; AID343694; AID371221; AID414719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PAX8Homo sapiens (human)AC504.58000.04885.435469.1700AID687027
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC500.93300.039815.002550.0000AID743267
Histone deacetylase 3Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 3Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 3Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Cytochrome P450 3A4Homo sapiens (human)INH24.80001.70002.85004.0000AID663472
Histone deacetylase 4Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 4Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 4Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 1Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 1Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 1Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 7Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 7Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 7Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 2Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 2Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 2Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Polyamine deacetylase HDAC10Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Polyamine deacetylase HDAC10Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Polyamine deacetylase HDAC10Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 11 Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 11 Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 11 Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 8Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 8Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 8Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 6Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 6Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 6Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 9Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 9Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 9Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
Histone deacetylase 5Homo sapiens (human)AC503.10000.01002.70207.9000AID90344
Histone deacetylase 5Homo sapiens (human)INH0.18850.02440.24340.5720AID1622899; AID603218
Histone deacetylase 5Homo sapiens (human)Inhibition0.08000.00350.04170.0800AID243634
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (1116)

Processvia Protein(s)Taxonomy
regulation of gene expressionLysine-specific demethylase 4EHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 4EHomo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of protein ubiquitinationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of protein localizationLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to UVLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to gamma radiationLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair-dependent chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuroblast proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
protein demethylationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuron projection developmentLysine-specific histone demethylase 1AHomo sapiens (human)
cerebral cortex developmentLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
neuron maturationLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cell sizeLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-templated transcriptionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
guanine metabolic processLysine-specific histone demethylase 1AHomo sapiens (human)
muscle cell developmentLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of androgen receptor signaling pathwayLysine-specific histone demethylase 1AHomo sapiens (human)
response to fungicideLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to cAMPLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cold-induced thermogenesisLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neural precursor cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of stem cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of platelet aggregationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of platelet activationTyrosine-protein kinase JAK2Homo sapiens (human)
response to antibioticTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of SMAD protein signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
microglial cell activationTyrosine-protein kinase JAK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
chromatin remodelingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
G protein-coupled receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
mesoderm developmentTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell-substrate adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
response to amineTyrosine-protein kinase JAK2Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase JAK2Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase JAK2Homo sapiens (human)
axon regenerationTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular mineralocorticoid receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of insulin secretionTyrosine-protein kinase JAK2Homo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-1 beta productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-17 productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of natural killer cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to hydroperoxideTyrosine-protein kinase JAK2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
symbiont-induced defense-related programmed cell deathTyrosine-protein kinase JAK2Homo sapiens (human)
response to tumor necrosis factorTyrosine-protein kinase JAK2Homo sapiens (human)
post-embryonic hemopoiesisTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to interleukin-3Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
collagen-activated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-3-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte-macrophage colony-stimulating factor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of protein import into nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
activation of Janus kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of DNA bindingTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
post-translational protein modificationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MHC class II biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of inflammatory responseTyrosine-protein kinase JAK2Homo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of NK T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
mammary gland epithelium developmentTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of leukocyte proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to interleukin-12Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-35-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to dexamethasone stimulusTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth factor dependent skeletal muscle satellite cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of epithelial cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of signaling receptor activityTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 1Homo sapiens (human)
chromatin organizationNuclear receptor corepressor 1Homo sapiens (human)
locomotor rhythmNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of glycolytic processNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of fatty acid metabolic processNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of JNK cascadeNuclear receptor corepressor 1Homo sapiens (human)
spindle assemblyNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of phospholipase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
neural tube closureTyrosine-protein kinase ABL1Homo sapiens (human)
B-1 B cell homeostasisTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of protein phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
B cell proliferation involved in immune responseTyrosine-protein kinase ABL1Homo sapiens (human)
transitional one stage B cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
mismatch repairTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of DNA-templated transcriptionTyrosine-protein kinase ABL1Homo sapiens (human)
autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
DNA damage responseTyrosine-protein kinase ABL1Homo sapiens (human)
integrin-mediated signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
associative learningTyrosine-protein kinase ABL1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
post-embryonic developmentTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
cerebellum morphogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
microspike assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of endocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
neuron differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of axon extensionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of microtubule polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of Cdc42 protein signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of interleukin-2 productionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of osteoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
response to endoplasmic reticulum stressTyrosine-protein kinase ABL1Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein modification processTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
signal transduction in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of vasoconstrictionTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase ABL1Homo sapiens (human)
alpha-beta T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of fibroblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
spleen developmentTyrosine-protein kinase ABL1Homo sapiens (human)
thymus developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
activated T cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
neuromuscular process controlling balanceTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of oxidoreductase activityTyrosine-protein kinase ABL1Homo sapiens (human)
neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
myoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of stress fiber assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
establishment of localization in cellTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrial depolarizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of focal adhesion assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
Bergmann glial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cardiac muscle cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
neuroepithelial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase ABL1Homo sapiens (human)
ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
DNA conformation changeTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
response to epinephrineTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of protein serine/threonine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of dendrite developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of long-term synaptic potentiationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of hematopoietic stem cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of extracellular matrix organizationTyrosine-protein kinase ABL1Homo sapiens (human)
podocyte apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to dopamineTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of establishment of T cell polarityTyrosine-protein kinase ABL1Homo sapiens (human)
DN4 thymocyte differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein localization to cytoplasmic microtubule plus-endTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of microtubule bindingTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of modification of synaptic structureTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of blood vessel branchingTyrosine-protein kinase ABL1Homo sapiens (human)
activation of protein kinase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of Wnt signaling pathway, planar cell polarity pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell motilityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of T cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
epidermal growth factor receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
cholesterol biosynthetic process3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
visual learning3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
coenzyme A metabolic process3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
negative regulation of protein catabolic process3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
negative regulation of protein secretion3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
long-term synaptic potentiation3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
regulation of ERK1 and ERK2 cascade3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
negative regulation of amyloid-beta clearance3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
isoprenoid biosynthetic process3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
sterol biosynthetic process3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
cognitionAmyloid-beta precursor proteinHomo sapiens (human)
G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglial cell activationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
suckling behaviorAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activation involved in immune responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of translationAmyloid-beta precursor proteinHomo sapiens (human)
protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
intracellular copper ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
endocytosisAmyloid-beta precursor proteinHomo sapiens (human)
response to oxidative stressAmyloid-beta precursor proteinHomo sapiens (human)
cell adhesionAmyloid-beta precursor proteinHomo sapiens (human)
regulation of epidermal growth factor-activated receptor activityAmyloid-beta precursor proteinHomo sapiens (human)
Notch signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
axonogenesisAmyloid-beta precursor proteinHomo sapiens (human)
learning or memoryAmyloid-beta precursor proteinHomo sapiens (human)
learningAmyloid-beta precursor proteinHomo sapiens (human)
mating behaviorAmyloid-beta precursor proteinHomo sapiens (human)
locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
axo-dendritic transportAmyloid-beta precursor proteinHomo sapiens (human)
cholesterol metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of cell population proliferationAmyloid-beta precursor proteinHomo sapiens (human)
adult locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
visual learningAmyloid-beta precursor proteinHomo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglia developmentAmyloid-beta precursor proteinHomo sapiens (human)
axon midline choice point recognitionAmyloid-beta precursor proteinHomo sapiens (human)
neuron remodelingAmyloid-beta precursor proteinHomo sapiens (human)
dendrite developmentAmyloid-beta precursor proteinHomo sapiens (human)
regulation of Wnt signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
extracellular matrix organizationAmyloid-beta precursor proteinHomo sapiens (human)
forebrain developmentAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection developmentAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of chemokine productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-1 beta productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-6 productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of tumor necrosis factor productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of multicellular organism growthAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of neuron differentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of glycolytic processAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of JNK cascadeAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAmyloid-beta precursor proteinHomo sapiens (human)
collateral sprouting in absence of injuryAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of inflammatory responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of synapse structure or activityAmyloid-beta precursor proteinHomo sapiens (human)
synapse organizationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular process controlling balanceAmyloid-beta precursor proteinHomo sapiens (human)
synaptic assembly at neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
neuron apoptotic processAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
neuron cellular homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAmyloid-beta precursor proteinHomo sapiens (human)
response to interleukin-1Amyloid-beta precursor proteinHomo sapiens (human)
modulation of excitatory postsynaptic potentialAmyloid-beta precursor proteinHomo sapiens (human)
NMDA selective glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of spontaneous synaptic transmissionAmyloid-beta precursor proteinHomo sapiens (human)
cytosolic mRNA polyadenylationAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionAmyloid-beta precursor proteinHomo sapiens (human)
cellular response to amyloid-betaAmyloid-beta precursor proteinHomo sapiens (human)
regulation of presynapse assemblyAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection maintenanceAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of T cell migrationAmyloid-beta precursor proteinHomo sapiens (human)
central nervous system developmentAmyloid-beta precursor proteinHomo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-alphaHomo sapiens (human)
neuron migrationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein phosphorylationHeat shock protein HSP 90-alphaHomo sapiens (human)
activation of innate immune responseHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of defense response to virus by hostHeat shock protein HSP 90-alphaHomo sapiens (human)
skeletal muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrial transportHeat shock protein HSP 90-alphaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-alphaHomo sapiens (human)
response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
response to coldHeat shock protein HSP 90-alphaHomo sapiens (human)
response to xenobiotic stimulusHeat shock protein HSP 90-alphaHomo sapiens (human)
response to salt stressHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of lamellipodium assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cardiac muscle cell apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein polymerizationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of interferon-beta productionHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-alphaHomo sapiens (human)
protein refoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to cocaineHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein import into nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein-containing complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
protein unfoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to estrogenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein insertion into mitochondrial outer membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein catabolic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cell sizeHeat shock protein HSP 90-alphaHomo sapiens (human)
response to antibioticHeat shock protein HSP 90-alphaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cardiac muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated autophagyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to virusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of tau-protein kinase activityHeat shock protein HSP 90-alphaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-alphaHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
proteolysisLeukotriene A-4 hydrolaseHomo sapiens (human)
lipid metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to zinc ionLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene biosynthetic processLeukotriene A-4 hydrolaseHomo sapiens (human)
protein metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
peptide catabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to peptide hormoneLeukotriene A-4 hydrolaseHomo sapiens (human)
type I pneumocyte differentiationLeukotriene A-4 hydrolaseHomo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
ossificationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
negative regulation of adaptive immune responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
phosphatidylethanolamine biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
inflammatory responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of cell-substrate adhesionPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
fatty acid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
bone mineralizationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of actin filament polymerizationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
response to endoplasmic reticulum stressPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cellular response to interleukin-13Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
wound healingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
apoptotic cell clearancePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cellular response to calcium ionPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of engulfment of apoptotic cellPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
leukotriene A4 metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
negative regulation of muscle cell apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
fatty acid oxidationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
unsaturated fatty acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
superoxide anion generationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
establishment of skin barrierPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
negative regulation of platelet aggregationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
leukotriene A4 metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxin B4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA-templated transcriptionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
positive regulation of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
methylationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
epigenetic programming of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
cellular response to amino acid stimulusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
chromosomal DNA methylation maintenance following DNA replicationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
cellular response to bisphenol ADNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell apoptotic processDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell differentiation involved in phenotypic switchingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
intracellular glucose homeostasisPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
negative regulation of cell-matrix adhesionPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of leukocyte migrationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
transcription by RNA polymerase IIPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
protein import into nucleusPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
immune responsePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damagePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of lamellipodium assemblyPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cytokine-mediated signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
B cell differentiationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
T cell differentiationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
osteoclast differentiationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of tumor necrosis factor productionPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cellular response to insulin stimulusPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of RNA splicingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
regulation of toll-like receptor 4 signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
substrate adhesion-dependent cell spreadingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cellular response to UVPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
response to endoplasmic reticulum stressPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
interleukin-18-mediated signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
natural killer cell mediated cytotoxicityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of protein import into nucleusPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
negative regulation of apoptotic processPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
negative regulation of osteoclast differentiationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of glucose importPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
protein stabilizationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of filopodium assemblyPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
negative regulation of stress fiber assemblyPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
growth hormone receptor signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
myeloid leukocyte migrationPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of focal adhesion disassemblyPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of endoplasmic reticulum unfolded protein responsePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
positive regulation of protein localization to plasma membranePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin receptor signaling pathwayPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
proteolysisProteasome subunit beta type-5Homo sapiens (human)
response to oxidative stressProteasome subunit beta type-5Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProteasome subunit beta type-5Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
hemopoiesisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
leukocyte homeostasisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
myeloid progenitor cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
pro-B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of cell population proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
response to organonitrogen compoundReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine-mediated signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
animal organ regenerationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
common myeloid progenitor cell proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
regulation of apoptotic processReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAP kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAPK cascadeReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
lymphocyte proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein autophosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to cytokine stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to glucocorticoid stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
dendritic cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
multicellular organism developmentReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
liver developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of protein phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vasculature developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
glucose metabolic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phagocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
epidermal growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of lamellipodium assemblyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle inactivityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of macroautophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
actin cytoskeleton organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
platelet activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of actin filament depolymerizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell costimulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of TOR signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to insulin stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle stretchPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of multicellular organism growthPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to L-leucinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of cellular respirationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of neuron apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
relaxation of cardiac musclePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
adipose tissue developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to glucose stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to hydrostatic pressurePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to dexamethasonePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle cell contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
energy homeostasisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of actin filament organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
autosome genomic imprintingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to butyratePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of protein localization to membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of fibroblast apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 4Homo sapiens (human)
regulation of cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein polyubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel remodelingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of heart rateE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrioventricular valve morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocardial cushion morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ventricular septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrial septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
traversing start control point of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of cell population proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to xenobiotic stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to toxic substanceE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to iron ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of protein processingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of neuron projection developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein ubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein sumoylationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein destabilizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to magnesium ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein localization to nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to cocaineE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
establishment of protein localizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to etherE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA-templated transcriptionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to antibioticE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of protein export from nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to steroid hormoneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of muscle cell differentiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteolysis involved in protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein autoubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cardiac septum morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complex assemblyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hydrogen peroxideE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to vitamin B1E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to alkaloidE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to growth factor stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to peptide hormone stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to estrogen stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hypoxiaE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to gamma radiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to UV-CE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
fibroblast activationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to actinomycin DE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to formaldehydeE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
amyloid fibril formationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to water-immersion restraint stressE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ovarian follicle developmentApoptosis regulator BAX Homo sapiens (human)
neuron migrationApoptosis regulator BAX Homo sapiens (human)
T cell homeostatic proliferationApoptosis regulator BAX Homo sapiens (human)
B cell homeostasisApoptosis regulator BAX Homo sapiens (human)
B cell apoptotic processApoptosis regulator BAX Homo sapiens (human)
kidney developmentApoptosis regulator BAX Homo sapiens (human)
release of cytochrome c from mitochondriaApoptosis regulator BAX Homo sapiens (human)
blood vessel remodelingApoptosis regulator BAX Homo sapiens (human)
myeloid cell homeostasisApoptosis regulator BAX Homo sapiens (human)
B cell negative selectionApoptosis regulator BAX Homo sapiens (human)
B cell homeostatic proliferationApoptosis regulator BAX Homo sapiens (human)
positive regulation of B cell apoptotic processApoptosis regulator BAX Homo sapiens (human)
glycosphingolipid metabolic processApoptosis regulator BAX Homo sapiens (human)
regulation of nitrogen utilizationApoptosis regulator BAX Homo sapiens (human)
apoptotic processApoptosis regulator BAX Homo sapiens (human)
germ cell developmentApoptosis regulator BAX Homo sapiens (human)
mitochondrial fusionApoptosis regulator BAX Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsApoptosis regulator BAX Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageApoptosis regulator BAX Homo sapiens (human)
apoptotic mitochondrial changesApoptosis regulator BAX Homo sapiens (human)
fertilizationApoptosis regulator BAX Homo sapiens (human)
response to toxic substanceApoptosis regulator BAX Homo sapiens (human)
response to salt stressApoptosis regulator BAX Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientApoptosis regulator BAX Homo sapiens (human)
response to gamma radiationApoptosis regulator BAX Homo sapiens (human)
positive regulation of calcium ion transport into cytosolApoptosis regulator BAX Homo sapiens (human)
negative regulation of mitochondrial membrane potentialApoptosis regulator BAX Homo sapiens (human)
hypothalamus developmentApoptosis regulator BAX Homo sapiens (human)
cerebral cortex developmentApoptosis regulator BAX Homo sapiens (human)
positive regulation of protein-containing complex assemblyApoptosis regulator BAX Homo sapiens (human)
negative regulation of protein bindingApoptosis regulator BAX Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisApoptosis regulator BAX Homo sapiens (human)
negative regulation of endoplasmic reticulum calcium ion concentrationApoptosis regulator BAX Homo sapiens (human)
release of matrix enzymes from mitochondriaApoptosis regulator BAX Homo sapiens (human)
negative regulation of peptidyl-serine phosphorylationApoptosis regulator BAX Homo sapiens (human)
regulation of mammary gland epithelial cell proliferationApoptosis regulator BAX Homo sapiens (human)
cellular response to unfolded proteinApoptosis regulator BAX Homo sapiens (human)
cellular response to UVApoptosis regulator BAX Homo sapiens (human)
ectopic germ cell programmed cell deathApoptosis regulator BAX Homo sapiens (human)
odontogenesis of dentin-containing toothApoptosis regulator BAX Homo sapiens (human)
regulation of apoptotic processApoptosis regulator BAX Homo sapiens (human)
positive regulation of apoptotic processApoptosis regulator BAX Homo sapiens (human)
negative regulation of neuron apoptotic processApoptosis regulator BAX Homo sapiens (human)
positive regulation of neuron apoptotic processApoptosis regulator BAX Homo sapiens (human)
mitochondrial fragmentation involved in apoptotic processApoptosis regulator BAX Homo sapiens (human)
development of secondary sexual characteristicsApoptosis regulator BAX Homo sapiens (human)
retinal cell programmed cell deathApoptosis regulator BAX Homo sapiens (human)
positive regulation of developmental pigmentationApoptosis regulator BAX Homo sapiens (human)
negative regulation of fibroblast proliferationApoptosis regulator BAX Homo sapiens (human)
spermatid differentiationApoptosis regulator BAX Homo sapiens (human)
post-embryonic camera-type eye morphogenesisApoptosis regulator BAX Homo sapiens (human)
response to axon injuryApoptosis regulator BAX Homo sapiens (human)
homeostasis of number of cells within a tissueApoptosis regulator BAX Homo sapiens (human)
protein insertion into mitochondrial membraneApoptosis regulator BAX Homo sapiens (human)
release of sequestered calcium ion into cytosolApoptosis regulator BAX Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolApoptosis regulator BAX Homo sapiens (human)
regulation of cell cycleApoptosis regulator BAX Homo sapiens (human)
regulation of mitochondrial membrane potentialApoptosis regulator BAX Homo sapiens (human)
Sertoli cell proliferationApoptosis regulator BAX Homo sapiens (human)
retina development in camera-type eyeApoptosis regulator BAX Homo sapiens (human)
apoptotic process involved in mammary gland involutionApoptosis regulator BAX Homo sapiens (human)
positive regulation of apoptotic process involved in mammary gland involutionApoptosis regulator BAX Homo sapiens (human)
vagina developmentApoptosis regulator BAX Homo sapiens (human)
calcium ion transport into cytosolApoptosis regulator BAX Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressApoptosis regulator BAX Homo sapiens (human)
thymocyte apoptotic processApoptosis regulator BAX Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorApoptosis regulator BAX Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaApoptosis regulator BAX Homo sapiens (human)
motor neuron apoptotic processApoptosis regulator BAX Homo sapiens (human)
apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
extrinsic apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
intrinsic apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
execution phase of apoptosisApoptosis regulator BAX Homo sapiens (human)
supramolecular fiber organizationApoptosis regulator BAX Homo sapiens (human)
cellular response to virusApoptosis regulator BAX Homo sapiens (human)
positive regulation of endoplasmic reticulum unfolded protein responseApoptosis regulator BAX Homo sapiens (human)
positive regulation of mitochondrial membrane permeability involved in apoptotic processApoptosis regulator BAX Homo sapiens (human)
apoptotic process involved in blood vessel morphogenesisApoptosis regulator BAX Homo sapiens (human)
apoptotic process involved in embryonic digit morphogenesisApoptosis regulator BAX Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in programmed necrotic cell deathApoptosis regulator BAX Homo sapiens (human)
positive regulation of apoptotic DNA fragmentationApoptosis regulator BAX Homo sapiens (human)
positive regulation of IRE1-mediated unfolded protein responseApoptosis regulator BAX Homo sapiens (human)
epithelial cell apoptotic processApoptosis regulator BAX Homo sapiens (human)
positive regulation of epithelial cell apoptotic processApoptosis regulator BAX Homo sapiens (human)
B cell receptor apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
positive regulation of reproductive processApoptosis regulator BAX Homo sapiens (human)
positive regulation of motor neuron apoptotic processApoptosis regulator BAX Homo sapiens (human)
negative regulation of apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayApoptosis regulator BAX Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator BAX Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process by cytochrome cApoptosis regulator BAX Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
peptide hormone processingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particle remodelingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
lipid oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma lipoprotein particle oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidylcholine catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor metabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of inflammatory responsePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of monocyte chemotaxisPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo sapiens (human)
positive regulation of extracellular matrix constituent secretionCarboxypeptidase B2Homo sapiens (human)
blood coagulationCarboxypeptidase B2Homo sapiens (human)
response to xenobiotic stimulusCarboxypeptidase B2Homo sapiens (human)
negative regulation of plasminogen activationCarboxypeptidase B2Homo sapiens (human)
protein catabolic processCarboxypeptidase B2Homo sapiens (human)
negative regulation of fibrinolysisCarboxypeptidase B2Homo sapiens (human)
cellular response to glucose stimulusCarboxypeptidase B2Homo sapiens (human)
liver regenerationCarboxypeptidase B2Homo sapiens (human)
negative regulation of hepatocyte proliferationCarboxypeptidase B2Homo sapiens (human)
proteolysisCarboxypeptidase B2Homo sapiens (human)
fibrinolysisCarboxypeptidase B2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to starvationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of DNA replicationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
synaptonemal complex assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
spermatid developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
long-term memoryHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
fertilizationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of protein modification processHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
organ growthHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
phenotypic switchingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to ethanolHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
behavioral response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
oocyte developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
neuron fate specificationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to fungicideHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to xenobiotic stimulusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of autophagosome assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
protein deacetylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein deacetylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrion organizationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
regulation of ketone biosynthetic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
response to nutrient levelsNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein demalonylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
peptidyl-lysine demalonylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein desuccinylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
peptidyl-lysine desuccinylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein deglutarylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
epigenetic regulation of gene expressionNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
negative regulation of DNA-templated transcriptionREST corepressor 3Homo sapiens (human)
regulation of transcription by RNA polymerase IIREST corepressor 3Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 2Homo sapiens (human)
lactationNuclear receptor corepressor 2Homo sapiens (human)
response to organonitrogen compoundNuclear receptor corepressor 2Homo sapiens (human)
regulation of cellular ketone metabolic processNuclear receptor corepressor 2Homo sapiens (human)
cerebellum developmentNuclear receptor corepressor 2Homo sapiens (human)
response to estradiolNuclear receptor corepressor 2Homo sapiens (human)
estrous cycleNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (334)

Processvia Protein(s)Taxonomy
metal ion bindingLysine-specific demethylase 4EHomo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activityLysine-specific demethylase 4EHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific demethylase 4EHomo sapiens (human)
histone deacetylase activityHistone deacetylase 1Mus musculus (house mouse)
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
telomeric DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
p53 bindingLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
oxidoreductase activityLysine-specific histone demethylase 1AHomo sapiens (human)
enzyme bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear receptor coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K4 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
identical protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
MRF bindingLysine-specific histone demethylase 1AHomo sapiens (human)
flavin adenine dinucleotide bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear androgen receptor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
telomeric repeat-containing RNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
promoter-specific chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
protein kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
signaling receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
heme bindingTyrosine-protein kinase JAK2Homo sapiens (human)
type 1 angiotensin receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
acetylcholine receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone H3Y41 kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone bindingTyrosine-protein kinase JAK2Homo sapiens (human)
identical protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
insulin receptor substrate bindingTyrosine-protein kinase JAK2Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK2Homo sapiens (human)
peptide hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
transcription cis-regulatory region bindingNuclear receptor corepressor 1Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 1Homo sapiens (human)
protein bindingNuclear receptor corepressor 1Homo sapiens (human)
nuclear receptor bindingNuclear receptor corepressor 1Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingNuclear receptor corepressor 1Homo sapiens (human)
nuclear thyroid hormone receptor bindingNuclear receptor corepressor 1Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
supercoiled DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
magnesium ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
four-way junction DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
bubble DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
phosphotyrosine residue bindingTyrosine-protein kinase ABL1Homo sapiens (human)
DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
transcription coactivator activityTyrosine-protein kinase ABL1Homo sapiens (human)
actin monomer bindingTyrosine-protein kinase ABL1Homo sapiens (human)
nicotinate-nucleotide adenylyltransferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase C bindingTyrosine-protein kinase ABL1Homo sapiens (human)
protein bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ATP bindingTyrosine-protein kinase ABL1Homo sapiens (human)
kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
SH3 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
syntaxin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
manganese ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
mitogen-activated protein kinase bindingTyrosine-protein kinase ABL1Homo sapiens (human)
proline-rich region bindingTyrosine-protein kinase ABL1Homo sapiens (human)
delta-catenin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
sequence-specific double-stranded DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
hydroxymethylglutaryl-CoA reductase (NADPH) activity3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
protein binding3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
GTPase regulator activity3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
NADPH binding3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
coenzyme A binding3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
serine-type endopeptidase inhibitor activityAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
heparin bindingAmyloid-beta precursor proteinHomo sapiens (human)
enzyme bindingAmyloid-beta precursor proteinHomo sapiens (human)
identical protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
transition metal ion bindingAmyloid-beta precursor proteinHomo sapiens (human)
receptor ligand activityAmyloid-beta precursor proteinHomo sapiens (human)
PTB domain bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein serine/threonine kinase bindingAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor activator activityAmyloid-beta precursor proteinHomo sapiens (human)
UTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
CTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
mRNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-alphaHomo sapiens (human)
sulfonylurea receptor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein phosphatase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-alphaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
dATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-alphaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
transmembrane transporter bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTPase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
Rho GDP-dissociation inhibitor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
scaffold protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-alphaHomo sapiens (human)
protein tyrosine kinase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
RNA bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
epoxide hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene-A4 hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
protein bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
peptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
zinc ion bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
tripeptide aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
metalloaminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C8Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
hepoxilin-epoxide hydrolase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
DNA bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
RNA bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA (cytosine-5-)-methyltransferase activityDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
protein bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
zinc ion bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
methyl-CpG bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA-methyltransferase activityDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
promoter-specific chromatin bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
phosphotyrosine residue bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
transmembrane receptor protein tyrosine kinase adaptor activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin receptor bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin-like growth factor receptor bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
neurotrophin TRKA receptor bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
protein bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
kinase activator activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
protein phosphatase bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase regulator activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase regulatory subunit bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
ErbB-3 class receptor bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
protein heterodimerization activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol kinase activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
enzyme-substrate adaptor activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase activator activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
1-phosphatidylinositol-3-kinase regulator activityPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
threonine-type endopeptidase activityProteasome subunit beta type-5Homo sapiens (human)
protein bindingProteasome subunit beta type-5Homo sapiens (human)
peptidase activityProteasome subunit beta type-5Homo sapiens (human)
endopeptidase activityProteasome subunit beta type-5Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
ATP bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
nuclear glucocorticoid receptor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein-containing complex bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
phosphatidylinositol 3-kinase activator activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
growth factor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
protein serine/threonine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein kinase activator activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
p53 bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
5S rRNA bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
zinc ion bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
SUMO transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
enzyme bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
receptor serine/threonine kinase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
peroxisome proliferator activated receptor bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ribonucleoprotein complex bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
NEDD8 ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
disordered domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein bindingApoptosis regulator BAX Homo sapiens (human)
lipid bindingApoptosis regulator BAX Homo sapiens (human)
channel activityApoptosis regulator BAX Homo sapiens (human)
Hsp70 protein bindingApoptosis regulator BAX Homo sapiens (human)
identical protein bindingApoptosis regulator BAX Homo sapiens (human)
protein homodimerization activityApoptosis regulator BAX Homo sapiens (human)
protein heterodimerization activityApoptosis regulator BAX Homo sapiens (human)
BH3 domain bindingApoptosis regulator BAX Homo sapiens (human)
BH domain bindingApoptosis regulator BAX Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
1-alkyl-2-acetylglycerophosphocholine esterase activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipid bindingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
hydrolase activity, acting on ester bondsPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
calcium-independent phospholipase A2 activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo sapiens (human)
zinc ion bindingCarboxypeptidase B2Homo sapiens (human)
metallocarboxypeptidase activityCarboxypeptidase B2Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
enzyme bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
C2H2 zinc finger domain bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K56 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9me2 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
promoter-specific chromatin bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
zinc ion bindingNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-malonyllysine demalonylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-succinyllysine desuccinylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-glutaryllysine deglutarylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD+ bindingNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein bindingREST corepressor 3Homo sapiens (human)
transcription corepressor activityREST corepressor 3Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA bindingNuclear receptor corepressor 2Homo sapiens (human)
chromatin bindingNuclear receptor corepressor 2Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 2Homo sapiens (human)
Notch bindingNuclear receptor corepressor 2Homo sapiens (human)
protein bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (175)

Processvia Protein(s)Taxonomy
nucleusLysine-specific demethylase 4EHomo sapiens (human)
nucleoplasmLysine-specific demethylase 4EHomo sapiens (human)
chromatinLysine-specific demethylase 4EHomo sapiens (human)
nucleusLysine-specific demethylase 4EHomo sapiens (human)
nucleoplasmHistone deacetylase 1Mus musculus (house mouse)
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
chromatinLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
chromosome, telomeric regionLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
nucleoplasmLysine-specific histone demethylase 1AHomo sapiens (human)
transcription regulator complexLysine-specific histone demethylase 1AHomo sapiens (human)
protein-containing complexLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair complexLysine-specific histone demethylase 1AHomo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
nucleoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK2Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
caveolaTyrosine-protein kinase JAK2Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
endosome lumenTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
membrane raftTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-23 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
postsynapseTyrosine-protein kinase JAK2Homo sapiens (human)
glutamatergic synapseTyrosine-protein kinase JAK2Homo sapiens (human)
euchromatinTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
nucleusNuclear receptor corepressor 1Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 1Homo sapiens (human)
cytosolNuclear receptor corepressor 1Homo sapiens (human)
membraneNuclear receptor corepressor 1Homo sapiens (human)
mitotic spindleNuclear receptor corepressor 1Homo sapiens (human)
histone deacetylase complexNuclear receptor corepressor 1Homo sapiens (human)
chromatinNuclear receptor corepressor 1Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 1Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
ruffleTyrosine-protein kinase ABL1Homo sapiens (human)
nucleusTyrosine-protein kinase ABL1Homo sapiens (human)
nucleoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
nucleolusTyrosine-protein kinase ABL1Homo sapiens (human)
cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrionTyrosine-protein kinase ABL1Homo sapiens (human)
cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeletonTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear bodyTyrosine-protein kinase ABL1Homo sapiens (human)
dendriteTyrosine-protein kinase ABL1Homo sapiens (human)
growth coneTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear membraneTyrosine-protein kinase ABL1Homo sapiens (human)
neuronal cell bodyTyrosine-protein kinase ABL1Homo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
postsynapseTyrosine-protein kinase ABL1Homo sapiens (human)
protein-containing complexTyrosine-protein kinase ABL1Homo sapiens (human)
plasma membraneTyrosine-protein kinase ABL1Homo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
peroxisomal membrane3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
endoplasmic reticulum3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
endoplasmic reticulum membrane3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
endoplasmic reticulum membrane3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
peroxisomal membrane3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
dendriteAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionAmyloid-beta precursor proteinHomo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
nuclear envelope lumenAmyloid-beta precursor proteinHomo sapiens (human)
cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
mitochondrial inner membraneAmyloid-beta precursor proteinHomo sapiens (human)
endosomeAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum lumenAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
Golgi lumenAmyloid-beta precursor proteinHomo sapiens (human)
Golgi-associated vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cytosolAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
clathrin-coated pitAmyloid-beta precursor proteinHomo sapiens (human)
cell-cell junctionAmyloid-beta precursor proteinHomo sapiens (human)
synaptic vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
membraneAmyloid-beta precursor proteinHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleAmyloid-beta precursor proteinHomo sapiens (human)
axonAmyloid-beta precursor proteinHomo sapiens (human)
growth coneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule lumenAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
endosome lumenAmyloid-beta precursor proteinHomo sapiens (human)
trans-Golgi network membraneAmyloid-beta precursor proteinHomo sapiens (human)
ciliary rootletAmyloid-beta precursor proteinHomo sapiens (human)
dendritic spineAmyloid-beta precursor proteinHomo sapiens (human)
dendritic shaftAmyloid-beta precursor proteinHomo sapiens (human)
perikaryonAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
apical part of cellAmyloid-beta precursor proteinHomo sapiens (human)
synapseAmyloid-beta precursor proteinHomo sapiens (human)
perinuclear region of cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
presynaptic active zoneAmyloid-beta precursor proteinHomo sapiens (human)
spindle midzoneAmyloid-beta precursor proteinHomo sapiens (human)
recycling endosomeAmyloid-beta precursor proteinHomo sapiens (human)
extracellular exosomeAmyloid-beta precursor proteinHomo sapiens (human)
receptor complexAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-alphaHomo sapiens (human)
membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
basolateral plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
apical plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
brush border membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
lysosomal lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
collagen-containing extracellular matrixHeat shock protein HSP 90-alphaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
endocytic vesicle lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm mitochondrial sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
myelin sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular regionLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleoplasmLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
extracellular exosomeLeukotriene A-4 hydrolaseHomo sapiens (human)
tertiary granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
ficolin-1-rich granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleusLeukotriene A-4 hydrolaseHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
lipid dropletPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytoplasmic side of plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytoplasmPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
sarcolemmaPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
sarcolemmaPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
female germ cell nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleoplasmDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
replication forkDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
pericentric heterochromatinDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
nucleusPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cytoplasmPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cis-Golgi networkPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cytosolPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
plasma membranePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
cell-cell junctionPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
membranePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
perinuclear endoplasmic reticulum membranePhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)
nucleusProteasome subunit beta type-5Homo sapiens (human)
cytoplasmProteasome subunit beta type-5Homo sapiens (human)
proteasome complexProteasome subunit beta type-5Homo sapiens (human)
nucleusProteasome subunit beta type-5Homo sapiens (human)
nucleoplasmProteasome subunit beta type-5Homo sapiens (human)
centrosomeProteasome subunit beta type-5Homo sapiens (human)
cytosolProteasome subunit beta type-5Homo sapiens (human)
extracellular exosomeProteasome subunit beta type-5Homo sapiens (human)
proteasome core complexProteasome subunit beta type-5Homo sapiens (human)
proteasome core complex, beta-subunit complexProteasome subunit beta type-5Homo sapiens (human)
cytosolProteasome subunit beta type-5Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endoplasmic reticulum lumenReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endosome membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
receptor complexReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
intercalated discPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
lamellipodiumPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
perinuclear region of cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IBPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
nuclear bodyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleolusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytosolE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
plasma membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
transcription repressor complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocytic vesicle membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cell peripheryApoptosis regulator BAX Homo sapiens (human)
nucleusApoptosis regulator BAX Homo sapiens (human)
nuclear envelopeApoptosis regulator BAX Homo sapiens (human)
cytoplasmApoptosis regulator BAX Homo sapiens (human)
mitochondrionApoptosis regulator BAX Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator BAX Homo sapiens (human)
endoplasmic reticulumApoptosis regulator BAX Homo sapiens (human)
endoplasmic reticulum membraneApoptosis regulator BAX Homo sapiens (human)
cytosolApoptosis regulator BAX Homo sapiens (human)
membraneApoptosis regulator BAX Homo sapiens (human)
extracellular exosomeApoptosis regulator BAX Homo sapiens (human)
mitochondrial permeability transition pore complexApoptosis regulator BAX Homo sapiens (human)
pore complexApoptosis regulator BAX Homo sapiens (human)
Bcl-2 family protein complexApoptosis regulator BAX Homo sapiens (human)
BAX complexApoptosis regulator BAX Homo sapiens (human)
BAK complexApoptosis regulator BAX Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator BAX Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
extracellular regionPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
high-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Rattus norvegicus (Norway rat)
nucleoplasmHistone deacetylase 3Rattus norvegicus (Norway rat)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo sapiens (human)
extracellular regionCarboxypeptidase B2Homo sapiens (human)
extracellular exosomeCarboxypeptidase B2Homo sapiens (human)
extracellular spaceCarboxypeptidase B2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nuclear speckHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrionNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial intermembrane spaceNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial matrixNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
cytosolNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial matrixNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
nucleoplasmREST corepressor 3Homo sapiens (human)
cytosolREST corepressor 3Homo sapiens (human)
histone deacetylase complexREST corepressor 3Homo sapiens (human)
transcription regulator complexREST corepressor 3Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo sapiens (human)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
nucleusNuclear receptor corepressor 2Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 2Homo sapiens (human)
membraneNuclear receptor corepressor 2Homo sapiens (human)
nuclear matrixNuclear receptor corepressor 2Homo sapiens (human)
nuclear bodyNuclear receptor corepressor 2Homo sapiens (human)
chromatinNuclear receptor corepressor 2Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 2Homo sapiens (human)
cytosolHistone deacetylase 6Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5938)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2005Journal of molecular biology, Nov-18, Volume: 354, Issue:1
Crystal structure of a bacterial class 2 histone deacetylase homologue.
AID1811Experimentally measured binding affinity data derived from PDB2005Journal of molecular biology, Nov-18, Volume: 354, Issue:1
Crystal structure of a bacterial class 2 histone deacetylase homologue.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1401372Inhibition of HDAC1 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1702152Metabolic stability in human liver pooled microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID652754Inhibition of recombinant human HDAC10 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID723461Inhibition of human HDAC8 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1482122Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1478598Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1622905Inhibition of recombinant human His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1819530Antitumor activity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as reduction on tumor size at 60 mg/kg, IG administered for 12 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1225984Inhibition of recombinant C-terminal His-tagged full length human HDAC2 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1312847Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1630606Inhibition of recombinant N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID723431Potentiation of 2.5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1200977Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as induction of p21 gene expression at 10 uM after 15 hrs by luciferase reporter gene assay relative to HDAC1 inhibitor SNDX-2752015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1861334Inhibition of HDAC in human DOHH-2 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1164174Cell cycle arrest in human K562 cells assessed as block at G1 phase at 40 uM after 24 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1832683Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1664987Cytotoxicity against human 2C4 cells assessed as reduction in cell viability at 2000 nM incubated for 20 hrs2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
AID760375Cytotoxicity against human BxPC3 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1548728Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr fo2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1164182Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate at 5 uM after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1861253Antiproliferative activity against human ES2 cells assessed as reduction in cell viability measured after 7 days2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID476646Antiproliferative activity against human K562 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1859930Inhibition of HDAC in human U-937 cells assessed as increase in acetylation level of H3K9-14ac at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID732144Inhibition of HDAC5 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1753840Inhibition of HDAC8 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1915584Inhibition of HDAC1 (unknown origin) at 0.1 microM relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID462789Inhibition of HDAC8 expressed in Escherichia coli assessed as Boc-Lys (acetyl)-AMC substrate hydrolysis by fluorimetric assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
AID1861311Induction of apoptosis in human OCILY3 cells measured by flow cytometry analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1449334Inhibition of HDAC1 in human CAL27 cells assessed as accumulation of histone 3 acetylation at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1514611Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells at 2.5 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 1.8 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1671980Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID1128544Inhibition of human HDAC-1 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID749703Inhibition of HDAC6 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1141816Oral bioavailability in ICR mouse at 10 mg/kg by LC-MS/MS analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID723421Potentiation of 25 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1849168Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1816188Inhibition of recombinant HDAC8 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis
AID1231812Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1614192Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.17%)
AID1469378Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID297488Cytotoxicity against human HCT116 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1578905Induction of apoptosis in human Bel7402 cells assessed as increase in cleaved PARP level at 5 uM after 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1639366Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1486302Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1578524Oral bioavailability in Balb/c nude mouse at 50 mg/kg measured upto 24 hrs by LC/MS/MS analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1441706Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in number of neutrophils in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1170742Inhibition of human recombinant HDAC3 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1321731Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1548287Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID1622907Inhibition of HDAC in human HeLa nuclear extract using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1730868Cytotoxicity against human FHC cells assessed as reduction of cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID748110Inhibition of HDAC5 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1855269Antitumor activity against mouse MC38 cells xenografted in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, ip administered every 2 days for 16 consecutive days2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1469383Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.3%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1605980Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1876341Inhibition of recombinant full length human HDAC3 expressed in insect Sf9 cells by EMSA analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID586611Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1547245Inhibition of GST-tagged BRD4 bromodomain (unknown origin) using biotinylated histone H4KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1441704Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in hyperemia of pulmonary alveolar septa at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by hematoxylin and eos2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1129789Induction of apoptosis in human Jurkat cells assessed as early apoptotic cells at 10 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based FACS flow cytometric analysis (Rvb = 0.32%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1466400Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 100 mg/kg/day administered via oral gavage for 16 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1441636Inhibition of recombinant human N-terminal His-tagged 15-LOX-1 expressed in Escherichia coli using arachidonic acid as substrate measured every 2 min intervals for 20 mins by fluorescence analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1436791Growth inhibition of human NCI-H292 cells in LDL depleted FBS containing medium after 72 hrs using compound after sonication in presence of LDL by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity.
AID1547262Inhibition of human recombinant His-tagged BRD2 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1887683Cytotoxicity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID544091Antimalarial activity against drug-resistant Plasmodium falciparum W22008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1206737Cytotoxicity against human HEL cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1478586Induction of apoptosis in human K562 cells assessed as necrotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.035%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID374818Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1063056Inhibition of recombinant HDAC1 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1141763Cytotoxicity against human H460 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1655804Cytotoxicity against human RH4 cells assessed as reduction in cell viability at 0.25 uM incubated for 72 hrs by CellTiter-Glo Luminescent cell viability assay relative to control2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1762489Inhibition of N-terminal GST-tagged and C-terminal His-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated f2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1550094Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1899586Inhibition of HDAC class 2b in human HT-29 cells using Boc-Lys-Ac as substrate incubated for 3 hrs by microplate reader assay
AID748111Inhibition of HDAC4 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID760378Cytotoxicity against human HUT78 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1449317Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1282233Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC62016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID247931Concentration required to inhibit human PC-3 prostate carcinoma cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.
AID463865Inhibition of human HDAC in human HeLa cell nuclear extract after 15 mins by colorimetric assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.
AID1865305Antitumor immunity against mouse 4T1 cells xenografted in BALB/c syngeneic mouse model assessed as fold increase in proportion of CD8+ T cells in spleen at 40 mg/kg, po qd for 12 days by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1739585Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated tubulin/GAPDH at 10 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1365025Selectivity ratio of IC50 for recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 for recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1174700Induction of apoptosis in human U937 cells assessed as late apoptotic cells at 1.5 uM after 24 hrs by annexin-V/propidium iodide staining-based flow cytometry (Rvb = 2.77%)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1762497Inhibition of HDAC3 (unknown origin)2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1707465Synergistic antifungal activity against Candida albicans 0304103 incubated for 48 hrs in presence of fluconazole by microdilution assay2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID1348917Inhibition of C-terminal His-tagged/N-terminal GST-tagged full length recombinant human HDAC3/NcoR2 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins 2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1826592Synergistic antiproliferative effect on HEL cells assessed as combination index at 0.0046 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID623021Inhibition of human HDAC8 expressed in Escherichia coli using Boc-Lys (acetyl)-AMC as substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group.
AID1055717Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1273878Inhibition of human CYP2D6 using 3-[2-(N,N-diethyl-N-methylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate at 10 uM after 30 mins by fluorimetric analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1754767Downregulation of HDAC11 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1201642Inhibition of HDAC (unknown origin) using Fluor de Lys substrate after 2 hrs by microplate reader2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1239052Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID156319Inhibitory activity against PC-3 cell line2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
QSAR studies of PC-3 cell line inhibition activity of TSA and SAHA-like hydroxamic acids.
AID476653Toxicity in FVB mouse assessed as effect on mean platelet volume at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test (Rvb = 8.4 +/- 0.5 microm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID461258Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID717659Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 3.125 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1511152Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1550151Antitumor activity against HEL cells xenografted in BALB/c nu mouse assessed as reduction in tumor volume at 60 mg/kg/day, ip administered for 16 days and measured every 3 days during compound dosing co-treated with 70 mg/kg/day, ip ruxolitinib by caliper2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1355710Antifungal activity against FLC resistant Candida albicans 100 after 48 hrs in presence of fluconazol by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1415639Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1742177Inhibition of recombinant human His-tagged HDAC1 expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID723146Potentiation of 40 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1177045Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1548250Inhibition of HDAC8 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1742653Cytotoxicity against human SUM159PT cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID408888Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1177042Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1563940Inhibition of recombinant HDAC1 (unknown origin) measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
AID1737142Induction of cell cycle arrest in human HCT116 cells assessed as cell accumulation at S phase at 3 uM after 24 hrs by Rnase/PI staining based flow cytometric analysis (Rvb = 25.2%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID618023Antitumor activity against mouse H22 cells xenografted in Kunming mouse assessed as reduction of pulmonary metastatic nodes in lungs at 90 mg/kg, po qd for 14 days2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1403154Inhibition of HDAC6 (unknown origin)2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1633989Inhibition of HDAC1 in human HuH7 cells assessed as increase in histone H3 K9/K14 acetylation at varying concentrations incubated for 24 hrs by Western blot analysis2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID1203895Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1848630Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID414731Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1269327Cytotoxicity against human MCF7 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID382342Inhibition of human HDAC in HeLa cells by flour de lys assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
AID663390Growth inhibition of human RXF393 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID80353Concentration required to inhibit the partially purified HDAC enzyme by 50% obtained from H1299 cell lysate2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID729522Inhibition of HDAC1/HDAC3/HDAC5/HDAC8 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate incubated for 5 mins prior to substrate measured after 30 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN).
AID1390015Selectivity ratio of IC50 for full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1808554Inhibition of recombinant human N-terminal FLAG tagged HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1597931Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1702059Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1739596Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 1 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID480069Cytotoxicity against human HCT116 cells after 71 hrs by MTS assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
AID1433304Induction of apoptosis in p53 null human U937 cells assessed as decrease in XIAP expression level by measuring ratio of XIAP to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID711159Inhibition of HDAC1 by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID1415641Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1127327Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1203893Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1404297Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1487005Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1605976Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1469325Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.4%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID274035Microsome stability: percent compound remaining2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1260652Cytotoxicity against human MV411 cells
AID420640Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 24 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1547263Inhibition of HDAC11 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1578477Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1274873Inhibition of HDAC3 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1275636Inhibition of recombinant human HDAC3 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1861264Selectivity index, ratio of IC50 for inhibition of HDAC3 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1293556Antiproliferative activity against human IGROV1 cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1690835Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus expression system using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured aft2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID274033Inhibition of MDA-MB-231 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID670972Inhibition of human recombinant His6-tagged and GST-fuses HDAC6 expressed in insect High5 cells using Boc-Lys(eacetyl)- AMC as substrate after 3 hrs by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
CCLab--a multi-objective genetic algorithm based combinatorial library design software and an application for histone deacetylase inhibitor design.
AID1888417Inhibition of fungal filamentation in azole-resistant Candida albicans 0304103 assessed as reduction in yeast-hypha transition at 64 ug/ml in presence of fluconazole by inverted microscopic analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID1848558Inhibition of HDAC in human NCI-H522 cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1469323Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.97%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID456795Inhibition of HDAC in human HeLa cell nuclear extracts after 15 mins by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID297487Cytotoxicity against human HCT15 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID717791Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 1.25 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID243474Percentage inhibition against histone deacetylase of HeLa cells at 100 uM2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.
AID1548301Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 46%)
AID308049Inhibition of human HDAC 12007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.
AID438220Selectivity ratio of IC50 for HDAC6 to IC50 for HDAC1/2 from human HeLa cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
AID659643Inhibition of HDAC in human DU145 cells assessed as histone H3 hyperacetylation at 2.5 to 5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID744378Inhibition of HDAC1/3/5/8 in human HeLa cell extract using Boc-Lys-(acetyl)-AMC as substrate incubated for 5 mins prior to substrate addition measured after 30 mins by fluorometric analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN).
AID723434Potentiation of 2.5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1170741Inhibition of human recombinant HDAC2 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID737907Selectivity index, ratio of IC50 for human HS68 cells to IC50 for human A549 cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1164189Inhibition of HDAC in human U937 cells assessed as hyperacetylation of histone H4 at Lys 16 residue at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1348918Inhibition of C-terminal His-tagged recombinant human HDAC8 (1 to 377 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluores2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID541646Inhibition of human HDAC3 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1182315Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
A potent HDAC inhibitor, 1-alaninechlamydocin, from a Tolypocladium sp. induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
AID616000Antiproliferative activity against human A549 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1547270Inhibition of HDAC1 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1821268Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID90342In vitro inhibitory activity against histone deacetylase (HDAC) isolated from HeLa nuclear extract2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.
AID1698864Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID1907400Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Dual-acting antitumor agents targeting the A
AID408884Inhibition of HDAC102008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1550326Synergistic antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs in presence of ruxolitinib by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID613293Plasma concentration in human at 800 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1633995Therapeutic index, ratio of CC50 for human HuH7 cells to EC50 for antiviral activity against HCV infected in human HuH7-luc/neo cells assessed as inhibition of DNA replication i2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID1321738Inhibition of PDE5A in human SH-SY5Y cells assessed as increase in CREB phosphorylation at Ser133 residue at 500 nM after 30 mins by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1246509Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1873387Inhibition of HDAC7 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1234889Inhibition of HDAC3 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID527044Cytotoxicity against human NCI-H23 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID723448Potentiation of 0.5 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.25 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1550327Synergistic antiproliferative activity against human K562 cells assessed as combination index after 48 hrs in presence of ruxolitinib by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1873419Inhibition of HDAC3 (unknown origin) at 5 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1677508Inhibition of class 1 HDAC in human HeLa cells assessed as increase in acetylation of H3 substrate at 0.3 to 3 uM after 6 to 12 hrs by Western blot analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1572343Selectivity ratio of IC50 for recombinant C-terminal His/FLAG-tagged human HDAC1 to IC50 for N-terminal GST-tagged human HDAC62019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID591327Inhibition of HDAC in human HeLa cells at 1 uM by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.
AID1406984Inhibition of HDAC6 in human NB4 cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1667068Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate class 2A preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1886187Inhibition of HDAC8 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID288446Inhibition of HDAC in HeLa cells by fluorescent activity assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID420326Inhibition of HDAC from human HeLa cells by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1487040Inhibition of HDAC in human HeLa-S3 cells lysates assessed as remaining enzyme activity at 1 x 10'-7 M pre-incubated for 15 mins before HDAC-Glo I/II substrate addition and measured after 30 mins post substrate addition2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID446347Oral bioavailability in CD1 mouse at 15 mg/kg2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID527038Cytotoxicity against human A549 cells by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1873389Inhibition of HDAC9 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1875510Selectivity index, ratio of IC50 for cytotoxicity against HMEC cells to GI50 for antiproliferative activity against human MDA-MB-231 cells2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID1203892Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID481559Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1821346Toxicity in mouse xenografted with human HepG2 cells assessed as necrosis in spleen at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1348912Inhibition of class 1 HDAC in human HeLa nuclear extracts using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1486999Inhibition of HDAC1 (unknown origin) by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID496805Inhibition of human HDAC52010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1917530Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID1441663Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 mRNA level at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID659494Inhibition of HDAC6 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1890313Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1783069Antifungal activity against fluconazole-sensitive Candida albicans 10061 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID81711Concentration required to inhibit the HCT116 cell growth by 50%.2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1676599Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1655898Inhibition of HDAC6 in human RH4 cells assessed as acetylated alpha-tubulin level at 0.15 uM incubated for 96 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1061950Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID322418Cell cycle arrest in human LNCap cells assessed as accumulation at S phase relative to control at 1 uM2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID1280270Inhibition of class1 HDAC in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID348805Antiproliferative activity against human A549 cells after 72 hrs by celltiter-blue viability assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID352523Antiproliferative activity against human MIAPaCa2 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1896934Cytotoxicity against human L02 cells assessed as reduction in cell viability by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID489913Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
AID1753836Selectivity index, ratio of IC50 for inhibition of recombinant human HDAC1 to IC50 for inhibition of recombinant human HDAC62021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1433271Inhibition of HDAC6 in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID353357Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G2/M phase at 3 uM after 16 hrs by flow cytometry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
AID463864Inhibition of human HDAC in human HeLa cell nuclear extract at 50 nM after 15 mins by colorimetric assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.
AID297499Cytotoxicity against human CCRF-CEM cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1312883Antitumor activity against human HCT116 cells xenografted in Balb/c nude mouse assessed as change in tumor mass at 50 mg/kg, ip administered every 2 days for 8 days measured every 2 days of compound dosing relative to control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1466064Inhibition of recombinant human full length HDAC8 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1816225Induction of apoptosis in mouse 4T1 cells assessed as rly apoptotic cells at 5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.12%)
AID526537Growth inhibition of human NCI-H23 cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1361627Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID297478Cytotoxicity against human NCI H69 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1234897Antiproliferative activity against human H7402 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1418667Inhibition of recombinant human HDAC3 using fluorogenic HDAC substrate after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID1863424Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1658889Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-pNA as substrate preincubated for 20 mins followed by substrate addition and further incubated for 90 mins by fluorescence assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.
AID1690836Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by 2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1127003Induction of apoptosis in human U937 cells assessed as necrotic cells using annexin-V/propidium iodide staining at 0.25 uM after 24 hrs by flow cytometry analysis (Rvb = 0.06%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1754752Inhibition of C-terminal 6XHis-tagged human recombinant full length HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1622964Inhibition of HDAC10 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID524988Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in CFTR protein level at 1 uM for 8 days by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID734734Cytotoxicity against human LNCAP cells assessed as growth inhibition by MTS assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1541565Inhibition of class 1 HDAC in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.5 uM preincubated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay (Rvb = 63.2 2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID760494Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1164029Inhibition of human recombinant HDAC5 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1623525Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate-3 by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1848582Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1126964Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC3 (unknown origin)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1469333Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1622965Inhibition of HDAC6 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1816205Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 2.5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 85.7%)
AID628446Induction of apoptosis in human HepG2 cells assessed as hyperacetylation of p53 after 24 hrs by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1578884Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1848619Cytotoxicity against human COLO 205 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID619048Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1702091Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID461259Antiproliferative activity against human Capan1 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1361647Induction of apoptosis in human A549 cells assessed as viable cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1401483Selectivity ratio of IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell to IC50 for HDAC3 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1449684Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID1550085Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1653142Cytotoxicity against human MGC803 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1164923Induction of cell differentiation in human BE(2)-C cells assessed as increase in acetylated tubulin at 2 to 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1900937Toxicity in mouse bearing intracranial tumor assessed as median survival time at 25 mg/kg, ip in presence of clorgyline for 10 days (Rvb=13.8 days)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID1476157Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1742720Induction of apoptosis in mouse 4T1 cells assessed as early apoptotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 1.65 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1689777Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1855259Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1266818Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1659650Inhibition of HDAC6 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID616005Inhibition of HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1702048Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1165114Cytotoxicity against human LNCAP cells2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1410011Reactivation of latent HIV1 infected in human U1 cells assessed as increase in p24 production after 48 hrs by ELISA2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
AID1598137Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as maximum LTR activity at 5 uM incubated for 48 hr by FACSCalibur flow cytometry relative to control2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID1702066Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1422517Inhibition of HDAC in MEF assessed as increase in histone H4K8 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1515840Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1865252Synergistic antiproliferative activity against human MV4-11 cells assessed as combination index measured in presence of SHP099 by Chou-Talalay method2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID90687Inhibitory concentration against maize Histone deacetylase 22003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1885693Antitumor activity at human A549 cells xenografted in BALB/c mouse assessed as reduction in tumor growth at 12 umol/kg, iv administered for 20 days and measured every 3 days for 21 days in presence of CDDO-Me2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy.
AID1421612Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1060991Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors.
AID1401902Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID723151Potentiation of 8 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1855260Antiproliferative activity against human MOLT-4 cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1730850Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1759728Inhibition of class 1 HDAC in quiescent human primary T-cell model of VSV-G pseudotyped HIV-1 latency assessed as reactivation of HIV latency incubated for 24 hrs in presence of 10% FBS by NanoGlo luciferase assay2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
AID1848279Inhibition of HDAC6 (unknown origin) at 100 nM2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID274027Clearance after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1127001Induction of apoptosis in human U937 cells assessed as late apoptotic cells using annexin-V/propidium iodide staining at 0.5 uM after 24 hrs by flow cytometry analysis (Rvb = 2.13%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1246517Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1566817Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1861329Inhibition of HDAC in human OCILY3 cells assessed as effect on total Stat3 levels at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID775833Inhibition of human recombinant MMP-12 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2.AcOH as substrate at 10 uM preincubated for 30 mins prior to substrate addition measured for 30 mins by fluorescence assay relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1639368Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1426429Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID1855255Antiproliferative activity against human HeLa cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID274062Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1702084Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1821339Toxicity in mouse xenografted with human HepG2 cells assessed as cellular inflammation in lung at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID328807Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1401537Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID723139Potentiation of 3.16 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID352762Toxicity against human HCT116 cells xenografted nude mouse assessed as body weight loss at 150 mg/kg, ip administered once daily for 18 days2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID420515Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at G2/M phase at IC90 using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1810050Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay
AID1206744Cytotoxicity against human KG1 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1541444Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 92019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1639369Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID609490Antiproliferative activity against human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID615998Inhibition of HDAC from human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1752944Inhibition of N-terminal GST-tagged full length human recombinant HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay
AID303348Inhibition of HDAC1 in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID723474Cytotoxicity against cisplatin resistant human KYSE-510 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1266813Antiproliferative activity against human SW480 cells assessed as cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1915595Inhibition of HDAC8 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID331957Increase in histone H3 acetylation in human HEK-TE cells at 5 uM after 6 hrs by Western blot analysis2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.
AID546548Inhibition of human recombinant HDAC6 expressed in HEK293 cells2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID594124Inhibition of full length HDAC2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Discovery of histone deacetylase 8 selective inhibitors.
AID1462230Inhibition of BRD4 (unknown origin)2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1659234Inhibition of human HDAC1 after 30 mins by microplate reader analysis2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
AID274076Inhibition of PC3 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID591331Antiproliferative activity against human HCT116 cells after 5 days by Alamar blue assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.
AID1482102Inhibition of HDAC 5 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1233265Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID1260643Inhibition of human recombinant HDAC7 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID392406Inhibition of HDAC1 in human 293T cells after 16 hrs by fluorimetry2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Sulfamides as novel histone deacetylase inhibitors.
AID1401341Inhibition of HDAC in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1401370Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 5 x 10'-8 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1246510Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1326521Inhibition of full length recombinant human HDAC6 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1431821Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1915596Inhibition of HDAC4 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1622906Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1250649Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1061954Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1127330Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1898917Inhibition of HDAC1/2 in human NCI-H460 cells at 7.4 uM assessed as increase in H4 acetylation measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1127320Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 72 hrs2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1141785Inhibition of HDAC6 in human HCT116 cells assessed as increase in HSP90 acetylation at 0.3 to 1 uM by coimmunoprecipitation analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID765378Inhibition of recombinant human HDAC4 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1177051Antiprotozoan activity against Trypanosoma cruzi Tulahuen C4 amastigotes2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1861663Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated histone H3 at 2000 nM measured after 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1623526Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1482128Cytotoxicity against human FR2 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1482133Induction of mitochondrial membrane potential loss in human HL60 cells at 1 uM measured after 48 hrs by Rh123 dye-based flow cytometric analysis (Rvb = 5.6%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1855262Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 1.5 uM incubated for 48 hrs by PI and annexin V-FITC staining based flow cytometry (Rvb = 3.4%)2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1129007Inhibition of human HDAC-5 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1548267Induction of cell cycle arrest in human KM3 cells assessed as reduction in cell cycle progression in S phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry
AID1816226Induction of apoptosis in mouse 4T1 cells assessed as late apoptotic cells at 5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.99%)
AID628437Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1478599Inhibition of Class 1 histone deacetylase in human K562 cells using Boc-Lys (acetyl)-AMC as substrate preincubated with compound for 3 hrs followed by substrate addition measured after 3 hrs by fluorometric analysis2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID274020Clearance after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1165116Cytotoxicity against human Jurkat gamma1 cells2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID316879Inhibition of human CEM cells assessed as viability2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1462222Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID593556Inhibition of human HDAC11 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1348920Inhibition of full length recombinant human HDAC5 preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1689778Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1129780Cell cycle arrest in human Jurkat cells assessed as accumulation at G0/G1-phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 2.39%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1816222Induction of apoptosis in mouse 4T1 cells assessed as late apoptotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.99%)
AID1600659Inhibition of recombinant human full length C-terminal Flag/His-tagged HDAC1 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID1848564Cytotoxicity against human WI-38 cells assessed as reduction in cell survival incubated for 30 mins by methylene blue staining based analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID344920Inhibition of HDAC12008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID1200971Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID420514Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at G2/M phase at IC80 using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID541652Inhibition of human HDAC6 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1246508Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1452274Inhibition of HDAC6 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID420643Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 48 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1336950Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at greater G2 phase at 2.5 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 0.20%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1349716Inhibition of recombinant human full length C-terminal flag-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1742744Genotoxicity in Salmonella typhimurium TA1537 by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1742186Inhibition of recombinant human N-terminal His-tagged HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1572358Induction of apoptosis in human T24 cells at 1 to 10 uM after 48 hrs by propidium iodide-staining based FACS analysis2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1667099Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G2 phase at 5 uM incubated for 48 hrs RNase/PI staining based flow cytometry assay (Rvb = 17.4 %)2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID525029Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in forskolin and genistein-stimulated Fdelta508 CFTR channel activity at 10 uM after 24 hrs relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID288455Inhibition of tumor growth in MDA-MB-231 cells xenografted BALA/c nude mouse at 30 mg/kg, ip2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID1162484Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate by fluorescence assay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
AID420505Antiproliferative activity against human IGROV1 cells after 72 hrs2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1384235Effective permeability of the compound at 50 uM after 18 hrs by UV spectroscopy based PAMPA2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1280281Selectivity index, ratio of HDAC6 inhibition in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 10 uM over class1 HDAC inhibition in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 10 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1349715Inhibition of human recombinant HDAC3/GST-tagged NCOR1 DAD (397 to 503 residues) expressed in baculovirus expression system after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID273167Inhibition of maize HD1A2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1128560Inhibition of human HDAC-7 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1541449Cytotoxicity against human A2780 cells assessed as reduction in cell survival measured after 72 hrs by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1816236Antitumor activity in human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 100 mg/kg, po administered daily for 14 days measured twice per week
AID273177Induction of granulocytic differentiation of U937 cells measured as CD11c expression level after 48 hrs at 5 uM2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1816171Inhibition of JAK/STAT pathway in human MDA-MB-231 cells at 3 to 10 uM incubated for 12 hrs in presence of INCB by chemiluminescence based Western blotting analysis
AID1274879Inhibition of HDAC9 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1275632Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1742722Induction of apoptosis in mouse 4T1 cells assessed as necrotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 5.00 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1873410Inhibition of HDAC3 (unknown origin) preincubated for 30 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1235256Inhibition of HDAC1/2 in human HeLa cell nuclear extracts preincubated for 5 mins followed by substrate addition measured after 0.5 hrs by Color de Lys assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
AID1486998Inhibition of HDAC in human HeLa-S3 cells lysates pre-incubated for 15 mins before HDAC-Glo I/II substrate addition and measured after 30 mins post substrate addition2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1548256Inhibition of class 1 HDAC n human HeLa cell nuclear extracts pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1653099Antiproliferative activity against human HeLa cells by CCK8 assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1885673Synergistic antiproliferative activity against human L02 cells at 2.5 to 12.5 uM measured after 72 hrs in presence of CDDO-Me by MTT assay2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy.
AID723159Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1548726Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1769652Inhibition of ALK L1196M mutant (unknown origin)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1441677Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction neutrophil count at 25 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1821276Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID297493Cytotoxicity against human Hec-1-A cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1826642Induction of apoptosis in HEL cells assessed as apoptotic cells at 0.5 uM incubated for 48 hrs by annexin V-FITC/PI staining based flow cytometry (Rvb = 4.23%)2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID221993Compound was tested for anti-proliferative activity in human bone marrow cells2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1511150Antiproliferative activity against human HL60 cells incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1677520Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1177050Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1281847Inhibition of full length His6-tagged GST-fused recombinant human HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1901767Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID593553Inhibition of human HDAC8 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1690106Inhibition of HDAC in human HeLa cell nuclear extract using fluorescence substrate incubated for 30 mins by fluorescence based assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID1478589Induction of apoptosis in human K562 cells assessed as viable cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 92.4%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1864254Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1898936Induction of DNA damage in human MM473 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1441696Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as reduction in hydroxyproline level at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 14 relative to control2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1164179Cell cycle arrest in human U937 cells assessed as block at G2-M phase at 5 uM after 24 to 96 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1651330Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID461269Antiproliferative activity against human CAL27 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID732444Inhibition of human MDA-MB-231 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID748100Inhibition of HDAC1 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1178594Inhibition of rat liver HDAC at 0.1 uM pre-incubated for 15 mins before Boc-Lys(Ac)-AMC substrate addition and measured after 30 mins by fluorometry2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1390024Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1720112Inhibition of EGFR (unknown origin)2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID465159Growth inhibition of human SU-8686 cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID723449Potentiation of 1 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1348923Inhibition of N-terminal GST-tagged human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1622978Inhibition of HDAC8 (unknown origin) expressed in Escherichia coli using BML-KI-178 as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1587859Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1566040Inhibition of recombinant human HDAC6 using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID1164797Half life in human hepatocytes at 5 uM by LCMS/MS analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1174690Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1234890Inhibition of HDAC6 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1441666Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 level pretreated at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID481572Cytotoxicity against mouse S180 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID586609Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1201644Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1206738Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1439780Inhibition of human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by trypsin-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa.
AID1312848Inhibition of full length recombinant human His-tagged p110 alpha/p85 alpha expressed in baculovirus expression system incubated for 1 hr by kinase-glo assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1390812Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
AID1421928Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1547266Inhibition of HDAC8 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1234901Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID737914Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1775546Inhibition of HDAC2 (unknown origin)2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1337261Antiproliferative activity against human MDA-MB-231 cells up to 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID308050Antiproliferative activity against mouse SC9 cells by MTS assay2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.
AID1566818Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1739588Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated H3/GAPDH at 10 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1848611Cytotoxicity against human SF-539 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1742760In vivo inhibition of HDAC in tumor of mouse 4T1 cells xenografted in BALB/c mouse assessed as increase in acetylated alpha-tubulin expression by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1753644Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylated histone H3 levels at 1 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1129006Inhibition of human HDAC-4 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID663403Half life in artificial gastric fluid2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1398823Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CDC6 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID717656Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 2.5 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1235258Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
AID1751995Inhibition of HDAC6 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1753843Selectivity index, ratio of IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1141786Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1164042Antiproliferative activity against human MOLT4 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1614138Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
AID461267Antiproliferative activity against human SCC15 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1754757Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID616001Antiproliferative activity against human Hep3B cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1655788Inhibition of human recombinant HDAC2 using AMC-K(Ac)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID499808Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1275644Growth inhibition of human A549 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1401532Antiproliferative activity against human A431 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1482115Cytotoxicity against human THP1 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1848622Cytotoxicity against human HCT-15 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID780573Growth inhibition of human HeLa cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
AID445124Inhibition of human recombinant HDAC1 expressed in baculovirus assessed as residual activity at 5 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID1864225Inhibition of full length recombinant N-terminal GST-tagged human HDAC8 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID420324Inhibition of HDAC1 by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1363798Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID1478594Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1808549Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID723129Potentiation of 50 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1349730Antitumor activity against human HCT116 cells xenografted in BALB/C nude mouse assessed as tumor growth inhibition at 25 mg/kg, ip bid administered for 21 consecutive days measured every 3 days2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1227025Retention time of the compound in HEPES buffer treated with SAHA-TAP at pH 7.4 by LC-MS analysis in presence of GSH2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID347873Growth inhibition of human Melanoma cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1193536Inhibition of isolated rat liver HDAC using substrate containing acetylated lysine side chain assessed as release of fluorophore at 0.01 uM by Fluor de Lys assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans.
AID1890331Stability in human plasma incubated for 6 hrs in presence of NADPH and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1421918Gametocytocidal activity against synchronized Plasmodium falciparum NF54 mature stage 5 gametocytes after 48 hrs by ATP bioluminescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID286790Inhibition of HDAC32007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID1497925Induction of CRBN ubiquitin ligase-mediated HDAC2 degradation in human MCF7 cells assessed as decrease in HDAC2 levels at 10 uM after 12 hrs by immunoblotting analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Development of the first small molecule histone deacetylase 6 (HDAC6) degraders.
AID1541446Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID105415Antiproliferative activity against MDA-435 (human breast carcinoma) cell line.2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
AID1758461Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1671982Cell cycle arrest in human HCT-116 cells assessed as accumulation at G2/M phase measured after 24 hrs2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID1861258Inhibition of HDAC2 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1652193Inhibition of human recombinant HDAC8 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1769643Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID366640Inhibition of HDAC1 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1545987Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1614191Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 5.03%)
AID1861251Inhibition of HDAC derived from human HeLa cell nucleus2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1896935Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID1235257Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
AID1493591Inhibition of human recombinant full-length HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID1901055Inhibition of HDAC2 (unknown origin) using trypsin and Ac-peptide as substrates2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID603544Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC in human HeLa cell nuclear extracts2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1655787Inhibition of human recombinant HDAC1 using AMC-K(Ac)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID593554Inhibition of human HDAC9 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1312849Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1326511Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1589336Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.
AID1659651Inhibition of HDAC7 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID1886183Inhibition of HDAC1 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1599724Cytotoxicity against human Meso163 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1266823Inhibition of HDAC in human HCT116 cells assessed as increase in acetyl-histone H3 expression at 5 uM after 48 hrs by immunoblotting analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1321701Inhibition of HDAC2 (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1598099Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as maximum LTR activity at 2.5 uM incubated for 48 hr using Chroma-Glo substrate by luciferase dual re2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID297498Cytotoxicity against human EOL1cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID760372Inhibition of HDAC in human jurkat cells assessed as increase in H4K12 acetylation after 12 hrs by FACS analysis relative to control2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID723436Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID90693Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID352516Inhibition of human recombinant HDAC12009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1126987Inhibition of HDAC2 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1263066Selectivity ratio of IC50 for human A549 cells to IC50 for African green monkey Vero cells2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.
AID1614233Induction of apoptosis in human MM1S cells assessed as viable cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 98.9%)
AID1898896Resistance index, ratio of IC50 for human NCI-H460 cells to IC50 for H460-R9A cells2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1578497Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 0.25 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 19.46 to 22.17 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID737916Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID760498Cytotoxicity against human U251 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID269669Antiproliferative activity against human PC3 cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1614197Induction of apoptosis in human MV4-11 cells assessed as viable cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 84.1%)
AID1128558Inhibition of human HDAC-5 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID308651Increase in p27kip1 gene expression in PANC1 cells after 24 hrs relative to control2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1597932Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID723466Inhibition of human HDAC1 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1659655Antiproliferative activity against human PC3 cells incubated for 24 hrs by CCK8 assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID329919Induction of apoptosis in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID753164Cytotoxicity against human A549 cells2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID1898898Antiproliferative activity against multi-drug resistant human A2780-DX cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1282292Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as death at 50 mg/kg, ip q2d for 9 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1816196Inhibition of HDAC in human BT-549 cells assessed as increase in level of acetyl-H3K9/14 substrate at 3 uM incubated for 12 hrs by chemiluminescence based Western blotting analysis
AID1859929Inhibition of HDAC in human U-937 cells assessed as increase in acetylation level of HSP90 at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1547332Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in OSM mRNA level at 10 uM after 24 hrs by RT-PCR analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1566039Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed b2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID1702055Inhibition of HDAC1 in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate measured after 2 hrs by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1234910Toxicity in human H7402 cells xenografted mouse assessed as change in toxic effect at 100 mg/kg/day, po for 16 days2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1566803Inhibition of recombinant full length human HDAC2 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1614196Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.17%)
AID1379287Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mi2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
AID524996Inhibition of HDAC8 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1702237Oral bioavailability in Balb/c mouse at 50 mg/kg measured up to 24 hrs by LC/MS/MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1848632Cytotoxicity against human TK-10 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1605972Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1449335Inhibition of HDAC1 in human Cal27CisR cells assessed as accumulation of histone 3 acetylation at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1832671Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1175813Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay2014Journal of natural products, Dec-26, Volume: 77, Issue:12
Reniochalistatins A-E, cyclic peptides from the marine sponge Reniochalina stalagmitis.
AID1349719Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID675298Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 1 uM by fluorescence assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
AID1177052Antiprotozoan activity against Leishmania donovani MHOM- ET-67/L82 amastigotes2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1415638Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID420641Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 48 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID628209Antiproliferative activity against human SH-SY5Y cells after 24 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID461255Antiproliferative activity against human H460 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID723423Potentiation of 5 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1173506Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1851613Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1263147Antiproliferative activity against human MDA-MB-231 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1709354Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human NAMALVA cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1764248Inhibition of HDAC in human CAL-27 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 18 hrs followed by susbtrate addition and measured after 3 hrs by fluorescence microplate reader assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1303691Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1765329Selectivity index, ratio of IC50 for human recombinant full length HDAC1 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1541554Inhibition of class 1 HDAC in human CAL27 cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID755615Cytotoxicity against SAHA-resistant human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1162487Growth inhibition of human HL60 cells after 72 hrs by CellTiter Glo assay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
AID1282260Cytotoxicity against human A549 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1361643Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1449683Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID84276Inhibitory concentration against HT1080 cells proliferation2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID374831Antiproliferative activity against human U937 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1065629Inhibition of human recombinant full length HDAC1 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1821314Antitumor activity against human HepG2 cells xenografted in mouse assessed as TGI at 12 mg/kg, ip administered every 2 days for 4 weeks2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID775829Inhibition of mushroom tyrosinase assessed as L-DOPA conversion to melanin at 10 uM preincubated for 10 mins prior to substrate addition measured after 10 mins by spectrophotometric analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1339579Inhibition of HDAC1/HDAC2/HDAC3 in human U937 cells assessed as increase in histone H3 acetylation at 2 uM after 18 hrs by Western blot method2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID1421613Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID618011Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1293557Antiproliferative activity against human H460 cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID748098Inhibition of HDAC3 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID310125Growth inhibition of human NB4 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.
AID1055714Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID628452Inhibition of HDAC in human HepG2 cells assessed as increase in histone H4 acetylation at 1 to 10 uM after 6 hrs by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1355709Antifungal activity against FLC resistant Candida albicans 100 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID760388Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1422518Inhibition of HDAC in MEF assessed as increase in histone H4 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID366645Inhibition of HDAC10 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1785331Inhibition of HDAC in human HeLa nuclear extract at 1000 nM using Boc-Lys(acetyl)-AMC as substrate measured after 1 hr by fluorescence microplate reader assay relative to control
AID1861307Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at G2/M phase in presence of pictilisib measured by flow cytometry analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID343689Inhibition of nuclear HDAC isolated from human HeLa cells2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
AID1410329Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1730852Antiproliferation activity against human SK-BR-3 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1246527Resistance index, ratio of IC50 for imatinib resistant human IR-K562 cells to IC50 for human K562 cells2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1783107Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLy-s(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence microtiter plate reader assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.
AID527207Induction of autophagy in human A549 cells assessed as increase in LC3II after 3 hrs relative to control2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1578150Cytotoxicity against human SC9 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID462792Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
AID1709350Cytotoxicity against human HS5 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID476828Toxicity in FVB mouse assessed as effect on number of RBC at 50 mg/kg, po administered 5 times per week for 2 weeks (Rvb = 7.7 +/- 0.1 10^6/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1166498Inhibition of human recombinant full length HDAC6 using (Boc-Lys (-acetyl)-AMC substrate after 30 mins2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID760376Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1543944Inhibition of human recombinant HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1727729Inhibition of HDAC1 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1785008Antimigratory activity in human HepG2 cells assessed as reduction in wound closure at 6 uM measured after 48 hrs by scratch wound healing assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1459953Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1709351Selectivity index, ratio of IC50 for human HS5 cells to IC50 for human Jurkat cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1783067Antifungal activity against fluconazole-sensitive Candida albicans 7781 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1487088Growth inhibition of human Jurkat cells assessed as cell viability at 1 uM incubated for 44 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1826625Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 0.04 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1901153Inhibition of HDAC3 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1901155Inhibition of HDAC6 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1127017Antitumor activity against human U937 cells xenografted in BALB/c nu mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 16 days relative to control2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1785329Inhibition of full length human CDK4 (1 to 303 residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system at 100 nM preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay
AID1848575Induction of ferroptosis in human NCI-H522 cells assessed as induction of lipid peroxidase accumulation at 5 uM incubated for 1 day by C11-BODIPY-581/591 staining based flow cytometry analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1863423Cytotoxicity against human HOP-62 cells assessed as cell viability after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1873403Inhibition of HDAC1 (unknown origin) preincubated for 120 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1900942Toxicity in mouse bearing intracranial tumor assessed as median survival time at 50 mg/kg, ip in presence of clorgyline for 10 days (Rvb=13.8 days)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID1754799Downregulation of SIRT6 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1433259Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID316941Inhibition of HDAC92008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1487011Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC8 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1784193Inhibition of recombinant human HDAC6 using ZMAL as substrate incubated for 90 mins by fluorescence based micro plate assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.
AID1812442Inhibition of human recombinant HDAC1 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1861660Inhibition of colony formation in human HCT-116 cells at 2000 nM2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1865265Inhibition of recombinant N-terminal GST-tagged human HDAC5 expressed in HEK293 cells using Ac-LeuGlyLys (TFA)-AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID482939Inhibition of HDAC12010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID632972Cytotoxicity against human MCF7 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1275651Antitumor activity against human HCT116 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 40 mg/kg, ip qd administered for 14 days measured every other day during compound dosing2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1572380Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1398807Inhibition of HDAC3 in human MCF7 cells assessed as increase in acetylated histone H4 expression after 8 hrs by Western blot analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1398822Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYBL2 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID90522Inhibitory concentration against rat liver Histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1063055Inhibition of recombinant HDAC8 (unknown origin) using Fluor-de-Lys-HDAC8 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1677513Binding affinity to full length His-tagged Bcl-xl (unknown origin) preincubated for 30 min followed by 5-FAM Bid-BH3 addition and measured after 20 mins by fluorescence polarization assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1525778Inhibition of HADC2 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1597941Antiproliferative activity against human BGC823 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID723430Potentiation of 0.75 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.25 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1469394Induction of apoptosis in human Hep3B cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 97.9%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1245688Inhibition of Class 1 histone deacetylase in human PC3 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1518827Antimalarial activity against ring stage Plasmodium falciparum 3D7 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID663356Growth inhibition of human NCI-H522 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1900929Toxicity in mouse bearing intracranial tumor assessed as median survival time at 50 mg/kg, ip for 10 days (Rvb= 13.8 days)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID1901148Inhibition of HDAC in human HeLa cell nuclear extracts using color de Lys as substrate measured after 30 mins by colorimetric assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1129005Inhibition of human HDAC-3/NCOR2 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID546545Inhibition of HDAC in human HeLa cell nuclear extracts2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1141804Antitumor activity against human HCT116 cells xenografted in nude athymic mouse assessed as tumor growth inhibition at 200 mg/kg/day, po after 2 to 16 days relative to control2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1239051Cytotoxicity against human RPMI8226 cells assessed as cell viability after 72 hrs by CCK8 assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID1321733Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 100 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1421603Inhibition of HDAC6 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID765213Cytotoxicity against human A2780 cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID476833Toxicity in FVB mouse assessed as effect on hematocrit at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1282251Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1597925Antiproliferative activity against human LoVo cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1303629Potentiation of 0.1 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1576455Cytotoxicity against human MCF10F cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID1855258Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1282252Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1541550Inhibition of HDAC6 in human CAL27 cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1737156Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 1 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.51%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1330926Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1515903Antiproliferative activity against human K562 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1518830Selectivity index, ratio of EC50 for human MDA-MB-231 cells to IC50 for ring stage Plasmodium falciparum K12019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID734732Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1865292Antitumor activity against human MV4-11 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 40 mg/kg, po qd administered for 20 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1897390Induction of cell cycle arrest in human SNU-16 cells assessed as accumulation of cells at G0/G1 phase at 0.03 to 1 uM incubated for 24 hrs by PI staining based flow cytometry analysis
AID1876473Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 5.80 %)2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID710841Inhibition of HDAC by fluorescence assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID1515915Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1897395Induction of apoptosis in human SNU-16 cells assessed as dead cells at 0.03 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 2.65%)
AID1234888Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1355687Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID476829Toxicity in FVB mouse assessed as effect on mean cell volume of red cells at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test (Rvb = 43.7 +/- 0.4 microm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID328826Antitumor activity against human HCT116 cells xenografted BALB/c mouse assessed as tumor growth inhibition at 100 mg/kg, ip administered for 5 days per week for 2.5 weeks2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1398799Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in Sf9 cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID723439Potentiation of 1 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1431819Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID723726Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID246080Effective Concentration of compound to inhibit the growth of human LOX-IMVI cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1688027Induction of apoptosis in human HL-60 cells assessed as increase in accumulation at sub-G1 phase at 0.5 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2.72 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1888591Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay
AID1481747Antiproliferative activity against human RPMI8266 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors.
AID1732192Cytotoxicity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1422521Inhibition of human recombinant HDAC1 at 2 uM after 15 to 30 mins by fluorometric method2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID659495Inhibition of HDAC8 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1246525Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human THP1 cells2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1441657Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in protein concentration in BALF at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1537556Selectivity index, ratio of IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells to IC50 for recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cel2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1451833Inhibition of GST tagged full length human recombinant HDAC8 (H90 to 30H) expressed in Baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluore2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1915523Inhibition of HDAC-1 (unknown origin) expressed in Escherichia coli BL21 (DE3) in HeLa nuclear extract using KI177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by Bradford reagent method2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1164176Cell cycle arrest in human MCF7 cells assessed as block at G1 phase at 5 uM after 24 to 96 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1165104Antileishmanial activity against promastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1215086Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1502989Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1205625Inhibition of HDAC in human HeLa cell nuclear extract using Fluor de Lys as substrate incubated with compound for 30 mins by microtiter-plate reading flourimeter analysis2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1785339Inhibition of HDAC8 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID723161Potentiation of 25 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1702068Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID392398Inhibition of human recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus by fluorimetry2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Sulfamides as novel histone deacetylase inhibitors.
AID1704068Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID420318Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1303621Potentiation of 0.025 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.125 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID723153Potentiation of 1 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1401506Inhibition of HDAC6 in human U937 cells assessed as increase in acetyl-alpha-tubulin levels at 5 uM after 18 hrs by Western blot method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1275592Inhibition of human recombinant HDAC3 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
AID1361642Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1709356Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 24 hrs MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1623537Selectivity index, ratio of IC50 for HDAC10 (unknown origin) to IC50 for human recombinant HDAC62019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1686353Drug metabolism in human liver microsomes assessed as o-glucuronidated metabolite formation in absence of UDP glucuronic acid incubated for 12 hrs at 37 degC by electrospray ionization liquid chromatography mass spectrometry2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
AID1832804Inhibition of human HDAC2 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID1858656Cytotoxicity against human SMMC-7721 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
AID639798Oral bioavailability in mouse2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID1848593Induction of cell cycle arrest in human NCI-H522 cells assessed as accumulation at G1 phase 5 uM incubated for 24 to 72 hrs by PI staining based flow cytometric analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID316905Inhibition of human LOX-IMVI cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1293569Inhibition of human recombinant C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1572352Inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 0.1 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID519584Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1826651Antitumor activity against HEL cells xenografted in BALB/C mouse assessed as T/C value at 10 mg/kg, po qd for 14 days consecutively by caliper method relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1864226Inhibition of full length recombinant N-terminal GST-tagged human HDAC4 (612 to end residues)expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1390009Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1821270Inhibition of HDAC1 (unknown origin) incubated for 30 mins by microplate reader assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID461262Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1293570Inhibition of human HDAC9 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1487000Inhibition of HDAC2 (unknown origin) by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1511131Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1614232Induction of apoptosis in human MM1S cells assessed as necrotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.32%)
AID1614227Induction of apoptosis in human MM1S cells assessed as late apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.42%)
AID1622901Cytotoxicity against human A549 cells after 72 hrs by CellTiter-Glo assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1897399Induction of apoptosis in human SNU-16 cells assessed as dead cells at 0.1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 2.65%)
AID669760Growth inhibition of human A549 cells after 48 hrs by SRB assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID759305Inhibition of human recombinant HDAC1 after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1449680Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID384318Selectivity for IC50 of maize histone deacetylase 1B over IC50 of maize histone deacetylase 1A2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID524995Inhibition of HDAC10 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID663399Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID546564Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1550087Activation of JAK in human MDA-MB-231 cells assessed as upregulation of p-STAT3-Tyr705 level at 5 uM after 12 hrs by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID762186Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.
AID1245680Inhibition of Class 1 histone deacetylase isolated from human HeLa cell nuclear extracts using Boc-Lys (acetyl)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1742686Induction of cell cycle arrest in mouse 4T1 cells assessed as G2/M phase accumulation at 2 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 38.51 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1061948Cytotoxicity against human H460 cells2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1401369Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 1 x 10'-7 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1545980Antiproliferative activity against human LoVo cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID420512Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at S phase at IC80 using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1464872Inhibition of HDAC8 (unknown origin)2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1702088Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID605529Antiproliferative activity against human LoVo cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1454680Decrease in alcohol intake in rat assessed as operant alcohol self-administration at 50 mg/kg, ip administered once in a week relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1578153Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1482130Antitumor activity against mouse P388 cells implanted in CDF1 mouse assessed as increase in median survival time at 50 mg/kg, ip administered for 9 consecutive days2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID723142Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1752936Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) as fluorogenic substrate incubated for 90 mins by fluorescence based assay
AID1753834Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1279129Inhibition of C-terminal His-tagged human recombinant HDAC8 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID1702083Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID226263Fold selectivity for classI HDAC2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID350727Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID286789Inhibition of HDAC22007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID524823Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in mutant Fdelta508 CFTR protein level at 1 uM for 8 days by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1384233Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 30 mins by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1280308Inhibition of human KDAC62016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1469375Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1876476Induction of cell cycle arrest in human HCT-116 cells assessed as increase in accumulation of cells at G2/M phase at 1 uM incubated for 24 hrs by flow cytometry analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1141778Induction of apoptosis in human HCT116 cells assessed as accumulation at sub-G1 phase at 1 uM by propidium iodide staining-based flow cytometric analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1915571Inhibition of HDAC (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID492806Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID723465Inhibition of human HDAC2 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1390026Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1821341Toxicity in mouse xenografted with human HepG2 cells assessed as spleen edema at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1282241Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID461257Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1279124Inhibition of HDAC1/2 in human HeLa cell nuclear extract using color de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 30 min by microtiter plate reader analysis2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID1653097Antiproliferative activity against human MCF7 cells by CCK8 assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1275634Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID71648Inhibitory concentration against friend cells proliferation2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID734731Cytotoxicity against human Jurkat gamma1 cells assessed as growth inhibition after 72 hrs by MTS assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1282287Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as change in body weight at 100 mg/kg, po q2d for 8 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1605978Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1859932Inhibition of HDAC in human HCT-116 cells assessed as increase in acetylation level of HSP90 at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1754815Inhibition of HDAC in human MCF7 cells assessed as increase in acetylated histone H3 mRNA level at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID274100Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 90% of isolates after 48h.2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID1326520Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1887691Cytotoxicity against human WI-38 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1808551Inhibition of recombinant human N-terminal GST-tagged HDAC7 expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1246518Cytotoxicity against human K562 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1653138Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by SRB assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1478593Inhibition of HDAC8 (unknown origin) using substrate after 30 mins by fluorometric analysis2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1633670Neurotoxicity against rat CGN cells assessed as cell viability at 50 uM incubated for 24 hrs by MTT assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1200999Cmax in ICR mouse at 50 mg/kg, po2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1469313Induction of apoptosis in human T47D cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 85.3%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1819514Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1550109Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1165109Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1487089Growth inhibition of human Jurkat cells assessed as cell viability at 10 uM incubated for 44 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID489911Inhibition of human HDAC82010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
AID1282239Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID723141Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1380941Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1478596Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1303624Potentiation of 0.5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 2.5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1764803Selectivity index, ratio of IC50 for recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay to IC50 recombinant for human HDAC6 using Ac-GA2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID723457Potentiation of cisplatin-induced toxicity in cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1848586Inhibition of full length C-terminal his-tagged human recombinant HDAC8 expressed in Sf9 insect cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1404296Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1482104Inhibition of HDAC 10 in human HeLa nuclear extract measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID440819Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
AID1193538Antiproliferative activity against human HCT116 cells after 5 days by Alamar Blue assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans.
AID723476Cytotoxicity against cisplatin sensitive human CAL27 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1406985Inhibition of HDAC6 in human NB4 cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1720097Inhibition of BRD4 (unknown origin) at 10 uM relative to control2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID1886250Antitumor activity against mouse H22 cells allografted in ICR mouse assessed as reduction in tumor weight at 25 mg/kg, ip administered qd measured after 21 days2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1548273Induction of cell cycle arrest in human RPMI8226 cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 23.5%)
AID350715Inhibition of HDAC in human HeLa cell nuclear extracts by fluorimetry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1633993Antiviral activity against HCV infected in human HuH7-luc/neo cells assessed as inhibition of DNA replication incubated for 3 days by luciferase reporter gene assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID1865250Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID480068Inhibition of human recombinant HDAC2 preincubated for 24 hrs followed by 1 hr reaction with substrate by protease coupled end-point assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
AID1451823Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1702064Inhibition of HDAC5 (unknown origin) using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1688038Induction of apoptosis in human HL-60 cells assessed as live cells at 2 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 89.29 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID350716Inhibition of human recombinant HDAC1 by fluorimetry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1164917Antiproliferative activity against human NCI-H929 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1164780Inhibition of HDAC1 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID580927Inhibition of HDAC activity in human HeLa cells at 0.1 uM after 24 hrs2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Antiproliferative and differentiating activities of a novel series of histone deacetylase inhibitors.
AID1441630Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID710836Cytotoxicity against human NCI-H23 cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID732878Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID749390Inhibition of human recombinant HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
The discovery of colchicine-SAHA hybrids as a new class of antitumor agents.
AID1200970Inhibition of HDAC6 in human A549 cells assessed as induction of tubulin acetylation after 17 to 18 hrs by ELISA2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1784970Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1764247Inhibition of HDAC in human A2780 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 18 hrs followed by susbtrate addition and measured after 3 hrs by fluorescence microplate reader assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1129783Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M-phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.30%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1622961Inhibition of HDAC2 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1549138Antifungal activity against azole-resistant Candida albicans 7781 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID765393Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1234904Antiproliferative activity against human 3AO cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1174701Induction of apoptosis in human U937 cells assessed as dead cells at 1.5 uM after 24 hrs by annexin-V/propidium iodide staining-based flow cytometry (Rvb = 0.95%)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1543943Inhibition of human recombinant HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1572351Inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 1 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1737656Cytotoxicity against human KG -1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID1785349Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
AID1605973Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1897393Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 0.03 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.02%)
AID1303626Potentiation of 5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 25 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID604139Inhibition of histone acetyltransferase in human U937 cells assessed as increase of pan-acetylated histone H4 level at 5 uM after 24 hrs by Western blotting2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
AID1742680Induction of cell cycle arrest in human MDA-MB-231 cells assessed as G2/M phase accumulation at 2 uM incubated for 24 hrs PI staining based by flow cytometry analysis (Rvb = 27.08 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1398814Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of GREB1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID481550Cytotoxicity against human HO8910 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1548244Inhibition of HDAC1/2 in human HeLa cell nuclear extracts pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1650410Inhibition of recombinant human HDAC62020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID1753842Selectivity index, ratio of IC50 for inhibition of HDAC3 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID663338Growth inhibition of human PC3 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1655792Inhibition of human recombinant HDAC6 using AMC-K(Ac)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1698863Inhibition of c-MET (unknown origin)2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID1888466Inhibition of purified human HDAC1 using Ac-Leu-Gly-(e-Ac)Lys-AMC by fluorometric HDAC assay2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.
AID1511971Inhibition of recombinant: C-terminal His-tagged human HDAC2 (1 to 426 residues)/N-terminal GDT-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluoresc2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
AID1578498Induction of apoptosis in human MV4-11 cells assessed as viable cells at 0.5 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 53.01 to 53.07 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1659647Inhibition of HDAC1 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID90529Inhibitory concentration against histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID717660Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 2.5 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID619138Half life in rat liver microsomes2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID663471Solubility in neutral water2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID481555Cytotoxicity against human KB cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID632975Cytotoxicity against human NCI-H460 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1469384Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.64%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1742761In vivo inhibition of STAT-3 in tumor of mouse 4T1 cells xenografted in BALB/c mouse assessed as decrease in STAT-3 phosphorylation by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1848304Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 1 uM incubated for 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.51%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID274016Percent inhibition of CYP450 2C9 at 1 uM concentration2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID348798Inhibition of HDAC32008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID440822Inhibition of human recombinant N-terminal FLAG-tagged HDAC5 (620-1122) expressed in baculovirus after 10 mins by fluorimetric analysis2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
AID1201645Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1518807Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in Ac-Tubulin level at 2.5 to 5 uM incubated for 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1655801Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent cell viability assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1764292Inhibition of HDAC in human CAL-27 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.7 uM pretreated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay (Rvb = 3.57 uM)2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1901160Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1422512Inhibition of HDAC in mouse FL5.12 cells assessed as increase in histone H3 acetylation at 5 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1205626Induction of RUNX transcriptional activation in mouse C2C12-6xOSE2 cells at 1 uM after 24 hrs by luciferase reporter assay relative to FGF-22015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1162217Cell cycle arrest in human HL60 cells assessed as accumulation at sub-G1 phase at 1 uM by propidium iodide staining-based flow cytometry (Rvb = 2.1%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID1676592Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1396991Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
AID1589335Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate at 50 uM by fluorescence assay relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.
AID1861345Inhibition of HDAC in human OCILY3 cells assessed as effect on pS6 levels at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID352760Antitumor activity against human HCT116 cells xenografted nude mouse assessed as tumor growth inhibition at 150 mg/kg, ip administered once daily for 18 days relative to control2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1901159Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID723453Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1349720Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1888585Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
AID310185Growth inhibition of human ACHN cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID723127Potentiation of 45 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID308649Increase in p21WAF1/CIP1 gene expression in PANC1 cells at 0.1 uM after 48 hrs relative to control2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1383986Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID605299Antiproliferative activity against human HCT116 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1355690Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1380942Antiproliferative activity against human AGS cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID669761Inhibition of human recombinant HDAC1 after 30 mins by fluorometric assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1129778Cell cycle arrest in human Jurkat cells assessed as accumulation at S-phase at 10 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 19.5%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID328800Inhibition of HDAC7 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1825921Inhibition of recombinant human full length C-terminal His tagged HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs
AID1784973Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1848321Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at S phase at 1 uM incubated for 48 hrs by AnnexinV/PI staining based flow cytometry (Rvb = 45.5%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID723132Potentiation of 50 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1476147Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID723156Potentiation of 1 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.25 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID609492Thermodynamic solubility of the compound at pH 6.82011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1321726Lipophilicity, log D of the compound at pH 7.42016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1783066Antifungal activity against fluconazole-sensitive Candida albicans 0304103 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1739597Antiproliferative activity against human HL60 assessed as reduction in cell growth at 1 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1901763Inhibition of full length human recombinant HDAC8 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1401387Inhibition of HDAC3 in human HeLa-S3 cell lysates assessed as remaining activity at 1 uM preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID481558Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1742649Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID273168Inhibition of maize HD1B2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1861260Inhibition of HDAC4 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1864241Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated H3 level at 1.25 to 5 uM by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1312851Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID723422Potentiation of 25 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1164187Inhibition of human recombinant HDAC6 using Z-MAL as substrate after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID775843Inhibition of HDAC2 (unknown origin)-mediated deacetylation preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1754742Induction of apoptosis in human MCF7 cells assessed as downregulation of c-Myc gene expression at 1 uM measured after 24 hrs whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1464885Terminal half life in Sprague-Dawley rat 2 mg/kg, iv administered via bolus by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID723148Potentiation of 40 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1493601Inhibition of HDAC6 in human A549 cells assessed as increase in acetylated alpha-tubulin levels at 500 nM after 3 hrs by Western blot analysis2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID1239049Inhibition of recombinant His6-tagged GST-fused human HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID243847Inhibitory activity against human histone deacetylase 4 (HDAC4) at 5 uM2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID441872Inhibition of human recombinant HDAC8 using fluorescent acetylated substrate2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Binding ensemble profiling with photoaffinity labeling (BEProFL) approach: mapping the binding poses of HDAC8 inhibitors.
AID1688030Induction of apoptosis in human HL-60 cells assessed as live cells at 0.5 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 89.29 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1897380Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID708273Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID421215Antitumor activity against human MCF10A cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID525000Inhibition of HDAC4 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1127321Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1633436Induction of neurogenesis in human SH-SY5Y cells assessed as stimulation of neurite outgrowth at 10 uM incubated for 72 hrs by phase contrast microscopic analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID1065945Inhibition of HDAC6 in human LNCAP cells assessed as increase in tubulin acetylation at 2.31 to 20 uM after 4 hrs by Western blotting analysis2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID639775Inhibition of KDM4E2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Lysine demethylases inhibitors.
AID1361654Induction of apoptosis in human A549 cells assessed as necrotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID628438Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC3/NCoR22011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1469376Induction of apoptosis in human A549 cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.7%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID373077Inhibition of human recombinant HDAC42009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1855245Inhibition of HDAC8 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC or Boc-Lys(triflouroacetyl)-AMC as substrate incubated for 30 mins and measured by fluorescence assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID732154Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID652751Inhibition of recombinant human HDAC7 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1915562Inhibition of human HDAC1 incubated for 30 mins by SpectraMax M2 microplate reader analysis2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1688023Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1702154Metabolic stability in rat liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1863169Inhibition of HDAC6 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID1129796Induction of apoptosis in human Jurkat cells assessed as caspase 3/7 activation at 10 uM after 48 hrs by luminescence assay (Rvb = 109,510 +/- 4710.453 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1897402Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 0.3 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.41%)
AID605537Antiproliferative activity against human COR-L23 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID481552Cytotoxicity against human HO8910 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID482959Octanol-water distribution coefficient, log D of the compound2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID723450Potentiation of 1 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1487095Inhibition of HDAC8 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID1418672GPx-like activity of the compound assessed as velocity for cumene hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID689653Inhibition of HDAC8 after 45 mins by microplate fluorometric analysis2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
Design, synthesis and evaluation of novel metalloproteinase inhibitors based on L-tyrosine scaffold.
AID1189851Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID1434351Inhibition of HDAC (unknown origin) expressed in mouse C2C12-6xOSE cells assessed as increase in RUNX3 transcriptional activation at 1 uM measured after 24 hrs by luciferase reporter gene assay relative to FGF22017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID456799Cytotoxicity against african green monkey Vero cells after 1 to 2 days by neutral red assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID473182Induction of HDAC-mediated H3/H4 histone acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1303625Potentiation of 1 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1312929Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of acetylated alpha-tubulin level at 2 uM after 6 hrs by Western blot method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID723458Potentiation of cisplatin-induced toxicity in cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1764284Inhibition of HDAC in human CAL-27 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.7 uM pretreated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay relative to cisplatin alo2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID274028AUC after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1742705Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 3.79 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID623097Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group.
AID1389950Cytotoxic activity against human MCF7 cells after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1487044Inhibition of HDAC1 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1260641Inhibition of human recombinant HDAC5 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1282255Cytotoxicity against human A2780 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1541562Inhibition of class 1 HDAC in human Cal27CisR cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1266837Induction of DNA damage in human HCT116 cells assessed as histone H2AX phosphorylation at S139 at 1 to 5 uM after 12 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID626566Growth inhibition of human HCT116 cells after 5 days by alamar blue assay2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
AID310184Growth inhibition of human HCT15 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1873390Inhibition of HDAC10 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID297489Cytotoxicity against human PC3 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID764215Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1819522Downregulation of SSRP-1 expression in human KG-1 cells assessed as chromatin damage at 0.5 to 2.5 uM measured after 24 hrs by Western blot analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID723452Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1543932Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1821275Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1816710Inhibition of HDAC2 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID274071Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID723144Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1206747Induction of nitric oxide release in human HEL cells at 100 uM after 3 to 5 hrs by Griess assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1873388Inhibition of HDAC8 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1742655Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1895827Inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Dec-15, Volume: 226Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).
AID723454Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1174695Inhibition of HDAC6 (unknown origin)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1614139Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay
AID1658891Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-pNA as substrate preincubated for 20 mins followed by substrate addition and further incubated for 90 mins by fluorescence assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.
AID1063037Inhibition of recombinant HDAC6 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1476121Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHKKAc as substrate in presence of ATP2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1389952Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 16 uM after 24 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1126993Induction of apoptosis in human U937 cells assessed as late apoptotic cells using annexin-V/propidium iodide staining at 1 uM after 12 hrs by flow cytometry analysis (Rvb = 1.83%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1861337Inhibition of HDAC in human OCILY3 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1141771Cytotoxicity against human MKN45 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1396985Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
AID1541563Inhibition of class 1 HDAC in human CAL27 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.5 uM preincubated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay (Rvb = 9.79 uM)2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1730861Antiproliferative activity against human NCI-H820 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1848617Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID605398Inhibition of HDAC6 in human HCT116 cells assessed as induction of alpha-tubulin acetylation after 30 hrs by Western blot analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1543938Antiproliferative activity against human Bel7402/5-FU cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1165115Cytotoxicity against human Jurkat cells2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1739568Antiproliferative activity against human HL60 assessed as reduction in cell growth at 100 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1754814Inhibition of HDAC in human MCF7 cells assessed as increase in acetylated histone H2A mRNA level at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1873406Inhibition of HDAC2 (unknown origin) preincubated for 60 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1759720Inhibition of recombinant human FLAG-tagged HDAC3 expressed in human HEK293F cells co-expressing His6-tagged SMRT (1 to 899 residues) using Fluor-de-lys substrate as substrate incubated for 3 hrs followed by substrate addition and measured after 60 mins b2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
AID461253Antiproliferative activity against human HCC827 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID619049Competitive inhibition of HDAC4 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID723135Potentiation of 10 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1898902Antiproliferative activity against human MM487 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1439351Antiproliferative activity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous Non-Radioactive assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID1690837Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluores2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1784987Inhibition of HDAC3 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID663375Growth inhibition of human SNB19 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1164026Inhibition of human recombinant HDAC3 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1633439Immunomodulatory activity in LPS treated Wistar rat primary microglial cells assessed as effect on TREM2 expression level at 5 to 50 uM incubated for 24 hrs by western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID80076Inhibitory activity against H1299 human lung carcinoma cell growth2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID1336936Inhibition of class 1 HDAC in human LNCAP cells assessed as acetylated histone H4 accumulation at 10 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1542181Inhibition of HDAC3 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID324956Inhibition of HDAC6 in HEK293 cells2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1273866Inhibition of HDAC in human HeLa cells nuclear extract using Fluor de lys as substrate after 15 mins by fluorometric analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1401530Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1605966Antiproliferative activity against human SR cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID725670Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate additio2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
AID1848277Inhibition of PI3Kalpha (unknown origin) by mobility shift assay2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID476836Toxicity in FVB mouse assessed as effect on body weight at 50 mg/kg, po administered 5 times per week for 2 weeks2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1739571Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated tubulin/GAPDH at 10 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1361641Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1865272Inhibition of SHP2 in human MV4-11 cells assessed as downregulation of ERK phosphorylation incubated for 24 hrs by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1462215Inhibition of recombinant human HDAC1 at 0.1 uM after 30 mins by fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1890309Inhibition of HDAC2 (unknown origin) using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1173505Inhibition of full length C-terminal 6x-His tagged human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1547271Inhibition of HDAC7 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1688026Inhibition of recombinant C-terminal FLAG-tagged full length human HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence base2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1826595Inhibition of full-length recombinant human HDAC1 expressed in Baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based microtite2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1348922Inhibition of C-terminal His-tagged recombinant human HDAC9 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1234887Inhibition of HDAC1/2 in human HeLa cell nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1421924Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1873405Inhibition of HDAC2 (unknown origin) preincubated for 30 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1898937Induction of DNA damage in human MM487 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID669757Growth inhibition of human Hep3B cells after 48 hrs by SRB assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1348919Inhibition of N-terminal GST/C-terminal His-tagged recombinant human HDAC4 (648 to 1057 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1826597Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1164025Inhibition of human recombinant HDAC2 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1816235Antitumor activity in human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 100 mg/kg, po administered daily for 14 days presence of ruxolitinib measured twice per week
AID603532Cytotoxicity against human HeLa cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID723140Potentiation of 3.16 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.25 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1361639Inhibition of HDAC in human A549 cells assessed as increase in histone H4 acetylation after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID619052Competitive inhibition of HDAC7 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1882977Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID1832686Inhibition of full length human HDAC2 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1671984Cell cycle arrest in human MCF7/ADR cells assessed as accumulation at G2/M phase measured after 24 hrs2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID1856989Inhibition of HDAC6 (unknown origin) preincubated for 5 mins followed by substrate addition and measured after 30 mins by multimode microplate reader analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID711157Inhibition of HDAC8 by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID446341Inhibition of histone acetylation in human K562 cells at 0.5 uM by flow cytofluorometry relative to control2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID1164193Inhibition of HDAC in human MCF7 cells assessed as hyperacetylation of histone H4 at Lys 16 residue at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1578493Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 2 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 19.46 to 22.17 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1541452Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID545854Inhibition of human HDAC in HeLa cells by fluorescent activity assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1765326Inhibition of human full-length recombinant HDAC3 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1819521Downregulation of SPT16 expression in human KG-1 cells assessed as chromatin damage at 0.5 to 2.5 uM measured after 24 hrs by Western blot analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID723478Cytotoxicity against cisplatin sensitive human MDA-MB-231 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1293558Antiproliferative activity against human LoVo cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1543937Antiproliferative activity against human Bel7402 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1633424Inhibition of GSK3beta in human SH-SY5Y cells assessed as reduction in copper-induced tau hyperphosphorylation at 10 uM preincubated for 1 hr followed by copper addition and measured after 26 hrs by ELISA2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID723441Potentiation of 0.5 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1415647Inhibition of HDAC2 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1260642Inhibition of human recombinant HDAC6 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1633994Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID269672Antiproliferative activity against human ACHN cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1548266Induction of apoptosis in human RPMI8226 cells assessed as induction of caspase-3/7 activation incubated for 24 hrs by fluorometric assay
AID1833062Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID1129773Increase in p21 mRNA level in human Jurkat cells at 10 uM after 24 hrs by quantitative RT-PCR analysis2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1915570Cytotoxicity against human MDA-MB-231 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1279127Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID1897491Toxicity in BALB/c nude mouse xenografted with human HCT-116 cells assessed as reduction in body weight at 30 mg/kg/day, po administered for 18 days and measured every 3 days
AID300839Growth inhibition of human hepatocytes after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID327547Increase in acetylated alpha tubulin level in human HCT116 cells at 10 uM after 24 hrs relative to control2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID1390962Inhibition of HDAC1 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).
AID1380948Antiproliferative activity against human HEL cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID350728Growth inhibition of human DMS114 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1282262Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID476651Toxicity in FVB mouse assessed as effect on number of platelets at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test (Rvb = 454 +/- 93 10^3/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID347869Growth inhibition of human Breast cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1281856Antiproliferative activity against human JeKo1 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID631666Inhibition of human recombinant full-length HDAC1 using fluorophore conjugated substrate by fluorescence assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).
AID723157Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1548914Induction of apoptosis in human RS4:11 cells harboring wild type p53/FLT3 assessed as cleavage of pro-caspase 3 at 5000 nM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1164027Inhibition of human recombinant HDAC8 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID538409Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1250654Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1900913Cytotoxicity against human TMZ-resistant U251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID1633672Inhibition of HDAC in mouse N9 cells assessed as suppression of LPS-induced decrease in histone H3 acetylation at 5 to 25 uM incubated for 24 hrs by Western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1722283Inhibition of human recombinant HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys(eacety1)-AMC as substrate incubated for 3 hrs measured after 30 mins by microplate reader based spectrophotometric analysis2020Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
AID1758464Dark toxicity in human HCT-116 cells assessed as reduction in cell viability incubated under dark for 48 hrs measured after 48 hrs by CCK8 assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1605979Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID482970Toxicity in human PC3 cells xenografted nude mouse2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1201650Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1293568Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1352480Inhibition of HDAC1 in human HeLa cells after 72 hrs by ELISA2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID274024Bioavailability after i.p. dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1201649Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 48 hrs by SRB assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID488237Inhibition of HDAC2 after 10 mins by fluorometric assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1266826Cytotoxicity against rat IEC-18 cells assessed as survival after 48 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1819505Inhibition of HDAC6 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID603538Antitumor activity against human MDA-MB-231 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 90 mg/kg, ip qd for 21 days2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1864220Binding affinity to 5' FAM and 3' TAMRA-labeled c-myc G4-quadruplex DNA Pu22 (unknown origin) assessed as change in melting temperature at 1 uM by fluorescence resonance energy transfer assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1677500Induction of apoptosis in human HeLA cells at 3 uM after 48 hr by annexin V FITC and propidium iodide staining based flow cytometric analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1240554Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 4 uM after 24 hrs using Annexin V-FITC and propidium iodide staining by flow cytometry (Rvb = 4.04%)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID328809Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID723124Potentiation of 8 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.25 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1248352Inhibition of human full length MMP2 using Mca-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate at 10 uM incubated for 2 hrs prior to testing measured for 15 mins by fluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID663359Growth inhibition of human HCT15 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID525015Inhibition of HDAC7 in human CFBE41o- cell line assessed as increase in stability of Fdelta508 CFTR protein at 5 uM after 24 hrs by pulse chase analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1810053Displacement of [3H]SCH58261 from adenosine A2A receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
AID1737141Induction of cell cycle arrest in human HCT116 cells assessed as cell accumulation at G0/G1 phase at 3 uM after 24 hrs by Rnase/PI staining based flow cytometric analysis (Rvb = 48.4%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID255817Inhibitory concentration against Histone deacetylase 1A in maize2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
AID545860Antimalarial activity against sPlasmodium falciparum VS/1 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1441634Inhibition of recombinant human N-terminal His-tagged 5-LOX expressed in Escherichia coli assessed as conversion of arachidonic acid to HpETEs measured for 300 secs by UV-visible spectrophotometric analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1548302Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G2/M phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 9.1%)
AID609508Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
AID748099Inhibition of HDAC2 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1384225Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1861328Inhibition of HDAC in human DOHH-2 cells assessed as effect on total Stat3 levels at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1873385Inhibition of HDAC5 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1777023Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin)2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase.
AID1384219Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells assessed residence time preincubated fopr 2 hrs followed by dilution and subsequent fluorogenic HDAC substrate 3 addition measured at 2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID545861Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCB1 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID456801Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W22010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID1737137Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1454051Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID348391Inhibition of HDAC in human NB4 cells assessed as induction of histone H4 acetylation after 6 hrs by Western blot analysis2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents.
AID1832691Inhibition of human N-terminal GST tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID366644Inhibition of HDAC6 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1848587Inhibition of full length N-terminal GST/C-terminal his-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in Sf9 insect cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID445134Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID1449333Inhibition of HDAC6 in human Cal27CisR cells assessed accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1890315Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1127012Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 0.125 to 1 uM by flow cytometry analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID618331Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 200 mg/kg, po qd for 21 days measured on day 152011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID723119Potentiation of 20 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1771468Inhibition of tubulin polymerization (unknown origin) measured after 1 min by fluorescence assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID482954Solubility at pH 72010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1476120Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells at 10 uM using RHKKAc as substrate in presence of ATP relative to control2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID655471Restoration of CFTR deltaF508 mutant trafficking to cell surface in human CFBE41o cells co-expressing halide-sensitive YFP-H148Q/I142L assessed as fluorescence quenching at 1 uM after 24 hrs relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1875503Inhibition of LSD1 (unknown origin) using H3K4me2 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence based analysis2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID1614129Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1826623Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 0.37 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1898527Acute toxicity in po dosed ICR mouse assessed as maximum tolerated dose measured after 7 days2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer.
AID1449323Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1709366Induction of apoptosis in human NAMALVA cells assessed as early apoptotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 5.07%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID723435Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1537560Antiproliferative activity against human NB-1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1578479Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells assessed as inhibitory constant using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1065637Inhibition of human recombinant HDAC5 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1390022Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1740130Inhibition of human C-terminal His-tagged HDAC3 (1 to 428 residues)/human N-terminal GST-tagged NcoR2 (395 to 489 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1816712Inhibition of HDAC11 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1864268Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c-nu/nu mouse assessed as increment ratio at 10 mg/kg, ip measured for 31 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1548263Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay
AID1650440Inhibition of class 1 histone deacetylase in human Cal27CisR cells assessed as increase in H3 histone acetylation at 3 uM incubated for 24 hrs by immunoblot analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID1702195Antitumor activity against human HepG2 cells xenografted in Ncr nude mouse assessed as tumor growth inhibition at 60 mg/kg, po QD with 5 days on and 2 days off dosing schedule for 2 weeks cotreated with 75 mg/kg pictilisib and measured at day 142018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1127322Antiproliferative activity against p53 defective cis-platinum-resistant human IGROV1/Pt1 cells assessed as growth inhibition after 72 hrs2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1482174Cytotoxicity against human MCF7 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1282300Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1848585Inhibition of full length C-terminal his6/FLAG-tagged human recombinant HDAC3 (1 to 2383 residues) expressed in Sf9 insect cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID350723Ratio of GI50 for human MKN45 cells to IC50 for human recombinant HDAC12009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1541457Inhibition of recombinant human C-terminal His-fusion tagged/N-terminal Strep-2 tagged HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1890339Antitumor immunity in C57BL/6 mouse xenografted with mouse CT26 cells assessed as increase in CD3+ CD8+ cytotoxic T cells at 100 mg/kg, po administered once daily for 21 days measured by flow cytometry analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1390020Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1441659Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in pulmonary edema by measuring lung wet/dry ratio at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by Evans blue dye based met2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID374829Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1650437Inhibition of HDAC6 in human Cal27CisR cells assessed as increase in acetylated alpha-tubulin at 3 uM incubated for 24 hrs by immunoblot analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID274102Inhibition of maize HD1-B (mean)2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID411262Cytotoxicity against HMEC after 72 hrs by trypan blue exclusion assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1282231Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID350729Growth inhibition of human LOXIMVI cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1861343Inhibition of HDAC in human OCILY3 cells assessed as effect on pS6 levels at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1698862Inhibition of HDAC1 (unknown origin)2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID1578886Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1245682Cytotoxicity against human HEL cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1548257Inhibition of class 2 HDAC n human HeLa cell nuclear extracts pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1775568Inhibition of human DNMT1 enzyme using polydeoxy-inosine polydeoxy-cytosine DNA as substrate incubated for 15 mins in presence of SAM by TR-FRET assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1650416Cytotoxicity against human CAL27 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID1537554Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID443633Inhibition of mouse recombinant serine racemase expressed in Escherichia coli MC1061 assessed as formation of D-serine at 5 mM after 30 mins by HPLC analysis2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.
AID1563941Inhibition of recombinant HDAC2 (unknown origin) measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
AID1848596Cytotoxicity against human CCRF-CEM cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1855249Binding affinity to pBR322 DNA (unknown origin) at 50 uM after 30 mins by Agarose gel electrophoresis2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID316892Inhibition of HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID274029Oral bioavailability after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1688021Cytotoxicity against human PC-3 cells assessed as reduction in cell viability after 96 hrs by MTT assay2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID525020Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1201651Antiproliferative activity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1451821Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1231808Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1263067Selectivity ratio of IC50 for human MCF7 cells to IC50 for African green monkey Vero cells2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.
AID1389954Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 70 uM after 24 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1686356Competitive type inhibition of C-terminal His-tagged recombinant human HDAC3 expressed in Sf9 cells pre-incubated for 2 hrs before acetylated lysine-aminomethyl coumarin-BOC addition and measured after 2 hrs by fluorescence based assay based L-B plot anal2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
AID663353Growth inhibition of human NCI-H23 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1174685Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1401535Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1897405Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.02%)
AID1293561Antiproliferative activity against mitoxantrone resistant human HT-29 cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID723451Potentiation of 1 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID723160Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1888407Synergistic antifungal activity against azole-resistant Candida albicans 0304103 assessed as fractional inhibitory concentration index in presence of fluconazole incubated for 48 hrs by CLSI based checkerboard microdilution assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID1166499Antiproliferative activity against human RPMI8226 cells after 72 hrs by WST8 assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1511153Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1275590Inhibition of human recombinant HDAC1 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
AID1464870Inhibition of HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID622258Inhibition of HDAC1 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1386704Inhibition of HDAC in human GM18407 cells harboring NPC1 R404Q/M1142T mutant assessed as restoration of cholesterol trafficking at 0.001 to 5 uM after 48 hrs by filipin-staining based fluorescence microscopic analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1848628Cytotoxicity against human ACHN cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID329926Induction of granulocytic differentiation in human U937 cells assessed as CD11c expression at 5 uM after 30 hrs2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID286792Effect on alpha tubulin acetylation in U937 cells at 1 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID613328Antitumor activity against human HCT116 cells xenografted in athymic nude mouse model assessed as change in tumor volume at 150 mg/kg, ip qd for 21 days relative to control2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID723444Potentiation of 1 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1890514Inhibition of HDAC8 (unknown origin)2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID328796Inhibition of HDAC4 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID760502Inhibition of HDAC11 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1511127Induction of apoptosis in human in human HL60 cells at 0.45 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometric analysis2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID297477Cytotoxicity against human A549 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1421611Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1742628Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated Histone H3 incubated for 8 hrs by Western blot analysis2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID765376Inhibition of recombinant human HDAC7 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID609497Half life in rat liver microsomes2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1441637Inhibition of LTA4H epoxide hydrolase in C57BL/6 mouse neutrophils assessed as suppression of fMLP-induced neutrophil migration pretreated for 30 mins followed by stimulation with fMLP for 1 hr by chemotaxis assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID421197Antitumor activity against human MCF7 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID605393Inhibition of human recombinant HDAC2 using fluor de Lys as substrate by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1164198Antiproliferative activity against human MCF7 cells assessed as reduction in doubling time at 5 uM after 10 to 18 hrs by real-time mode analysis2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1861648Antiproliferative activity against human HCT-116 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID316878Inhibition of HDAC in human CEM cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID421217Inhibition of HDAC3 from human HeLa cells at 5 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID1061952Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1847778Inhibition of HDAC6 in human HeLa cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID1855244Inhibition of HDAC6 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC or Boc-Lys(triflouroacetyl)-AMC as substrate incubated for 30 mins and measured by fluorescence assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1639364Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1812434Antiplasmodial activity against asynchronous asexual culture of Plasmodium falciparum NF54 assessed as parasite growth inhibition2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1403152Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID481565Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1129012Inhibition of human HDAC-10 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1337256Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1439771Inhibition of Pseudomonas aeruginosa PA0321 using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by trypsin-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa.
AID1542187Inhibition of HDAC9 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1655894Inhibition of EZH2 in human U937 cells assessed as H3K27me3 level at 0.5 uM incubated for 120 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1865262Inhibition of full length recombinant his-tagged human HDAC2 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1201646Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1235116Cytotoxicity against human ES2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1597936Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1281867Induction of apoptosis in human RPMI8226 cells assessed as late apoptotic cells at 3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 4.4%)2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1515916Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1777021Inhibition of HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase.
AID408882Inhibition of HDAC32008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1234896Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID744873Cytotoxicity against human U251 cells by MTT assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Discovery of adamantane based highly potent HDAC inhibitors.
AID1676601Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1515909Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1664992Inhibition of class 1 HDAC in CD4 positive cells derived from HIV-infected patient assessed as reactivation of HIV latency by measuring increase in HIV gag p24 level at 400 nM incubated for 72 hrs2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
AID1861326Inhibition of HDAC in human DOHH-2 cells assessed as effect on total Stat3 levels at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1550127Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 7.55%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID255813Inhibitory concentration against Histone deacetylase 2 in maize2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
AID1890311Inhibition of HDAC8 (unknown origin) using Boc-Lys-(triflouroacetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1200972Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1614120Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
AID1164916Inhibition of HDAC11 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1722285Inhibition of HDAC6 in human Hela cells assessed as accumulation of alpha tubulin acetylation at 1.25 to 5 uM incubated for 24 hrs by Western blot analysis2020Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
AID1248356Inhibition of HDAC1/2 in human HeLa cells using Boc-Lys (acetyl)-AMC as substrate incubated for 2 hrs prior to substrate addition measured after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID723133Potentiation of 10 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1915524Inhibition of HDAC-6 (unknown origin) expressed in Escherichia coli BL21 (DE3) in HeLa nuclear extract using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by Bradford reagent method2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1173500Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1326515Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID717792Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID476835Toxicity in FVB mouse assessed as effect on body weight at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1597934Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1614245Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as increase in H3 acetylation at 1 uM after 6 hrs by Western blot analysis
AID1063035Inhibition of recombinant HDAC11 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1614259Toxicity against NOD/SCID mouse xenografted with human MM1S cells assessed as mouse survival at 50 mg/kg, po qd administered for 10 days
AID1754753Inhibition of C-terminal His-tagged human recombinant full length HDAC3 (1 to 428 residues)/N-terminal GST-tagged human recombinant NCOR2 (395 to 489 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin r2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1808552Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1274877Inhibition of HDAC7 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1511136Inhibition of HDAC7 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID734736Inhibition of HDAC1 (unknown origin) at 10 uM after 60 mins by SAMDI spectrophotometric analysis relative to control2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1915564Inhibition of human HDAC6 incubated for 30 mins by SpectraMax M2 microplate reader analysis2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID675299Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate by fluorescence assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
AID603533Cytotoxicity against human K562 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1751994Selectivity ratio of IC50 for HDAC11 (unknown origin) to IC50 for HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID663395Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1765327Inhibition of human full-length recombinant HDAC6 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID723447Potentiation of 0.5 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1511130Inhibition of HDAC3 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1704065Inhibition of c-MET(unknown origin) using FAM labelled peptide substrate at 100 nM preincubated for 10 mins followed by substrate addition and measured by microplate reader method2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID1622963Inhibition of HDAC8 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID538408Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1890510Inhibition of HDAC1 (unknown origin)2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1324233Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID1441698Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in total cell number in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1274871Inhibition of HDAC1 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID488238Inhibition of HDAC3 after 10 mins by fluorometric assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID546549Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1863422Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1127002Induction of apoptosis in human U937 cells assessed as early apoptotic cells using annexin-V/propidium iodide staining at 0.5 uM after 24 hrs by flow cytometry analysis (Rvb = 1.57%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1127333Induction of apoptosis in human IGROV1 cells at IC80 after 72 hrs by TUNEL and flow cytometry analysis (Rvb = 4%)2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1760297Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
AID1578475Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1599783Inhibition of HDAC6 in human Meso163 cells assessed as upregulation of p21 mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID420503Antiproliferative activity against human H460 cells after 72 hrs2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID373081Inhibition of human recombinant HDAC82009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID663334Growth inhibition of human K562 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1127329Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1441700Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1702090Antiproliferative activity against human SNU-398 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1742752Antitumor activity against human MDA-MB-231 cells xenografted in nude mouse assessed as tumor growth inhibition at 150 mg/kg, po administered for 34 days and measured on day 342020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1647328Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as improvement in short-term non-spatial working memory by measuring increase in novel object recognition2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID765222Cytotoxicity against human SKOV3 cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID1816192Inhibition of JAK1 (unknown origin) preincubated for 60 mins followed by reagent A addition and measured after 60 mins in presence of ATP by using microplate reader method
AID1622980Cytotoxicity against human MDA-MB-231 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1164039Antiproliferative activity against human HT1080 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1651331Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID1690842Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assa2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID456796Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID1293563Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1336925Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1380966Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 100 nM after 6 hrs by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1547267Inhibition of HDAC5 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1887064Cytotoxicity against human NCI-H522 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis.
AID1890314Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1449325Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1578148Antiproliferative activity against human HT1080 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1235114Cytotoxicity against HEL cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID723475Cytotoxicity against cisplatin resistant human CAL27 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1174682Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID329918Induction of p21 expression in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID663389Growth inhibition of human ACHN cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID414719Inhibition of HDAC in human HeLa cells assessed as induction of cellular histone H3 hyperacetylation2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1915594Inhibition of HDAC2 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1751997Inhibition of HDAC11 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1599726Cytotoxicity against human ADCA72 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1605937Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID511063Inhibition of HDAC12010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1865258Inhibition of recombinant human HDAC using fluorogenic substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID420513Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at S phase at IC90 using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1469289Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.88%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID411257Selectivity for ratio of IC50 for human HDAC6 to IC50 for human HDAC1/2 by fluorimetric assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID90352In vitro inhibitory activity against human histone deacetylase (HDAC) using HeLa nuclear extract2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.
AID1915526Antiproliferative activity against human DU-145 cells incubated for 48 hrs by Sulforhodamine B staining method2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1614229Induction of apoptosis in human MM1S cells assessed as viable cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 98.9%)
AID1821956Inhibition of HDAC in human HeLa nuclear extracts using fluorometric substrate at 1 uM incubated for 30 mins by fluorescence plate reader analysis relative to control
AID1865308Antitumor immunity against mouse 4T1 cells xenografted in BALB/c syngeneic mouse model assessed as increase in proportion of dendritic cell in lymph node at 40 mg/kg, po qd for 12 days by flow cytometry analysis (Rvb = 17%)2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID353356Inhibition of HDAC in human SHSY5Y cells by fluorimetric cellular activity assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
AID527041Cytotoxicity against human NCI-H226 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1591852Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system at 1000 nM using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay relative to cont2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID411256Inhibition of HDAC6 from human HeLa cells nuclear extract by cell free fluorimetric assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1127009Induction of apoptosis in human U937 cells assessed as late apoptotic cells using annexin-V/propidium iodide staining at 0.125 uM after 24 hrs by flow cytometry analysis (Rvb = 2.13%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1164925Induction of HDAC6 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID331898Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from HDAC in human HeLa nuclear cell extract by fluorescence p2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID750108Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate at 10 uM by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
AID1240553Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 1 uM after 24 hrs using Annexin V-FITC and propidium iodide staining by flow cytometry (Rvb = 2.60%)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID663368Growth inhibition of human NCI-ADR-RES cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID708270Growth inhibition of human HGC27 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1514594Inhibition of HDAC1 (unknown origin) at 20 nM using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID243846Inhibitory activity against human histone deacetylase 1 (HDAC1) at 5 uM2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID274019Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID723158Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1622937Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID358682Increase in E2F1 mRNA expression in rat ST14A cells after 72 hrs by RT-PCR relative to control2007The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators.
AID1545830Antiproliferative activity against human HCT116 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1723743Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
AID473031Ex vivo inhibition of human HDAC5 in human Caco-2 cells by fluorometric cellular activity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID604038Inhibition of histone acetyltransferase in human U937 cells assessed as increase of histone H3 acetylation level at 5 uM after 15 mins by Western blotting2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
AID1454055Growth inhibition of human T47D cells after 3 days by WST1 assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1861655Inhibition of HDAC3 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID421218Inhibition of HDAC8 from human HeLa cells at 5 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID1812441Inhibition of Plasmodium falciparum NF54 HDAC using extract measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1614121Antiproliferative activity against human Raji cells after 72 hrs by MTT assay
AID631667Inhibition of human recombinant full-length HDAC2 using fluorophore conjugated substrate by fluorescence assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).
AID1164032Inhibition of human recombinant HDAC6 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1808553Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID274096Inhibition of maize HD1-A (mean)2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID1421923Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting 2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID749702Inhibition of HDAC8 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1699973Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1890515Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1518829Selectivity index, ratio of EC50 for human MDA-MB-231 cells to IC50 for ring stage Plasmodium falciparum 3D72019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1742660Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID445122Inhibition of HDAC2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID1401507Inhibition of HDAC1/2/3 in human U937 cells assessed as increase in acetyl-histone H3 levels at 5 uM after 18 hrs by Western blot method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1848600Cytotoxicity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1897406Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.41%)
AID723162Potentiation of 25 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1129785Cell cycle arrest in human Jurkat cells assessed as accumulation at G1-phase at 10 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 59.10%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1754781Upregulation of NFkB2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1401531Antiproliferative activity against human Capan1 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1730855Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1816213Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 2.5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.09%)
AID1203889Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID723145Potentiation of 40 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1698861Inhibition of c-MET (unknown origin) at 100 nM relative to control2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID723117Potentiation of 20 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1614231Induction of apoptosis in human MM1S cells assessed as late apoptotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.42%)
AID1189854Therapeutic index, ratio of CC50 for human HuH7 cells to EC50 for HCV genotype 1b infected in human Huh7 cells2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID1764802Selectivity index, ratio of IC50 for recombinant human HDAC1 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay to IC50 for recombinant human HDAC6 using Ac-GAK(2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1784990Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID781052Inhibition of HDAC in human HeLa cell nuclear extracts using Fluor de Lys as substrate at 1 uM by fluorescence assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID1246519Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID90195Concentration required to inhibit Histone Deacetylase (HDAC) from K562 erythroleukemia cells2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).
AID488236Inhibition of HDAC in human SCC4 cells assessed as increase in histone acetylation at 1 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1312850Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1421911Inhibition of recombinant full length human C-terminal His/FLAG tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate measured after 90 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1178598Inhibition of human HDAC8 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1233266Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID1200984Half life in ICR mouse at 10 mg/kg, iv2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1410328Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID760492Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1380945Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID603541Antitumor activity against human MDA-MB-231 cells xenografted in athymic nude mouse assessed as tumor growth delay at 90 mg/kg, ip qd for 21 days2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID81123Percent of HL-60 cells (from human acute promyelocytic leukemia) to develop the ability to reduce nitroblue tetrazolium after administration (1 uM)1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID1330948Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1873418Inhibition of HDAC2 (unknown origin) at 5 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID723477Cytotoxicity against cisplatin resistant human MDA-MB-231 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1361635Inhibition of HDAC8 (unknown origin) after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1737152Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 5.14%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1441667Plasma concentration in human2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID710834Cytotoxicity against human NUGC3 cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID1476156Antiproliferative activity against human XG6 cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1667093Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G1 phase at 5 uM incubated for 48 hrs RNase/PI staining based flow cytometry assay (Rvb = 64.3 %)2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID316906Inhibition of human SKOV3 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID348390Inhibition of HDAC in human NB4 cells assessed as induction of histone H3 acetylation after 6 hrs by Western blot analysis2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents.
AID663331Inhibition of HDAC in human HeLa cell nuclear extracts using Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorimetry2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1469489Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as tumor growth inhibition at 130 mg/kg, ip administered daily for 18 days measured after 8 to 25 days by bioluminescence assay relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID655470Inhibition of HDAC1 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1178597Inhibition of human HDAC3 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1469436Inhibition of HDAC1 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot method2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1141787Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1141788Inhibition of HDAC6 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID723121Potentiation of 8 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1239048Inhibition of recombinant His6-tagged GST-fused human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID1576448Inhibition of HDAC (unknown origin) nuclear extract at 0.5 uM relative to control
AID1861664Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated histone H4 at 2000 nM measured after 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID481557Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID473030Ex vivo inhibition of human HDAC3 in human Caco-2 cells by fluorometric cellular activity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1547268Inhibition of HDAC4 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1155320Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1742756In vivo inhibition of HDAC in tumor of human MDA-MB-231 cells xenografted in BALB/c mouse assessed as increase in acetylated histone-H3 expression by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1178596Inhibition of human HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1763822Inhibition of human recombinant HDAC6 incubated for 15 mins by fluorogenic assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID1819516Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID274117Inhibition of HeLa cell proliferation2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
A series of novel, potent, and selective histone deacetylase inhibitors.
AID723134Potentiation of 10 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1421929Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1274875Inhibition of HDAC5 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID623022Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group.
AID1274835Toxicity in SCID mouse xenografted with human NCI-H460 cells assessed as body weight loss at 50 mg/kg, po qd administered for 15 consecutive days measured daily during compound dosing relative to vehicle-treated control2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1572347Inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 10 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID348799Inhibition of HDAC62008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID1403157Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID274170Antiproliferative activity against H1299 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID286793Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID316910Inhibition of human HDAC82008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID723728Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1251316Inhibition of HDAC1 (unknown origin)2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID723125Potentiation of 45 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID765385Inhibition of recombinant human HDAC6 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1486303Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1181307Inhibition of HDAC6 in human U937 cells assessed as increase in acetyl-alpha-tubulin level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID105419Antiproliferative activity against human MDA-435 breast carcinoma cell line2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
AID313729Inhibition of HDAC12008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID708274Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID748109Inhibition of HDAC6 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1225988Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 2.76%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1865302Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on lung at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID316877Inhibition of human liver HDAC2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID734738Inhibition of HDAC8 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1630598Inhibition of recombinant full length C-terminal His-tagged human HDAC2 expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID760496Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID310182Growth inhibition of human MDA-MB-231 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1437245Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID465157Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1764816Inhibition of Nanoluc-fused HDAC6 CD2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1723742Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
AID373079Inhibition of human recombinant HDAC62009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1597974Inhibition of HDAC in human HeLA cell nuclear extracts2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1141241Inhibition of MMP2 (unknown origin) using succinylated gelatin as substrate preincubated for 10 mins before substrate addition measured after 30 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Design, synthesis and preliminary evaluation of α-sulfonyl γ-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors.
AID1709357Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 48 hrs MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1275655Toxicity in athymic nude mouse xenografted with human HCT116 cells assessed as mortality at 40 mg/kg, ip qd administered for 14 days measured every other day during compound dosing2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1401905Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1482173Cytotoxicity against human A549 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1482121Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID420499Toxicity in athymic nude Swiss mouse bearing human H460 cells assessed as tolerance at 20 to 100 mg/kg, po QD administered 5 days a week for 4 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1348934Upregulation of CDH1 gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1754766Downregulation of HDAC10 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID759311Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1166500Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1688029Induction of apoptosis in human HL-60 cells assessed as increase in accumulation at sub-G1 phase at 2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2.72 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1600735Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1622927Inhibition of maize HD2 using [3H]acetate-labelled histone as substrate by liquid scintillation counting method2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1542184Inhibition of HDAC6 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID288454Growth inhibition of NCI-H23 cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID374817Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1514602Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H4 levels at 1.25 uM by Western blot analysis relative to beta-actin (Rvb = 1 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1887065Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human NCI-H522 cells by methylene blue staining based analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis.
AID675297Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 0.1 uM by fluorescence assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
AID1266092Inhibition of HDAC1 (unknown origin) by fluorimetric assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1702070Inhibition of human full length HDAC11 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1410323Inhibition of recombinant human full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID723128Potentiation of 45 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1469283Induction of apoptosis in human HepG2 cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 96.7%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1667080Inhibition of STAT3 in human MDA-MB-231 cells assessed as downregulation of Bcl-xL expression after 24 hrs by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1863434Inhibition of HDAC2 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1421626Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1727745Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase after 24 hrs by flow cytometry2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID344916Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess 2-oxoglutarate and 10 uM Fe2 by FDH coupled assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID1859931Inhibition of HDAC in human HCT-116 cells assessed as increase in acetylation level of alpha-tubulin at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID672028Inhibition of human recombinant HDAC8 expressed in Escherichia coli using BML-KI-178 as substrate preincubated with compound for 5 mins at 10 uM measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1321724Cytotoxicity against mouse primary glial cells assessed as reduction in cell viability after 72 hrs by luminescence based ATPlite assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID711145Inhibition of HDAC8 at 0.3 uM in presence of 10 mol% Cu(I) by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID1851615Cytotoxicity against HUVEC cells assessed as inhibition of cell growth2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1702087Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID526532Growth inhibition of human PC3 cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1622974Inhibition of HDAC8 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1754763Downregulation of HDAC5 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1901761Inhibition of full length human recombinant HDAC3 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID723473Cytotoxicity against cisplatin sensitive human KYSE-510 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID420501Antiproliferative activity against human NB4 cells after 72 hrs2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID695300Induction of Oct3/4 gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes.
AID1379282Inhibition of class 2 HDAC in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 10 uM after 24 hrs by Western blot analysis2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
AID1401505Cytotoxicity against human Jurkat cells assessed as cell viability at 10 uM after 44 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1466379Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as body weight at 100 mg/kg/day administered via oral gavage for 16 days (Rvb = 19.91 +/- 1.26 g)2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1812435Cytotoxicity against human Hep-G2 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1399552Antiproliferative activity against human A549 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID1572354Antiproliferative activity against human HuH7 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1730862Inhibition of EGFR exon19 deletion/T790M/C797S double mutant (unknown origin) expressed in Ba/F3 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID723131Potentiation of 50 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1597971Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 10 uM incubated for 36 hrs by propidium iodide staining based flow cytometry (Rvb = 10.83%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID269670Antiproliferative activity against human HCT15 cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1182314Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
A potent HDAC inhibitor, 1-alaninechlamydocin, from a Tolypocladium sp. induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
AID609505Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
AID1459947Antiproliferative activity against human HCT116 cells measured after 48 hrs by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID344917Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess H3K9me3 peptide and 10 uM Fe2 by FDH coupled assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID373074Inhibition of human recombinant HDAC12009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID90702Inhibition of Histone deacetylase 6 (HDAC6) of HeLa nuclear extracts2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1415649Inhibition of HDAC6 in human HepG2 cells assessed as increase in acetylated-alpha tubulin level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1398806Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID723443Potentiation of 1 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1275633Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1371070Antiparasitic activity against tachyzoite stage of Toxoplasma gondii2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1622983Cytotoxicity against human PC3 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1875511Selectivity index, ratio of IC50 for cytotoxicity against HMEC cells to GI50 for antiproliferative activity against human NCI-H526 cells2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID1493590Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID1622899Inhibition of HDAC in human HeLa nuclear extract at 100 uM using Fluor-de-lys as substrate measured after 15 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1861649Antiproliferative activity against human MCF7 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1126959Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1129009Inhibition of human HDAC-7 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID487874Antiproliferative activity against human A549 cells after 48 hrs2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
AID1240556Induction of apoptosis in human MDA-MB-231 cells assessed as total apoptotic cells at 1 uM after 24 hrs using Annexin V-FITC and propidium iodide staining by flow cytometry2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID1578896Inhibition of HDAC in human Bel7402 cells assessed as increase in acetylated alpha-tubulin expression at 5 uM incubated for 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1742182Inhibition of recombinant human full-length N-terminal GST-tagged HDAC5 expressed in baculovirus infected Sf9 insect cells using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1861255Antiproliferative activity against human A549 cells assessed as reduction in cell viability2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1652195Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1785337Inhibition of recombiant human HDAC6 using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence microplate reader assay
AID1433298Induction of DNA damage in p53 null human U937 cells assessed as decrease in Rad51 expression level by measuring ratio of Rad51 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1633990Inhibition of HDAC2 in human HuH7 cells assessed as increase in histone H3 K9/K14 acetylation at varying concentrations incubated for 24 hrs by Western blot analysis2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID765374Inhibition of recombinant human HDAC9 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1126960Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID772639Inhibition of full length FLAG-tagged recombinant HDAC3 (unknown origin) transfected in human HeLa cells assessed as deacetylation of [3H]-acetylated histones after 2 hrs by scintillation counting analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.
AID1898895Antiproliferative activity against human H460-R9A cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1576449Inhibition of recombinant HDAC1 (unknown origin) expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence based protease coupled assay
AID1876344Inhibition of recombinant full length HDAC11 (unknown origin) expressed in insect Sf9 cells by EMSA analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID708279Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID445136Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID1873401Inhibition of HDAC1 (unknown origin) preincubated for 60 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1542183Inhibition of HDAC5 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID541650Inhibition of human HDAC7 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1785350Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
AID1380987Antitumor activity against human HT-29 cells xenografted in BALB/c nu mouse assessed as tumor growth inhibition at 100 mg/kg, po administered for 25 consecutive days measured every 3 days during compound dosing relative to control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID628439Inhibition of human recombinant HDAC8 using Fluor de Lys as substrate2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1202584Inhibition of His-tagged HDAC6 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID760493Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1126978Antiproliferative activity against HEL cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID628208Antiproliferative activity against human SH-SY5Y cells after 48 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID723471Inhibition of HDAC in cisplatin resistant human MDA-MB-231 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1783064Antifungal activity against Cryptococcus neoformans H99 assessed as inhibition of fungal growth incubated for 72 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1486323Genotoxicity in Salmonella typhimurium TA102 at 50 times antiproliferative IC50 by Ames test2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID749697Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTS assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1063058Inhibition of recombinant HDAC3 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID737910Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID420508Induction of apoptosis in human IGROV1 cells at IC80 after 72 hrs by TUNEL assay2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1547315Increase in phosphorylated STAT3 expression in tumor tissue of BALB/cAnNCrl mouse xenografted with human HCT116 cells at 30 mg/kg, po administered on day 1 to day 19 measured on day 19 by immunohistochemical analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1591721Inhibition of Class 1 histone deacetylase in mouse RAW264.7cells cells assessed as increase in histone acetylation at 0.3 to 3 uM after 24 hrs by Western blot analysis2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1280280Inhibition of class1 HDAC in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 0.1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1451824Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1888410Cytotoxicity against human HaCaT cells assessed as inhibition of cell growth2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID723442Potentiation of 5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1201643Inhibition of human recombinant FLT3 after 1 hr by LanthaScreen assay platform2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID445137Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID663339Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1173504Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1127326Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1739589Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated H3/GAPDH at 1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID482973Antitumor activity against human PC3 cells xenografted in nude mouse assessed as inhibition of tumor growth at 160 mg/kg, ip administered for 21 days measured or day 222010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID603534Cytotoxicity against human NB4 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID663367Growth inhibition of human OVCAR8 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1282285Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as change in body weight at 50 mg/kg, ip q2d for 9 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1541443Inhibition of human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1650408Inhibition of HDAC6 in human CAL27 cells assessed as increase in acetylated alpha-tubulin at 3 uM incubated for 24 hrs by immunoblot analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID208380Concentration required to inhibit complete cell proliferation of T/5 cells1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID673991Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1282259Cytotoxicity against human H460 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1864253Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1888420Inhibition of human HDAC2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID759308Therapeutic index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells expressing ERalpha and ERbeta2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1449319Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1684873Toxicity in mouse LL/2 cells inoculated C57BL/6J mouse assessed as effect on body weight by measuring initial body weight at 25 mg/kg, ip administered for 12 days measured for every 2 days (Rvb = 18.4 +/- 0.4 g)
AID1549162Inhibition of HDAC in azole-resistant Candida albicans 0304103 protoplasts using Boc-Lys(Ac)-AMC as substrate preincubated for 12 hrs followed by substrate addition and measured after 4 hrs by fluorimetry2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1614228Induction of apoptosis in human MM1S cells assessed as necrotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.32%)
AID1235260Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
AID1742721Induction of apoptosis in mouse 4T1 cells assessed as late apoptotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 2.24 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID723427Potentiation of 0.75 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1396959Antiproliferative activity against human HCT116 cells2018Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
AID1330946Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1398802Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID525024Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 1 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1898901Antiproliferative activity against human MM473 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1127004Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 0.25 uM after 24 hrs by flow cytometry analysis (Rvb = 96.24%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID605622Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 300 nM after 15 hrs by propidium iodide staining based flow cytometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1758470Inhibition of human recombinant HDAC10 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1227024Half life in patient serum at 400 mg single dose2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID732871Inhibition of HDAC2 in human MDA-MB-231 cells assessed as decrease in acetylation levels of histone H4 at 1 uM by Western blot analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID411260Cytotoxicity against human DU145 cells after 72 hrs by trypan blue exclusion assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1165117Inhibition of HDAC6 in human LNCAP cells assessed as tubulin acetylation by Western blot analysis2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1901156Inhibition of HDAC4 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1280275Inhibition of HDAC6 in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 10 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID246069Effective Concentration of compound to inhibit the growth of human SNB-78 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1576454Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID269917Selectivity index, EC50 for histone H4 acetylation/EC50 for alpha-tubulin acetylation in HCT116 cells2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID1126980Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1917528Inhibition of PI3Kdelta (unknown origin) measured by ADP-Glo assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID1633435Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of N-myc mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID616004Inhibition of HDAC4 using Boc-Lys(TFA)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID440820Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
AID1466061Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1765324Inhibition of human full-length recombinant HDAC1 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1129004Inhibition of human HDAC-2 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1863438Inhibition of HDAC6 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1126958Inhibition of HDAC in human HeLa nuclear extracts using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1469380Inhibition of HDAC1 (unknown origin)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1234895Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1614123Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay
AID488235Inhibition of HDAC in human SCC4 cells assessed as increase in tubulin acetylation at 1 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1751993Selectivity ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1421916Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID748982Inhibition of HDAC4 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID350724Ratio of GI50 for human MKN45 cells to IC50 for human recombinant HDAC22009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1486307Antiproliferative activity against human HCC1937 cells after 3 days by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1275643Growth inhibition of human MDA-MB-231 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID732877Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1548269Inhibition of class 1 HDAC in human RPMI8226 cells assessed as increase in Ac-H3 accumulation at 10 to 1000 nM incubated for 24 hrs Western blotting analysis
AID1514608Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 1.25 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 3.2 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID511066Inhibition of HDAC62010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID732145Inhibition of HDAC3 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1164775Stability of the compound in aqueous solution at pH 1.2 after 24 hrs2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1466056Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1623536Selectivity index, ratio of IC50 for human recombinant HDAC7 to IC50 for human recombinant HDAC62019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1127000Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 0.5 uM after 24 hrs by flow cytometry analysis (Rvb = 96.24%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1486674Inhibition of HDAC1 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID663337Growth inhibition of human OVCAR3 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID748984Inhibition of HDAC2 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1543967Induction of DNA damage in human Bel7402/5-FU cells assessed as increase in phosphorylated H2AX levels at 5.0 uM incubated for 72 hrs by Western blot assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1742661Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1898919Inhibition of POLA1 in human NCI-H460 cells at 7.4 uM assessed as upregulation of p21 expression and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1273876Inhibition of human CYP1A2 using 3-cyano-7-ethoxycoumarin as substrate at 10 uM after 15 mins by fluorimetric analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID473032Ex vivo inhibition of human HDAC7 in human Caco-2 cells by fluorometric cellular activity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID420654Toxicity in athymic nude Swiss mouse bearing human HCT116 cells assessed as body weight loss at 100 mg/kg, po QD administered 5 days a week for 4 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID717818Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 2.5 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1518810Effect on human KMS-12-BM cells assessed as increase in H3K9Me2 level at 2.5 to 5 uM incubated for 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID443647Binding affinity to pyridoxal-5'-phosphate assessed as formation of syn- and anti-PLP-aldoxime by NMR spectroscopy2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.
AID1141777Induction of apoptosis in human HCT116 cells assessed as accumulation at sub-G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID489914Cytotoxicity against human U251 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
AID1280272Selectivity index, ratio of HDAC6 inhibition in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 10 uM over class1 HDAC inhibition in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 10 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1742179Inhibition of recombinant human GST-fused HDAC3/NCOR1 (397 to 503 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID616003Inhibition of human HDAC8 using Boc-Lys(TFA)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID760377Cytotoxicity against human Jurkat cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1478585Induction of apoptosis in human K562 cells assessed as viable cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 92.4%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID526534Growth inhibition of human ACHN cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1263142Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1371076Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID411258Cytotoxicity against human SKMES1 cells after 72 hrs by trypan blue exclusion assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1361633Inhibition of HDAC3 (unknown origin) after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1742178Inhibition of human full-length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1737155Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 3 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.51%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1330925Inhibition of HER2 (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1383999Inhibition of HDAC1/2/3 in human HeLa cells assessed as increase in acetyl-histone H4 level at 2 uM after 12 hrs by Western blot analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1667082Inhibition of STAT3 in human MDA-MB-231 cells assessed as change in Bcl-2 expression at 0.8 to 1.6 uM after 24 hrs by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1742656Cytotoxicity against human Bcap37 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID440821Inhibition of human recombinant N-terminal FLAG-tagged HDAC4 (612-1034) expressed in baculovirus after 10 mins by fluorimetric analysis2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
AID1246522Cytotoxicity against HEK293 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1469374Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1548262Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay
AID1650412Inhibition of recombinant human HDAC22020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID347867Growth inhibition of human lung cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1811394Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as TGI at 50 mg/kg, po administered 3 times week for 21 days2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID1826627Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 0.0046 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1873413Inhibition of HDAC3 (unknown origin) preincubated for 120 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID482946Inhibition of HDAC62010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1622902Cytotoxicity against human K562 cells after 72 hrs by CellTiter-Glo assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1550120Induction of apoptosis in HEL cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 0.023%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1279128Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID1266839Activation of p53 in human HCT116 cell at 0.1 to 5 uM after 12 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1861250Inhibition of PARP-1 derived from human HeLa cell nucleus2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1164172Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by trypan blue dye exclusion method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1231813Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1401480Selectivity ratio of IC50 for HDAC6 in human HeLa-S3 cell lysates to IC50 for HDAC3 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID481573Cytotoxicity against mouse S180 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1055716Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1515905Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1821272Inhibition of HDAC3 (unknown origin) incubated for 30 mins by microplate reader assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1647331Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as ratio of cerebral blood flow in left parietal area at 25 mg/kg, ip administered post surgery measured 2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1709347Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1865299Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on heart at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID297476Cytotoxicity against human NCI H460 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1129786Cell cycle arrest in human Jurkat cells assessed as accumulation at S-phase at 10 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 23%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1231807Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1355731Protection against spleen enlargement in SCID mouse xenografted with human HEL cells at 10 mg/kg, ip qd2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1667096Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at S phase at 5 uM incubated for 48 hrs RNase/PI staining based flow cytometry assay (Rvb = 11.5 %)2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1548284Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID313732Inhibition of HDAC42008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1441631Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID672022Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1486295Antiproliferative activity against human T47D cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID723425Potentiation of 5 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1164024Inhibition of human recombinant HDAC1 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1421627Antiproliferative activity against human KMS-12-BM cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1422516Inhibition of HDAC in MEF assessed as increase in histone H4K5 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1437240Inhibition of HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID1129770Inhibition of HDAC in human Jurkat cells assessed as increase in H3K23 acetylation at 10 uM after 12 hrs by FACS flow cytometric analysis relative to control2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1572349Inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 0.1 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1888581Inhibition of recombinant human HDAC1 expressed in baculovirus infection system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay
AID1274878Inhibition of HDAC8 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID655477Inhibition of recombinant human HDAC2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1537557Antiproliferative activity against human CHP134 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1266093Inhibition of HDAC2 (unknown origin) by fluorimetric assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID775832Inhibition of human carbonic anhydrase 2 assessed as p-nitrophenyl acetate conversion to p-nitrophenolate anion at 10 uM preincubated for 10 mins prior to substrate addition measured for 20 mins by spectrophotometric analysis relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1206768Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect S9 cells after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1514609Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells at 1.25 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 1.8 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID90359Concentration required for inhibition of histone deacetylase HD2 in vitro.2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity.
AID316876Inhibition of human SQ20B cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1821964Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
AID1769648Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by addition of substrate and trypsin measured by flourescence assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1398800Inhibition of human full length C-terminal His-tagged HDAC3/N-terminal GST-tagged human NCOR2 (395 to 489 residues) expressed in baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1421903Antiplasmodial activity against multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1832687Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured 2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1811370Inhibition of HDAC6 (unknown origin) at 1 uM using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID1890335Stability in human liver microsomes assessed as clearance and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1246516Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID525027Inhibition of HDAC7 in human CFBE41o- cell line assessed as correction of mutant Fdelta508 CFTR trafficking to cell surface as glycoform at 5 uM by Immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID663380Growth inhibition of human M14 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1352483Inhibition of HDAC6 in human HeLa cells after 72 hrs by ELISA2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID1832801Inhibition of human recombinant HDAC1 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID631669Inhibition of human recombinant full-length HDAC6 using fluorophore conjugated substrate by fluorescence assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).
AID434538Cytotoxicity against human H460 cells after 24 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.
AID663382Growth inhibition of human SK-MEL-2 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1205627Growth inhibition of human PC3 cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID482975Antitumor activity against human HCT116 cells xenografted in BALB/c mouse at 200 mg/kg, po after 21 days2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID711158Inhibition of HDAC2 by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID1227047Cytotoxicity against human HH cells assessed as cell proliferation after 70 hrs by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1861327Inhibition of HDAC in human OCILY3 cells assessed as effect on total Stat3 levels at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID316885Antiproliferative activity against human A549 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1690104Growth inhibition of human NCI-H1975 cells incubated for 48 hrs by SRB assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID288451Growth inhibition of PC3 cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID316880Inhibition of mouse liver HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID274073AUC after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1720096Inhibition of HDAC (unknown origin)2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID619041Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1548291Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID473185Induction of P21WAF1 gene expression in human Caco-2 cells at 5 uM after 24 hrs by Western blotting2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1478591Inhibition of HDAC1 (unknown origin) using substrate after 30 mins by fluorometric analysis2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1164781Inhibition of HDAC2 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1688025Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins 2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1826600Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1129011Inhibition of human HDAC-9 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1205633Induction of myc-tagged RUNX3 acetylation in human HEK293 cells assessed as acetylated RUNX3 level at 1 uM after 24 hrs by immunoprecipitation analysis relative to TSA2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1537567Cell cycle arrest in human G55T2 cells assessed as accumulation in S phase at 3 uM incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 14.7 %)2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1876339Cytotoxicity against human MRC9 cells assessed as cell viability incubated for 72 hrs by Cell titer- blue assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID1898497Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer.
AID1515881Induction of apoptosis in human HCT116 cells assessed as live cells at 500 nM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 89.6%)2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID343687Inhibition of recombinant HDAC1 expressed in HEK293 cells2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
AID1599774Inhibition of HDAC6 in human A549 cells assessed as increase in alpha tubulin acetylation at 2.5 uM measured after 6 to 20 hrs by Western blot analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1535345Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.
AID1127323Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID420502Inhibition of HDAC2 in human HeLa cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1614195Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 5.03%)
AID1164786Inhibition of HDAC11 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1812439Inhibition of human HDAC using human HeLa cell nuclear extract measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID84275Antiproliferative activity against human HT1080 fibrosarcoma cell line2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
AID481547Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1742185Inhibition of recombinant human C-terminal His-tagged HDAC10 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID449261Antiproliferative activity against human HCT116 cells after 2 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors.
AID765384Inhibition of recombinant human HDAC10 enzyme using tetrapeptide Ac-ArgThr-Lys(Ac)Lys(Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1250656Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1164180Induction of apoptosis in human U937 cells using annexin-V/PI staining after 48 hrs by flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1431820Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1897372Inhibition of FGFR4 (unknown origin)
AID382344Viability of human DU145 cells after 72 hrs by MTS assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
AID274074Oral bioavailability after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1390017Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1441640Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in pathological changes at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by hematoxylin and eosin staining based2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID725667Inhibition of C-terminal His-tagged human recombinant HDAC9 (amino acids 604- 1066) expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured afte2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
AID652765Induction of CFTR deltaF508 mutant mRNA expression in cystic fibrosis patient lung cells relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1727730Inhibition of HDAC6 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1873392Antiproliferative activity against human MV4-11 cells2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1518784Antiproliferative activity against human KMS-12-BM cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1655790Inhibition of human recombinant HDAC4 using AMC-K(TFA)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID328832Toxicity in ip dosed BALB/c mouse assessed as maximum tolerated dose2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1518785Antiproliferative activity against human NCI-H929 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1848322Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase at 1 uM incubated for 48 hrs by AnnexinV/PI staining based flow cytometry (Rvb = 11.5%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID1897398Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 0.1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.41%)
AID1274881Inhibition of HDAC11 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID329915Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1821267Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID747266Growth inhibition of human HeLa cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1384229Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 100 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID297497Cytotoxicity against human K562 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1752940Antiplasmodial activity against drug-sensitive asexual intraerythrocytic stage of Plasmodium falciparum 3D7 infected in human O+ erythrocytes assessed as inhibition of parasite growth incubated for 48 hrs followed by addition of [3H]hypoxanthine for 24 hr
AID1633422Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 5 uM incubated for 30 hrs by Western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID1227032Inhibition of human recombinant HDAC6 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1915563Inhibition of human HDAC2 incubated for 30 mins by SpectraMax M2 microplate reader analysis2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID603543Inhibition of HDAC6 in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID90671Inhibitory activity afgainst maize Histone deacetylase 1-A2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1545817Antiproliferative activity against human MCF7 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1633437Immunomodulatory activity in LPS treated Wistar rat primary microglial cells assessed as decrease in NOS2 expression level at 5 to 50 uM incubated for 24 hrs by western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID1754777Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl3 gene expression at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1742668Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID732873Inhibition of HDAC2a in human MDA-MB-231 cell lysate using Boc-Lys(trifluroacetyl)-AMC as substrate at 10 uM preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID723118Potentiation of 20 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID417069Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives.
AID1518781Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1742667Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1623529Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1742759In vivo inhibition of HDAC in tumor of mouse 4T1 cells xenografted in BALB/c mouse assessed as increase in acetylated histone-H3 expression by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1281852Antiproliferative activity against human RPMI8226 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1139707Growth inhibition of human HeLa cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.
AID1231809Inhibition of recombinant HDAC8 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID723428Potentiation of 0.75 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1819515Antiproliferative activity against HEL cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1129793Induction of apoptosis in human Jurkat cells assessed as caspase 3/7 activation at 10 uM after 6 hrs by luminescence assay (Rvb = 59,417 +/- 10002.74 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1449214Inhibition of C-terminal FLAG/His-tagged recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID1548245Inhibition of HDAC1 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1578155Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1547344Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in LIFR expression at 10 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1339586Growth inhibition of human MOLM13 cells after 44 hrs by MTT assay2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID1754773Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID723446Potentiation of 0.5 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1348933Upregulation of TIMP3 gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1355715Synergistic antifungal activity against FLC resistant Candida albicans 100 assessed as FIC index after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID717806Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1296349Inhibition of recombinant human HDAC6 using Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition measured after 20 mins by fluorescence assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.
AID1537561Antiproliferative activity against human G55T2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID759301Cytotoxicity against human MCF7 cells expressing ERalpha and ERbeta assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID670099Antitumor activity against human A549 cells xenografted in nude mouse assessed as time to end point at 200 mg/kg, po administered QD till end point2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1200975Intrinsic clearance in human liver microsomes at 1 uM preincubated for 10 mins followed by NADPH addition measured over 30 mins by LC-MS/MS analysis2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1888406Synergistic antifungal activity against azole-resistant Candida albicans 0304103 assessed as fractional inhibitory concentration incubated for 48 hrs by CLSI based checkerboard microdilution assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID1348915Inhibition of C-terminal FLAG/His-tagged full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1578917Inhibition of PI3K/AKT/mTOR signaling in human Bel7402 cells assessed as reduction in AKT phosphorylation at 5 uM after 24 to 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID302099Antiproliferative activity against H661 cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues.
AID603536Cytotoxicity against human ES2 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1126998Induction of apoptosis in human U937 cells assessed as early apoptotic cells using annexin-V/propidium iodide staining at 1 uM after 24 hrs by flow cytometry analysis (Rvb = 1.57%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1563943Inhibition of recombinant HDAC6 (unknown origin) measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
AID1864240Inhibition of HDAC in human MDA-MB-231 cells incubated for 45 mins by luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1422513Inhibition of HDAC in MEF assessed as increase in histone H3K9 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1170746Inhibition of human recombinant HDAC11 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1282254Cytotoxicity against human Ramos cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1548729Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1697202Inhibition of HDAC6 (unknown origin)2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID289928Antiproliferative activity against human H661 cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and biological evaluation of the suberoylanilide hydroxamic acid (SAHA) beta-glucuronide and beta-galactoside for application in selective prodrug chemotherapy.
AID343688Inhibition of recombinant HDAC6 expressed in HEK293 cells2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
AID300836Growth inhibition of human MDA-MB-231 cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID1511133Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1821273Inhibition of HDAC6 (unknown origin) incubated for 30 mins by microplate reader assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1622960Inhibition of HDAC1 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1731760Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life at 5 uM preincubated for 5 mins followed by NADPH addition and measured after 60 mins by LCMS analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
AID1401476Selectivity ratio of IC50 for HDAC3 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1599730Cytotoxicity against human ADCA72 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1865267Inhibition of recombinant his-tagged human HDAC6 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1326516Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated alpha-tubulin after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID747268Inhibition of human recombinant HDAC7 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1409640Inhibition of HDAC in human HeLa cells using Boc-K(Ac)-AMC as substrate by fluorescence assay2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.
AID1785346Inhibition of full length human CDK6 (1 to 326 end residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay
AID1250655Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1266810Antiproliferative activity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1591856Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID1869146Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
AID674000Growth inhibition of human HeLa cells after 72 hrs by XTT assay2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1451832Inhibition of GST tagged human recombinant HDAC4 (H86 to 31G) expressed in Baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1576466Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 5 uM after 72 hrs by Annexin V-phycoerythrin/7-AAD staining based flow cytometric analysis (Rvb = 1.84%)
AID274015Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1401534Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID499800Inhibition of HDAC82010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1462217Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1887682Cytotoxicity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID329920Induction of granulocytic differentiation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID546547Inhibition of human recombinant HDAC1 expressed in HEK293 cells2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID90685Inhibition of Histone deacetylase 2 (HDAC2) activity of HeLa nuclear extracts2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1449324Inhibition of HDAC in human A2780CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1890328Induction of apoptosis in mouse CT26 cells assessed as apoptotic cells at 6 uM measured by Annexin V-FITC/PI staining based flow cytometry method2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID373073Inhibition of HDAC from human HeLa cells2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID465152Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1482118Cytotoxicity against human COLO205 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1129800Induction of apoptosis in human Jurkat cells assessed as caspase 8 responsive cells level at 10 uM after 24 hrs by FACS flow cytometric analysis (Rvb = 0.32%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1162486Growth inhibition of human PC3 cells after 72 hrs by CellTiter Glo assay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
AID1566037Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence b2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID316931Inhibition of HDAC32008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1441670Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in macrophage number in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID496806Inhibition of human HDAC62010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID723126Potentiation of 45 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1164184Inhibition of human recombinant HDAC6 using Z-MAL as substrate at 5 uM after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1380946Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1164038Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1225986Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.05%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID316896Inhibition of human HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1898925Antiproliferative activity against human NCI-H460 cells at 7.4 uM assessed as reduction in PIN1 level and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1339584Growth inhibition of human Jurkat cells at 1 to 10 uM after 44 hrs by MTT assay2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID310181Growth inhibition of human PC3 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1502979Antiproliferative activity against human SW620 cells incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID316908Inhibition of human St4 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID344919Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of 50 uM Fe by FDH coupled assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID482950Inhibition of HDAC112010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1177056Antiprotozoan activity against Leishmania donovani MHOM- ET-67/L82 amastigotes at 1 uM2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1614133Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID663371Growth inhibition of human DU145 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1164784Inhibition of HDAC8 (unknown origin) using fluorogenic tetrapeptide RHK(Ac)K(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1901228Half life in dog liver microsomes by LC-MS/MS analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID90681Inhibition of mouse HDAC12004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID1742662Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID604039Inhibition of histone acetyltransferase in human MCF7 cells assessed as increase of alpha-tubulin acetylation level at 5 uM after 15 mins by Western blotting2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
AID732146Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID228859Activity in histone hyperacetylation assay in cells2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1250657Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1464877Anti-proliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1763817Antiproliferative activity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID1819545Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as fold increase in proportion of macrophages in spleen by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID605298Inhibition of HDAC in human HeLa cells nuclear extract using fluor de Lys as substrate preincubated for 5 mins by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1676591Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID723445Potentiation of 1 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.25 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1403159Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1296347Inhibition of recombinant human HDAC8 using Fluor de Lys as substrate preincubated for 90 mins followed by BML-KI176 addition measured after 45 mins by fluorescence assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.
AID1482119Cytotoxicity against human Caco2 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1225978Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1260656Binding affinity to human recombinant HDAC8 by fluorescence assay
AID1737149Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 4.01%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1848320Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G0/G1 phase at 1 uM incubated for 48 hrs by AnnexinV/PI staining based flow cytometry (Rvb = 33.1%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID1614230Induction of apoptosis in human MM1S cells assessed as early apoptotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.38%)
AID1737134Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID353355Inhibition of HDAC in human SHSY5Y cells at 10 uM by fluorimetric cellular activity assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
AID1401536Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1622935Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1361626Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1275645Growth inhibition of human PC3 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID373078Inhibition of human recombinant HDAC52009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1174687Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID525018Inhibition of HDAC in human CFBE41o- cell line assessed as increase in mutant Fdelta508 CFTR protein level at 5 uM after 4 hrs by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1821323Antitumor activity against human HepG2 cells xenografted in mouse assessed as upregulation of acetylated alpha tubulin level at 12 mg/kg, ip administered every 2 days for 4 weeks by western blot analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1164195Inhibition of HDAC in human MCF7 cells assessed as hyperacetylation of p53 at Lys 382 residue at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1348921Inhibition of N-terminal GST-tagged human HDAC7 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID465149Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1547345Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in JAK1 expression at 10 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1129013Inhibition of human HDAC-11 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID663404Half life in artificial intestinal fluid2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1441650Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in TNFalpha level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1859933Inhibition of HDAC in human HCT-116 cells assessed as increase in acetylation level of H3K9-14ac at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1067347Inhibition of HDAC1/2 in human HeLa cell extracts using acetylated histone peptide as substrate after 30 mins2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1864676Inhibition of full length recombinant human HDAC6 in MV4-11 cells assessed as upregulation of acetylated histone H3 at 1 uM measured upto 24 hrs by western blot analysis
AID1578883Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID488277Inhibition of HDAC82010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1126976Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1754772Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1174681Antiproliferative activity against human U266 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1294804Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate at 0.5 uM by fluorometric assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors.
AID604081Inhibition of JMJD2E pre-incubated for 30 mins2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Inhibitors of histone demethylases.
AID1415648Inhibition of HDAC3 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1542182Inhibition of HDAC4 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1785352Synergistic antiproliferative activity against human A549 cells assessed as combination index in presence of palbociclib by Chou-Talalay method
AID1865243Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID544093Antimalarial activity against drug-resistant Plasmodium falciparum TM90C2A2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID652753Inhibition of recombinant human HDAC9 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1155322Selectivity index, ratio of IC50 for erythrocytes (unknown origin) to IC50 for Plasmodium falciparum2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1250647Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1434362Inhibition of HDAC in HEK293 cells assessed as ratio of acetylated-RUNX3 level to histone-3 acetylation level at 1 uM measured after 24 hrs by Western blot analysis relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1882466Inhibition of HDAC3 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1336933Inhibition of HDAC6 in human LNCAP cells assessed as acetylated tubulin accumulation in cytosol at 10 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID663392Growth inhibition of human TK10 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID525025Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 0.1 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID476834Toxicity in FVB mouse assessed as effect on hematocrit at 50 mg/kg, po administered 5 times per week for 2 weeks2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1739582Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated H3/GAPDH at 10 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID274036Hepatocyte stability2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID476642Antiproliferative activity against human HT-29 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1469334Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID622255Inhibition of HDAC1 after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1676597Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1251317Inhibition of HDAC6 (unknown origin)2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1566805Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1164185Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1887684Cytotoxicity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID329917Induction of alpha tubulin hyperacetylation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1578887Inhibition of human HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1751985Antiproliferative activity against human A549 cells assessed as reduction in cell viability2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID445135Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID1352479Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID1832796Cytotoxicity against human HL-60 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID1890350Selectivity ratio of IC50 for recombinant human HDAC1 over IC50 for recombinant human HDAC62022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID672030Selectivity ratio of IC50 for human HDAC2 preincubated with compound for 3 hrs to IC50 for human HDAC1 preincubated with compound for 3 hrs2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1633434Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of MAP-2 mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID748983Inhibition of HDAC1 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1441703Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as intact alveolar structure at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by hematoxylin and eosin staining based microsc2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1742222Tmax in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1821338Toxicity in mouse xenografted with human HepG2 cells assessed as cellular inflammation in heart at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID622254Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1355096Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
AID1886184Inhibition of HDAC2 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1742669Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID274068Oral bioavailability after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1421913Inhibition of HDAC in synchronized trophozoite stage Plasmodium falciparum 3D7 infected in human erythrocytes assessed as increase in acetylated H4 level at 5 times IC50 after 3 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1566822Antiproliferative activity against human Raji cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1487006Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC3 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1754775Induction of apoptosis in human MCF7 cells assessed as increase in caspase 3/7 activity at 1 to 3 uM measured after 48 hrs by ELISA2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1816189Inhibition of recombinant HDAC4 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis
AID1263060Inhibition of NTHi-induced NF-kappaB activation in human BEAS-2B cells treated 1 hr before NTHi stimulation measured after 5 hrs by luciferase assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.
AID1702141Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin at Lys40 residue incubated for 3 hrs by ELISA2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1404300Antiproliferative activity against human SK-MEL-28 cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1396989Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
AID1231814Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID755622Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1754769Inhibition of HDAC in human MCF7 cells assessed as increase in histone H2A acetylation at 1 to 3 uM incubated for 24 hrs by Western blot analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1164035Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1742650Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID717826Inhibition of HDAC1 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1754762Downregulation of HDAC4 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1263146Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID481549Cytotoxicity against human HO8910 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1352482Inhibition of HDAC4 in human HeLa cells after 72 hrs by ELISA2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID1652192Inhibition of human recombinant HDAC6 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1861652Cytotoxicity against human L02 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1826612Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 10 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1164033Inhibition of human recombinant HDAC10 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1563944Inhibition of recombinant HDAC8 (unknown origin) measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
AID618083Toxicity in athymic nu/nu Harlan mouse xenografted with human HCT116 cells assessed as body weight loss at 200 mg/kg, po QD for 21 days measured on day 192011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1326526Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as tumor growth inhibition at 200 mg/kg, po qd2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1398815Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of TFF1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1821266Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1380952Inhibition of HDAC1 (unknown origin) using fluorogenic substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1464878Anti-proliferative activity against human MRC5 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID652748Inhibition of recombinant human HDAC4 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1702092Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID765383Inhibition of recombinant human HDAC11 enzyme using Ac-LeuGlyLys(Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID609496Cardiac safety index, Ratio of IC50 for human ERG to IC50 for human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1454054Growth inhibition of human MDA-MB-231 cells after 3 days by WST1 assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID322414Antiproliferative activity against human LNCap by MTT assay2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID1246512Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1401906Selectivity ratio of IC50 for human recombinant HDAC2 to IC50 for human recombinant HDAC62018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID316903Inhibition of human HCT116 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1699972Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1126994Induction of apoptosis in human U937 cells assessed as early apoptotic cells using annexin-V/propidium iodide staining at 1 uM after 12 hrs by flow cytometry analysis (Rvb = 1.58%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1864270Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c-nu/nu mouse assessed as tumor growth inhibition at 10 mg/kg, ip measured for 31 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID732449Inhibition of human U937 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID737915Inhibition of recombinant HDAC6 (unknown origin) after 10 mins by fluorimetric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1751987Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1542180Inhibition of HDAC2 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1269323Cytotoxicity against human U251MG cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID711146Inhibition of HDAC8 at 0.3 uM in absence of Cu(I) by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID759300Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1752946Antiplasmodial activity against liver stage exo-erythrocytic forms of Plasmodium berghei sporozoites infected in human HepG2-A16-CD81EGFP cells assessed as inhibition of parasite growth compound incubated with cells for 24 hrs prior to infection and measu
AID760512Inhibition of HDAC1 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID411254Inhibition of HDAC8 from human HeLa cells nuclear extract by cell free fluorimetric assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1816223Induction of apoptosis in mouse 4T1 cells assessed as necrotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.35%)
AID350721Growth inhibition of human MKN45 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID663361Growth inhibition of human KM12 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1459946Antiproliferative activity against human A549 cells measured after 48 hrs by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1548265Induction of apoptosis in human RPMI8226 cells incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry
AID1550121Induction of apoptosis in HEL cells assessed as necrotic apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 0.011%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID748107Inhibition of HDAC9 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1754754Inhibition of N-terminal GST-tagged/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based anal2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID628451Inhibition of HDAC in human HepG2 cells assessed as increase in histone H4 acetylation at 1 to 10 uM after 24 hrs by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1246520Cytotoxicity against human THP1 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1550104Inhibition of HDAC2 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1441688Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 level in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1246511Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1764251Inhibition of recombinant human full length C-terminal GST-fusion tagged HDAC2 expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID461266Antiproliferative activity against human LNCAP cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1178595Inhibition of human HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID503663Effect on FXN mRNA expression in human GM15850 cells at 5 uM after 12 hrs by qRT-PCR analysis2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1469395Induction of apoptosis in human Hep3B cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.91%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1566038Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID1233268Therapeutic index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID1293566Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1775548Inhibition of HDAC6 (unknown origin)2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID628449Induction of apoptosis in human HepG2 cells assessed as hyperacetylation of p53 at 1 to 10 uM by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID775830Inhibition of human recombinant ACE/CD143 somatic form using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2.AcOH as substrate at 10 uM preincubated for 10 mins prior to substrate addition measured for 30 mins by spectrophotometric analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1129776Cell cycle arrest in human Jurkat cells assessed as accumulation at G0/G1-phase at 10 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 4.16%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1578882Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID663372Growth inhibition of human SF268 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1355744In vivo antifungal activity against FLC resistant Candida albicans 0304103 infected in ICR mouse assessed as mouse survival at 5 mg/kg, ip qd up to 20 days in co-treated with 1 mg/kg, ip qd fluconazol (Rvb = 4.5 day)2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID541645Inhibition of human HDAC2 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID373075Inhibition of human recombinant HDAC22009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1273879Inhibition of human CYP3A4 using 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate at 10 uM after 30 mins by fluorimetric analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID613327Antitumor activity against human HCT116 cells xenografted in athymic nude mouse model assessed as tumor growth inhibition at 5 mg/kg, iv2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1614136Inhibition of recombinant full length C-terminal His-tagged human HDAC9 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1865295Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID652759Increase of HDAC7-meidated histone H3 acetylation in human CFBE41o cells at 0.2 to 5 uM by Western blot analysis2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1174688Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID420504Antiproliferative activity against human HCT116 cells after 72 hrs2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1633674Immunomodulatory activity in mouse N9 cells assessed as increase in LPS-induced MRC1 expression at 5 to 25 uM incubated for 24 hrs by Western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1321621Antiproliferative activity against human A549 cells measured after 72 hrs by WST1 assay2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.
AID1433255Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1141766Cytotoxicity against human HSC3 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1406993Inhibition of HDAC6 in human SH-SY5Y cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1476160Antiproliferative activity against human NKYS cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1469300Induction of apoptosis in human NCI-H460 cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.11%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1688033Induction of apoptosis in human HL-60 cells assessed as necrotic cells at 0.5 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 1.01 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1826621Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 3.33 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID524997Inhibition of HDAC7 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1486298Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1126982Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1547354Inhibition of HDAC in human HCT116 cells assessed as induction of autophagy at marginal level by measuring p62 degradation at 10 uM measured after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1462227Inhibition of BRD4/HDAC1 in human OCI-AML2 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID525034In vivo inhibition of HDAC2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1206742Cytotoxicity against human MDA cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1280259Inhibition of human HDAC1 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID723437Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID404445Cytotoxicity against human SU 86.86 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID90340Inhibition of Histone deacetylase (HDAC)of HeLa nuclear extracts2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1398804Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1441668Plasma concentration in mouse by liquid chromatography mass spectrometry2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1885700Toxicity in ICR mouse assessed as effect on ALT level at 12 umol/kg, ip measured after 12 hrs in presence of CDDO-Me2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy.
AID1888421Inhibition of fungal HDAC using Boc-Lys (acetyl)-AMC as substrate preincubated for 12 hrs followed by substrate addition and measured after 6 hrs by fluorescence-based analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID374819Inhibition of wild type His-tagged HDAC5 catalytic domain T678-L1122 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1390810Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
AID527320Growth inhibition of human U937 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
AID750110Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate at 1 uM by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
AID1482142Induction of mitochondrial membrane potential loss in human MOLT4 cells assessed as intact mitochondrial membrane potential at 1 uM measured after 48 hrs by Rh123 dye-based flow cytometric analysis (Rvb = 90.4%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1727742Inhibition of HDAC8 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1464886Oral bioavailability in Sprague-Dawley rat 20 mg/kg administered via gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1578919Inhibition of PI3K/AKT/mTOR signaling in human Bel7402 cells assessed as reduction in mTOR phosphorylation at 5 uM after 24 to 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID476645Antiproliferative activity against human HL60 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1164766Efflux ratio of permeability from apical to basolateral side to basolateral to apical side of human Caco2 cells in presence of digoxin2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1578494Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 0.25 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 9.2 to 9.63 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1422519Inhibition of human recombinant HDAC1 at 2 uM after 15 to 30 mins by COLOR DE LYS-based colorimetric method2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1572341Inhibition of recombinant C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID619139Half life in dog liver microsomes2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID352517Inhibition of human recombinant HDAC32009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1511967Inhibition of full length recombinant FLAG/His-tagged C-terminal human HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
AID1566813Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID313731Inhibition of HDAC32008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1164774Toxicity in human A2780 cells xenografted athymic nude mouse assessed as body weight loss at 100 mg/kg, po qd for 5 days a week for 2 weeks2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1864679Inhibition of full length recombinant human HDAC6 in expressing mouse J774.A1 cells assessed as upregulation of acetylated histone H3 at 1 uM measured after 0.1 to 24 hrs by western blot analysis
AID764218Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1433253Antiproliferative activity against human CMY cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1434356Growth inhibition of human HCT15 cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1566806Inhibition of recombinant full length human HDAC4 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1502986Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged human HDAC1 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1737136Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1434352Inhibition of HDAC in human HeLa cell nuclear extract using acetylated lysine side chain of histone as substrate measured after 30 mins by fluorometric assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1141242Inhibition of pig kidney microsomal APN using L-Leu-p-nitroanilide as substrate preincubated for 5 mins before substrate addition measured after 30 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Design, synthesis and preliminary evaluation of α-sulfonyl γ-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors.
AID1783063Antifungal activity against fluconazole-resistant Candida tropicalis 3890 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1754759Downregulation of HDAC2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID593551Inhibition of human HDAC6 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID541654Inhibition of human HDAC11 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1234898Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1260637Inhibition of human recombinant HDAC1 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1401545Antiproliferative activity against human KM-H2 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1600657Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric m2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID1784989Inhibition of HDAC6 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1848278Inhibition of PI3Kalpha (unknown origin) at 1 uM by mobility shift assay2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID755620Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1518806Inhibition of HDAC1/2/3 in human KMS-12-BM cells assessed as increase in Ac-H3 level at 2.5 to 5 uM incubated for 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1587865Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1449332Inhibition of HDAC6 in human CAL27 cells assessed as accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1861257Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1511140Inhibition of HDAC11 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID461260Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1758462Dark toxicity in human A549 cells assessed as reduction in cell viability incubated under dark for 48 hrs measured after 48 hrs by CCK8 assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1394887Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) after 3 hrs by fluorescence polarization assay2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1599729Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1667069Antiproliferative activity in human A549 cells assessed as inhibition of cell viability after 72 hrs by MTS assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID487873Inhibition of HDAC in human HeLa cells extracts after 60 mins by fluorescence assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
AID1421927Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1849159Selectivity index, ratio of IC50 for inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells to IC50 for inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed 2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1754770Inhibition of HDAC in human MCF7 cells assessed as increase in histone H3 acetylation at 1 to 3 uM incubated for 24 hrs by Western blot analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1548276Antiproliferative activity against bortezomib resistant human KM3/BTZ cells assessed combination index in presence of bortezomib at 1:1 compound to bortezomib ratio incubated for 48 hrs by MTT assay
AID1281866Induction of apoptosis in human RPMI8226 cells assessed as dead cells at 3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2%)2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1469437Inhibition of HDAC1 in human Hep3B cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot method2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1821344Toxicity in mouse xenografted with human HepG2 cells assessed as liver edema at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1543960Induction of apoptosis in human Bel7402/5-FU cells assessed as live cells at 5.0 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 93.12%)2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1676588Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1785338Inhibition of HDAC7 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID1225983Inhibition of recombinant C-terminal His-tagged full length human HDAC3/NcoR2 complex expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1361650Induction of apoptosis in human A549 cells assessed as necrotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID663374Growth inhibition of human SF539 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID292436Inhibition of HDAC in HeLa cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
AID1356280Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1263145Inhibition of human recombinant HDAC6 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1441680Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as LTB4 level at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 (Rvb = 139.23 pg/ml)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1355707Antifungal activity against FLC resistant Candida albicans 0304103 after 48 hrs in presence of fluconazol by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID663393Growth inhibition of human UO31 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1514601Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H3 levels at 5 uM by Western blot analysis relative to beta-actin (Rvb = 0.5 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID652763Inhibition of HDAC6 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID350732Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1201653Antiproliferative activity against human OVCAR5 cells assessed as growth inhibition after 48 hrs by SRB assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1816195Inhibition of HDAC in human BT-549 cells assessed as increase in level of acetyl alpha tubulin substrate at 3 uM incubated for 12 hrs by chemiluminescence based Western blotting analysis
AID1819549Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as fold increase in downregulation of CD200R expression in spleen by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1915578Inhibition of VEGFR2 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID71776Tested in vivo for the inhibition of proliferation of friend leukemic cells2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID482967Volume of distribution at steady state in mouse at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID527042Cytotoxicity against human NCI-H460 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1897506Antiangiogenic activity against BALB/c mouse xenografted with human HCT-116 cells assessed as downregulation of CD31 expression in tumor at 30 mg/kg/day, po administered for 18 days by immunohistochemical staining based analysis
AID593552Inhibition of human HDAC7 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1754778Downregulation of NFkB1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1890438Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID1273872Inhibition of HDAC6 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1487016Inhibition of HDAC2 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1482141Induction of mitochondrial membrane potential loss in human MOLT4 cells at 1 uM measured after 48 hrs by Rh123 dye-based flow cytometric analysis (Rvb = 9.6%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID541655Growth inhibition of human H460 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID273179Induction of apoptosis in U937 cells at 5 uM by AnnexinV/PI double staining2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1901173Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM treated for 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1917531Selectivity index, ratio IC50 for inhibition of HDAC6 (unknown origin) to IC50 for inhibition of HDAC1 (unknown origin)2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID780576Growth inhibition of human MCF7 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
AID411255Selectivity for ratio of IC50 for human HDAC8 to IC50 for human HDAC1/2 by fluorimetric assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID663345Growth inhibition of human HL-60(TB) cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1361652Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1572357Induction of apoptosis in human MDA-MB-231 cells at 1 to 10 uM after 48 hrs by propidium iodide-staining based FACS analysis2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1898526Cytotoxicity against human L02 cells assessed as reduction in cell viability at 32 uM incubated for 48 hrs by MTT assay relative to control2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer.
AID1363818Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID1630597Inhibition of recombinant full length C-terminal FLAG-tagged/C-terminal His-tagged human HDAC1 using fluorogenic substrate at 10 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID310123Inhibition of HDAC2 in HeLa cell lysates2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.
AID1415671Half life in rat liver microsomes at 5 uM in presence of NADPH by LC-MS analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1863440Inhibition of HDAC8 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID241474Inhibitory concentration against maize histone deacetylase 22005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID723426Potentiation of 5 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.25 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1177054Antiprotozoan activity against Giardia lamblia G12015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1886185Inhibition of HDAC3 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1487014Inhibition of HDAC6 in human U937 cells assessed as increase in acetylated-alpha-tubulin level at 5 uM incubated for 18 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1759727Inhibition of class 1 HDAC in human Jurkat 2C4 model of HIV latency assessed as reactivation of HIV latency incubated for 18 to 24 hrs in presence of 5% heat inactivated NHS by Steady-Glo luciferase assay2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
AID1403156Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID723123Potentiation of 8 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID240810Inhibitory concentration against human histone deacetylase2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1421909Selectivity index, ratio of IC50 for human HepG2A16 cells to IC50 for drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID708770Inhibition of HDAC in human HeLa cells nuclear extracts by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID1126986Inhibition of HDAC1 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID525010Inhibition of HDAC7 in human CFBE41o- cell line assessed as increase in Fdelta508 CFTR protein trafficking at 1 uM every 24 hrs by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1415652Inhibition of HDAC4 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1653139Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability by SRB assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1280279Inhibition of class1 HDAC in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1433250Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID371222Cytotoxicity against human HCT116 cells2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Alpha-mercaptoketone based histone deacetylase inhibitors.
AID473175Induction of HDAC-mediated histone acetylation in human Caco-2 cells at 5 uM after 6 hrs by indirect ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1233250Inhibition of human recombinant HDAC1 after 15 mins by fluorogenic assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID1783070Antifungal activity against fluconazole-sensitive Candida albicans 9770 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1897404Induction of apoptosis in human SNU-16 cells assessed as live cells at 1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 90.92%)
AID320398Induction of tubulin hyperacetylation in human MCF7 cells at 10 uM by Western blot2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode.
AID1667088Inhibition of STAT3 in human MDA-MB-231 cells assessed as slight down regulation of pSTAT3 expression at 50 to 100 uM after 24 hrs by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1543972Induction of autophagy in human Bel7402/5-FU cells assessed as up regulation of LC3-2 levels at 5.0 uM incubated for 72 hrs by Western blot assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID310183Growth inhibition of human NUGC3 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID717805Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1855254Antiproliferative activity against human HCT-116 cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID759303Inhibition of human recombinant HDAC8 after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID725669Inhibition of C-terminal His-tagged full length human recombinant HDAC2 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
AID482952Antiproliferative activity against human A2780 cells2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1404301Antiproliferative activity against human NCI-H460 cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1754756Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID446348Hepatic blood flow in mouse2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID1816214Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 2.5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.8%)
AID1173507Inhibition of full length N-terminal GST-tagged human HDAC11 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1371051Antilieshmanial activity against promastigote stage of Leishmania donovani by fluorimetric assay2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1709368Induction of apoptosis in human NAMALVA cells assessed as necrotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 1.05%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1785334Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells measured after 30 mins by fluorescence microplate reader ass
AID327541Inhibition of human HDAC in HeLa cells at 1 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID90839Inhibition of Histone deacetylase 8 (HDAC8) of HeLa nuclear extracts2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID499799Inhibition of HDAC in human HeLa cell nuclear extracts2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1897494Toxicity in BALB/c nude mouse xenografted with human SNU-16 cells assessed as reduction in body weight at 50 mg/kg/day, ip administered for 18 days and measured every 3 days
AID1141784Inhibition of HDAC in human HCT116 cells assessed as increase in alpha-tubulin acetylation after 3 hrs by Western blotting analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1215096Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis relative to rifampicin2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1401903Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1631200Inhibition of HDAC8 (unknown origin) using fluorophore-conjugated substrate by fluorescence assay2016ACS medicinal chemistry letters, Oct-13, Volume: 7, Issue:10
Development of a Potent and Selective HDAC8 Inhibitor.
AID1164907Inhibition of HDAC2 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID663365Growth inhibition of human OVCAR4 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID663366Growth inhibition of human OVCAR5 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1811379Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth measured after 2 days by CCK8 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID723440Potentiation of 1 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1128562Inhibition of human HDAC-10 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1633438Immunomodulatory activity in LPS treated Wistar rat primary microglial cells assessed as decrease in MRC1 expression level at 5 to 50 uM incubated for 24 hrs by western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID308647Antiproliferative activity against human drug-resistant PT45 cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID90345Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1); Potent inhibitor2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
AID1454031Inhibition of recombinant human N-terminal His-tagged BRD4 bromodomain 1 (49 to 170 residues) expressed in Escherichia coli at 100 uM using biotinylated peptide containing acetylated lysine as substrate pretreated for 15 mins followed by substrate additio2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1410362Antitumor activity against mouse LLC cells implanted in immunocompetent C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd administered via gavage for 14 consecutive days measured every 4 days relative to control2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID374830Antiproliferative activity against human MCF7 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1164921Induction of cell differentiation in human BE(2)-C cells assessed as neurite outgrowth at 2 uM by CCK-8 assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1168913Inhibition of HDAC1/HDAC2 in human HeLa cell extract incubated for 5 mins prior to substrate addition measured after 30 mins by microtitre plate reader analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif.
AID1547264Inhibition of HDAC10 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID591330Inhibition of HDAC in human HeLa cells by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.
AID761581Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID258011Inhibition of HDAC in human leukemic CEM cells2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
AID1322159Inhibition of recombinant human full length GST-tagged HDAC8 expressed in Escherichia coli DH5alpha (DE3) assessed as inhibition of deacetylation activity using Fluor-de-Lys as substrate measured after 15 mins by fluorimetric assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of novel HDAC8 inhibitory 2,5-disubstituted-1,3,4-oxadiazoles containing glycine and alanine hybrids with anti cancer activity.
AID1433270Inhibition of HDAC in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1476151Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1275585Inhibition of HDAC in mouse forebrain assessed as acetylation of histone H3K9 at 10 uM after 24 hrs by immunofluorescence-based detection analysis2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
AID1655800Cytotoxicity against human U937 cells assessed as reduction in cell viability at 0.25 uM incubated for 72 hrs by CellTiter-Glo Luminescent cell viability assay relative to control2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID723470Inhibition of HDAC in cisplatin sensitive human CAL27 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1200976Intrinsic clearance in mouse liver microsomes at 1 uM preincubated for 10 mins followed by NADPH addition measured over 30 mins by LC-MS/MS analysis2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID618093Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as body weight loss at 200 mg/kg, po QD for 21 days measured on day 192011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID456797Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID761577Induction of apoptosis in human NB4 cells after 48 hrs by Annexin V test2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID1426425Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID1742224AUC (0 to t) in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID105420Concentration required for the antiproliferation of Human MDA-435 breast carcinoma cells2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).
AID672033Ratio of IC50 for human HDAC2 preincubated for 3 hrs to IC50 for human HDAC2 preincubated for 5 mins2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1600733Antiproliferative activity against human CAL27 cells after 72 hrs by microplate reader based MTT assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1462024Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability.
AID1863175Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID1410326Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1865300Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on liver at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1330924Inhibition of wild-type EGFR (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1467045Effect on renilla recombinant luciferase protein expressed in HEK293 cells at 10 uM after 24 hrs in presence of 10 uM cycloheximide by renilla luciferase reporter gene assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy.
AID1324232Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level at 10 uM measured after 24 hrs relative to control2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID1410324Inhibition of recombinant human GST-tagged IDO1 (1 to 404 residues) using D-Tryptophan as substrate2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID316902Inhibition of human SNB78 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1409642Inhibition of HDAC in human K562 cells using Boc-K(Ac)-AMC as substrate by fluorescence assay2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.
AID1758467Inhibition of human recombinant HDAC3 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID414718Inhibition of human recombinant HDAC6 expressed in HEK293 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1168916Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif.
AID1466057Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID246082Effective Concentration of compound to inhibit the growth of human RXF-631L cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1464879Inhibition of recombinant human ERG expressed in HEK293 cells at -80 mV holding potential measured for 9 mins by Qpatch clamp method2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1769649Inhibition of HDAC2 (unknown origin)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID613114Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Epigenetic profiling of the antitumor natural product psammaplin A and its analogues.
AID1897401Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 0.3 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.02%)
AID1260647Inhibition of human recombinant HDAC11 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1784974Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1816697Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID669763Inhibition of human recombinant HDAC6 after 30 mins by fluorometric assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1361640Inhibition of HDAC6 in human A549 cells assessed as increase in alpha-tubulin acetylation at 2.5 to 5 uM after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1399810Solubility in PG/EtOH (96%) at 30 mg/mL after 24 hrs by UV-spectrometric method2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
AID723456Potentiation of cisplatin-induced toxicity in cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1861306Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at G2/M phase measured by flow cytometry analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1279125Inhibition of C-terminal GST-tagged human recombinant HDAC2 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID476652Toxicity in FVB mouse assessed as effect on number of platelets at 50 mg/kg, po administered 5 times per week for 2 weeks (Rvb = 514 +/- 42.8 10^3/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1600732Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1355729Toxicity in BALB/C nude mouse xenografted with human HEL cells at 10 mg/kg, ip bid treated for 21 consecutive days2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1193537Inhibition of isolated rat liver HDAC using substrate containing acetylated lysine side chain assessed as release of fluorophore at 0.1 uM by Fluor de Lys assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans.
AID737918Inhibition of recombinant HMG-CoA reductase (unknown origin) after 10 mins by spectrophotometric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1235259Cytotoxicity against human K562 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
AID1730857Inhibition of HDAC1 (unknown origin)2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1865241Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1633654Inhibition of human recombinant HDAC6 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID672021Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID331899Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID1225976Cytotoxicity against HLF assessed as growth inhibition after 72 hrs by MTT assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1401377Inhibition of HDAC1 in human HeLa-S3 cell lysates assessed as remaining activity at 1 uM preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1449216Inhibition of full length human recombinant C-terminal His-tagged HDAC3/NcoR2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID613122Inhibition of HDAC1 in human U937 cells assessed as up-regulation of p21 / WAF1 at 5 uM after 24 hrs by Western blot analysis2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Epigenetic profiling of the antitumor natural product psammaplin A and its analogues.
AID1493593Inhibition of human recombinant full-length C-terminal GST-tagged HDAC3 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID622257Inhibition of HDAC6 after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1451848Antitumor activity against human HCT116 cells xenografted in BALB/C nude mouse assessed as tumor growth inhibition at 25 mg/kg, ip bid administered for 21 consecutive days measured after 30 to 33 days post implantation relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1783110Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.
AID1486306Antiproliferative activity against human Raji cells after 3 days by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1511157Inhibition of HDAC in human HL60 cells assessed as increase in acetylation of H3 at 0.08 to 1.6 uM incubated for 24 hrs by western blot analysis2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1811367Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 6 days by WST8 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID1061949Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1622973Inhibition of HDAC4 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1897382Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID1614122Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
AID1832685Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1415640Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1326509Inhibition of C-terminal His/FLAG-tagged full length recombinant human HDAC1 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1459954Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1888405Synergistic antifungal activity against azole-resistant Candida albicans 0304103 assessed as fractional inhibitory concentration in presence of fluconazole incubated for 48 hrs by CLSI based checkerboard microdilution assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID1764250Antiproliferative activity against human CAL-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1275646Growth inhibition of human Aspc-1 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1441684Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta mRNA level in BALF compound administered intraperitoneally once daily for 7 days post BLM challenge measured on day 7 by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1487043Inhibition of HDAC in human HeLa-S3 cells lysates assessed as remaining enzyme activity at 2.5 x 10'-8 M pre-incubated for 15 mins before HDAC-Glo I/II substrate addition and measured after 30 mins post substrate addition2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1650413Inhibition of HDAC in human A2780 cells2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID1821966Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
AID1250640Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID669758Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1720109Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID1808542Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 cells measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID723155Potentiation of 1 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1181305Inhibition of human recombinant HDAC6 pre-incubated at room temperature for 15 min before substrate addition by fluorimetric assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID544094Cytotoxicity against mouse RAW264.7 cells by MTT assay2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1478588Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 4.78%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1677511Inhibition of HDAC2 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID618020Antitumor activity against human HCT116 cells xenografted in BALB/c nu mouse assessed as tumor growth inhibition at 90 mg/kg, po qd for 19 days relative to control2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1855242Inhibition of HDAC1/HDAC2 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate and measured by fluorometric method2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID489912Cytotoxicity against human NCI-H460 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
AID663396Growth inhibition of human Hs 578T cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1361648Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1389949Inhibition of human recombinant LSD1/CoREST3 expressed in Escherichia coli using monomethylatedH3meK4 peptide as substrate preincubated for 15 mins followed by substrate addition measured after 12 mins by fluorescence based assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1855247Binding affinity to calf thymus DNA at 50 uM incubated for 30 mins and measured by fluorescence spectroscopy2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID421213Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation at 5 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID316898Inhibition of HDAC22008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1865264Inhibition of recombinant his-tagged human HDAC8 using Boc-Lys (TFA)-AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1410012Reactivation of latent HIV1 infected in human U1 cells assessed as increase in p24 production after 48 hrs by ELISA relative to vorinostat2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
AID1336937Inhibition of HDAC in human LNCAP cells assessed as down regulation of androgen receptor expression at 10 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1578147Inhibition of HDAC in human K562 nuclear extract2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1065960Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID732152Inhibition of HDAC6 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1848629Cytotoxicity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID404446Cytotoxicity against nontransformed human microvascular epithelial cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID619045Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1652190Inhibition of human recombinant HDAC1 expressed in Escherichia coli BL21(DE3) cells using KL177 as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1550108Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID420500Toxicity in athymic nude Swiss mouse bearing human H460 cells assessed as death administered QD 5 days a week for 2 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1202591Cytotoxicity against human KB cells after 72 hrs by MTS assay2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID1127325Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID449260Inhibition of HDAC1/HDAC2 from human Hela nuclear extracts using [3H]acetylated histone peptide by colorimetry2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors.
AID672031Selectivity ratio of IC50 for human HDAC2 preincubated with compound for 24 hrs to IC50 for human HDAC1 preincubated with compound for 3 hrs2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1753838Inhibition of HDAC2 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID672029Inhibition of human recombinant HDAC8 expressed in Escherichia coli using BML-KI-178 as substrate preincubated with compound for 3 hrs at 10 uM measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1293553Inhibition of HDAC in human HeLa nuclear extract using BOC-Ac-Lys-AMC as substrate incubated for 90 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1367346Antiproliferative activity against human HCT116 cells by MTT assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Synthesis and biological evaluation of Santacruzamate-A based analogues.
AID1598104Activation of non-specific gene expression in human J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as CMV driven gene expression incubated for 48 hr by FACSCalibur flow cytometry2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID503689Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 12 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID605542Antiproliferative activity against human MCR5-SV2 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID717797Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 3.125 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID723143Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1273869Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1689779Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1292165Induction of apoptosis in human HCT116 cells assessed as apoptotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometric analysis2016European journal of medicinal chemistry, Jun-10, Volume: 115Novel spiropyrazolone antitumor scaffold with potent activity: Design, synthesis and structure-activity relationship.
AID1403158Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID628440Inhibition of human recombinant HDAC3/NCoR2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1389958Inhibition of HDAC in human MCF7 cell nuclear extract using acetylated lysine as substrate at 35 uM after 1 hr in presence of tranylcypromine by colorimetric analysis relative to control2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1337290Antiproliferative activity against human KHYG cells after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID274098Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 90% of isolates after 24h.2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID1248353Inhibition of human full length MMP9 using Mca-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate at 10 uM incubated for 2 hrs prior to testing measured for 15 mins by fluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID1321620Antiproliferative activity against human HCT116 cells measured after 72 hrs by WST1 assay2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.
AID1439781Inhibition of human HDAC5 using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by trypsin-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa.
AID246068Effective Concentration of compound to inhibit the growth of human HCT116 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1065968Inhibition of HDAC6 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacYGC as substrate after 60 mins by SAMDI mass spectrometric analysis2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID313735Inhibition of HDAC72008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1321702Inhibition of HDAC3 (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1900912Cytotoxicity against human TMZ-sensitive U251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID1482169Cytotoxicity against human COLO205 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID408886Selectivity for HDAC6 over HDAC12008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1449328Inhibition of human HDAC8 using Z-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1572381Antiproliferative activity against human THP1 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID488274Inhibition of HDAC22010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID655475Restoration of CFTR deltaF508 mutant trafficking to cell surface as glycoforms in human CFBE41o cells at 5 uM after 24 hrs by Western blotting2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID274072Clearance after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1401478Selectivity ratio of IC50 for HDAC2 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1622982Cytotoxicity against human RWPE1 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1441702Inhibition of LTA4H in C57BL/6 mouse assessed as reduction in LTB4 production pre-incubated for 30 mins before 5-(methylamino)-2-({(2R,3R,6S,8S,9R,11R)-3,9,11-trimethyl-8-[(1S)-1-methyl-2-oxo-2-(1H-pyrrol-2-yl)ethyl]-1,7-dioxaspiro[5.5]undec-2-yl}methyl)-2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID586614Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID352748Inhibition of C-terminal FLAG tagged HDAC32009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1487047Inhibition of HDAC6 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1819534Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as liver damage at 60 mg/kg, IG administered for 12 days H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1785351Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
AID1384208Inhibition of HDAC3 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID723136Potentiation of 10 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.25 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1623531Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate-3 by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID352753Antiproliferative activity against human A549 cells after 72 hrs by celltiter-blue cell viability assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1572360Inhibition of human HDAC6 in human T24 cells assessed as up-regulation of GRP78 by measuring volume intensity at 10 uM after 48 hrs by Western blot analysis relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1702142Inhibition of PI3K/AKT/mTOR signaling in human HepG2 cells assessed as reduction in EGF-stimulated phosphorylation of Akt at S473 residue incubated for 3 hrs followed by stimulation with 50 ng/ml growth factor EGF for 15 mins by by ELISA2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1566819Antiproliferative activity against human ARD cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1848565Ratio of IC50 for cytotoxicity against human WI-38 cells to IC50 for cytotoxicity against human NCI-H5222022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1689812Antiproliferative activity against human H460 cells assessed as inhibition of cell growth at 2 uM measured after 72 hrs by CCK-8 assay relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1174692Inhibition of HDAC1 (unknown origin)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID297485Cytotoxicity against human non-proliferating RKOp21 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1233267Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID353353Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
AID1826629Synergistic antiproliferative effect on HEL cells assessed as combination index at 3.33 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID328805Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1337195Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1758469Inhibition of human recombinant HDAC8 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1441686Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta level in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1578889Inhibition of human HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID527045Cytotoxicity against human H441 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1578503Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 2 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 9.2 to 9.63 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1649505Antileishmanial activity against Leishmania infantum MON-1 intracellular amastigotes infected in Swiss mouse BMDM measured after 48 hrs by Giemsa staining based optical microscopic analysis2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
AID1753635Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-based assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1886237Antivascular activity against HUVEC cells assessed as inhibition of capillary-like tubule formation at 1 uM measured after 6 hrs by inverted microscopy2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1677494Antiproliferative activity against siRNA-induced BAX knock down human HeLa cells after 48 hrs by MTT assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID324948Inhibition of HDAC1 in HEK293 cells2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1227049Cytotoxicity against human Jurkat cells assessed as cell proliferation after 70 hrs by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1754782Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1/S phase at 1 uM incubated for 4 hrs by PI staining based flow cytometric analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1783093Inhibition of HDAC in Cryptococcus neoformans H99 using Boc-Lys(Ac)-AMC as substrate preincubated with protoplast for 12 hrs followed by incubation with substrate for 6 hrs by fluorimetric assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID252895Concentration required to inhibit growth of human LNCaP prostate cancer cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.
AID1126996Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 1 uM after 24 hrs by flow cytometry analysis (Rvb = 96.24%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1882456Inhibition of HDAC1 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1065638Inhibition of human recombinant HDAC4 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1410325Inhibition of recombinant human GST-tagged IDO1 (1 to 404 residues) at 1 uM using D-Tryptophan as substrate relative to control2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1336923Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1545988Antiproliferative activity against human Aspc-1 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1614135Inhibition of recombinant full length N-terminal GST-tagged human HDAC7 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1383987Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID772655Inhibition of full length FLAG-tagged recombinant HDAC1 (unknown origin) transfected in human HeLa cells assessed as deacetylation of [3H]-acetylated histones after 2 hrs by scintillation counting analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.
AID723730Cytotoxicity against human A2780 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1349725Inhibition of recombinant human N-terminal GST-tagged HDAC4 (612 to end residues) expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1434358Growth inhibition of human NUGC3 cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1482129Cytotoxicity against human MCF10A cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1686352Drug metabolism in human liver microsomes assessed as o-glucuronidated metabolite formation in presence of UDP glucuronic acid incubated for 12 hrs at 37 degC by electrospray ionization liquid chromatography mass spectrometry2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
AID1690834Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluoresc2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1386691Inhibition of HDAC in human GM18453 cells harboring NPC1 mutant assessed as increase in 250 kDa NPC1 protein expression at 5 uM pretreated for 48 hrs followed by PNGaseF addition and measured after overnight incubation by Western blot analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1225981Inhibition of recombinant C-terminal His-tagged full length human HDAC8 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC class 2a substrate after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1558003Inhibition of HDAC6 CD2 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
AID496803Inhibition of human HDAC32010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1812443Inhibition of human recombinant HDAC2 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID781050Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID1548891Induction of apoptosis in human MV4-11 cells harboring wild type p53/FLT3-ITD mutant assessed as cleavage of pro-caspase 3 at 5000 nM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID481556Cytotoxicity against human KB cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID420635Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 4 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID546562Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1576467Induction of apoptosis in human A549 cells assessed as necrotic cells at 5 uM after 72 hrs by Annexin V-phycoerythrin/7-AAD staining based flow cytometric analysis (Rvb = 0.45%)
AID1614194Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 uM after 48 hrs in presence of 0.3 uM RAPA by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 10.7%)
AID525003Inhibition of HDAC1 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1832798Cytotoxicity against human MOLT-4 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID1543933Antiproliferative activity against human H1299 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1543969Induction of autophagy in human Bel7402/5-FU cells assessed as increase in red fluorescence at 5.0 uM incubated for 72 hrs by acridine orange staining based fluorescence microscopy2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID723137Potentiation of 3.16 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1730851Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1174693Inhibition of HDAC2 (unknown origin)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1737657Cytotoxicity against human THP-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID1863176Selectivity index, ratio of IC50 for HDAC7 (unknown origin) to IC50 for HDAC6 (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID1451820Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1441709Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as TGF-beta1 level at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 14 by by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1764254Inhibition of recombinant human C-terminal His-fusion tagged/N-terminal Strep2 tagged HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by 2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID473189Growth inhibition of human BJ cells at 0.05 to 100 uM after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1487003Inhibition of HDAC8 (unknown origin) by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1227031Inhibition of human recombinant HDAC3 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1401540Antiproliferative activity against human Maver2 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1434354Growth inhibition of human MDA-MB-231 cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID352747Inhibition of C-terminal FLAG tagged HDAC22009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1441685Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 mRNA level in BALF compound administered intraperitoneally once daily for 7 days post BLM challenge measured on day 7 by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1469385Induction of apoptosis in human HepG2 cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.32%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID316886Antiproliferative activity against human SKBR3 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID482944Inhibition of HDAC42010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1281851Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1898525Cytotoxicity against human MCF-10 A cells assessed as reduction in cell viability at 32 uM incubated for 48 hrs by MTT assay relative to control2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer.
AID465153Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID723429Potentiation of 0.75 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 0.5 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1785336Inhibition of HDAC5 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID1227022Binding affinity to human HDAC8 C153A mutant assessed as loss of activity at 2 to 8 uM by Fluor-de-Lys activity assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1882467Inhibition of HDAC8 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID580940Antitumor activity against human HCT116 cells xenografted in athymic nude mouse assessed as decrease in tumor volume at 50 mg/kg, iv administered once daily for 5 days per week by caliper measurement2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Antiproliferative and differentiating activities of a novel series of histone deacetylase inhibitors.
AID1720098Growth inhibition of human THP-1 cells2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID1373249Inhibition of HDAC8 (unknown origin) at 1 uM preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
AID760008Downregulation of Gli1 mRNA expression in human DaOY cells at 2.5 uM relative to DMSO-treated control2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere.
AID1406978Inhibition of class 1 HDAC in human NB4 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1774969Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate at 10 uM preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors.
AID258010Inhibition of HDAC in rat liver homogenate2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
AID1821962Selectivity index, ratio of IC50 for inhibition of recombinant human N-terminal GST tagged HDAC6 expressed in baculovirus infected Sf9 insect cells to IC50 for inhibition of recombinant human His-tagged HDAC3 expressed in baculovirus insect cells
AID1280266Inhibition of HDAC6 in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 10 uM for 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1303627Potentiation of 0.025 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.125 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1469397Induction of apoptosis in human Hep3B cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.97%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1155321Cytotoxicity against erythrocytes (unknown origin)2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1203890Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1677514Binding affinity to full length His-tagged Mcl1 (unknown origin) preincubated for 30 min followed by 5-FAM Bid-BH3 addition and measured after 20 mins by fluorescence polarization assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID760499Cytotoxicity against human KM12 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1339585Growth inhibition of human Jurkat cells after 44 hrs by MTT assay2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID525016Inhibition of HDAC in human CFBE41o- cell line assessed as hyperacetylation of histone H3 at 5 uM after 8 hrs by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1282299Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID618097Toxicity in athymic nu/nu Harlan mouse xenografted with human HCT116 cells assessed as mouse survival at 200 mg/kg, po QD for 21 days measured on day 222011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1379286Inhibition of recombinant human His-tagged c-Met cytoplasmic domain (956 to 1390 residues) expressed in baculovirus expression system using poly (Glu,Tyr)4:1 as substrate after 60 mins by spectrophotometric analysis2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
AID1383994Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1754810Upregulation of SIRT4 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID594125Inhibition of full length HDAC8 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Discovery of histone deacetylase 8 selective inhibitors.
AID1206750Induction of apoptosis in human HEL cells at 0.5 to 2 uM after 24 hrs by 7-AAD-annexin-V/propidium iodide staining-based flow cytometric analysis2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1688028Induction of apoptosis in human HL-60 cells assessed as increase in accumulation at sub-G1 phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2.72 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID525031Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1066162Antimigratory activity against human HCT116 cells at 50 uM after 72 hrs2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
AID1178600Inhibition of human HDAC9 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1348913Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1404299Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID348392Antiproliferative activity against human NB4 cells after 48 hrs2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents.
AID619044Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1652194Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1511128Induction of apoptosis in human in human HL60 cells at 0.25 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometric analysis2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID670517Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.
AID723122Potentiation of 8 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1275245Inhibition of VEGFR2 (unknown origin) preincubated for 5 mins followed by addition of ATP/gastrin precursor(Tyr87) biotinylated peptide cocktail incubated for 30 mins by ELISA2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.
AID1742757In vivo inhibition of HDAC in tumor of human MDA-MB-231 cells xenografted in BALB/c mouse assessed as increase in acetylated alpha-tubulin expression by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1155331Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for asexual blood stage of Plasmodium falciparum 3D72014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID90353Inhibitory concentration against human histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID747264Growth inhibition of human BGC823 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID732142Inhibition of HDAC9 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID762187Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.
AID1784971Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID760507Inhibition of HDAC6 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1273871Inhibition of HDAC3 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1742630Inhibition of STAT3 in human MDA-MB-231 cells assessed as reduction in STAT-3 phosphorylation at 2.5 to 40 uM incubated for 8 hrs by Western blot analysis2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1399544Inhibition of recombinant human HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID1572356Antiproliferative activity against human T24 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1650419Inhibition of class 1 histone deacetylase in human CAL27 cells assessed as increase in H3 histone acetylation at 3 uM incubated for 24 hrs by immunoblot analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID1433256Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID723149Potentiation of 8 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1.5 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1449215Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID1653140Cytotoxicity against human U251 cells assessed as reduction in cell viability by SRB assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1855243Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC or Boc-Lys(triflouroacetyl)-AMC as substrate incubated for 30 mins and measured by fluorescence assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1467237Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured within 30 mins by fluorometr2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1293564Inhibition of human recombinant C-terminal His-tagged, N-terminal GST-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1650414Cytotoxicity against human A2780 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID619043Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID663362Growth inhibition of human SW620 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1280261Inhibition of human HDAC8 using Z-L-Lys(eta-trifluoroacetyl)-AMC as substrate after 90 mins by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1722282Inhibition of human recombinant HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate incubated for 24 hrs measured after 30 mins by microplate reader based spectrophotometric analysis2020Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
AID1890308Inhibition of recombinant human HDAC6 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1321712Inhibition of HDAC in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 50 nM after 2 hrs by AlphaLisa assay relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID527318Growth inhibition of human HCT116 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
AID748106Inhibition of HDAC8 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1873420Inhibition of HDAC1 (unknown origin) at 1 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID652752Inhibition of recombinant human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID717794Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 2.5 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1462218Inhibition of human BRD4 bromo domain 2 at 5 uM2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID603545Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC6 in human HeLa cell nuclear extracts2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID717796Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1688045Upregulation of acetylated alpha-tubulin level in human HL-60 cells at 2 uM measured after 12 hrs by Western blot analysis2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1915567Cytotoxicity against human RWPE-1 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID525013Inhibition of HDAC7 expressed in hamster BHK cell line assessed as increase in plasma membrane Fdelta508 CFTR protein at 5 uM by immunofluorescence method2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID628288Antiproliferative activity against human HepG2 cells after 24 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID748113Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1597940Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID414750Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1754765Downregulation of HDAC6 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1469301Induction of apoptosis in human NCI-H460 cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 97.3%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1597933Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID670516Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.
AID1384206Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1688040Induction of apoptosis in human HL-60 cells assessed as late apoptotic cells at 2 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 7.24 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID525033Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1337254Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1129782Cell cycle arrest in human Jurkat cells assessed as accumulation at S-phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 20.90%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1174686Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1848302Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.95%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID663387Growth inhibition of human 786-0 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1689772Antiproliferative activity against human H460 cells assessed as inhibition of cell growth at 8 uM measured after 72 hrs by CCK-8 assay relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1742225AUC (0 to infinity) in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1476183Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells at 10 uM using RHKKAc as substrate in presence of ATP2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1784185Inhibition of Schistosoma mansoni HDAC8 using Fluor de Lys as substrate incubated for 90 mins by fluorescence method2021European journal of medicinal chemistry, Dec-05, Volume: 225Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.
AID1915601Cytotoxicity against human SMMC-7721 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID760510Inhibition of HDAC3 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID737911Cytotoxicity against human A549 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1399811Solubility in pH 7.4 phosphate buffer solution at 100 uM after 24 hrs by HPLC method2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
AID1482097Inhibition of HDAC 1 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1676596Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1547346Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in STAT3 phosphorylation at 10 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID619047Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID256473Selectivity for class I (HD1B) against class II (HD1A) histone deacetylases2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
AID274101Inhibition of maize HD2 (mean)2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID328808Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1403170Antimigratory activity in human HepG2 cells at 1 uM after 24 hrs by wound-healing assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1753839Inhibition of HDAC3 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1398821Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CCND1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1816202Antiproliferative activity against human CAL-51 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
AID1655888Inhibition of HDAC in human U937 cells assessed as Ac-H3 level at 0.5 uM incubated for 96 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1127005Induction of apoptosis in human U937 cells assessed as late apoptotic cells using annexin-V/propidium iodide staining at 0.25 uM after 24 hrs by flow cytometry analysis (Rvb = 2.13%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID764216Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID385230Inhibition of HDAC62008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
AID374828Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID626564Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 10 uM by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
AID747259Growth inhibition of human A431 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1547272Inhibition of HDAC6 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1467239Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 0.2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured after 30 mins by fluoromet2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1622929Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1235111Cytotoxicity against mouse B16 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1361632Inhibition of HDAC2 (unknown origin) after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1486297Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1873424Inhibition of HDAC in human MV4-11 cells assessed as histone H3 acetylation preincubated for 3 hrs followed by compound washout and measured within 30 mins by Western blot analysis2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID764647Inhibition of HDAC1/HDAC3/HDAC5/HDAC8 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate incubated for 5 mins prior to substrate measured after 30 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Novel β-dicarbonyl derivatives as inhibitors of aminopeptidase N (APN).
AID1886186Inhibition of HDAC6 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID95277Compound was tested for anti-proliferative activity in Jurkat human leukemia cell line2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1282257Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1422495Cytotoxicity against mouse FL5.12 cells assessed as vacuole formation at 10 uM after 3 hrs by fluorescence microscopic analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1441699Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1775545Inhibition of HDAC1 (unknown origin)2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1633653Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1655793Inhibition of human recombinant HDAC8 using AMC-K(Ac)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID473179Induction of HDAC-mediated histone acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1256442Inhibition VEGFR2 (unknown origin) for 30 mins by ELISA2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.
AID1441648Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta mRNA level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1821347Toxicity in mouse xenografted with human HepG2 cells assessed as necrosis in heart at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1308510Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
AID1737148Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 10 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 4.01%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID350718Inhibition of human recombinant HDAC8 by fluorimetry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1275642Growth inhibition of human HT-29 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1280271Inhibition of class1 HDAC in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 0.1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID765211Cytotoxicity against human A2780C/P cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID1164776Stability of the compound in aqueous solution at pH 7.4 after 24 hrs2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1280282Selectivity index, ratio of HDAC6 inhibition in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 1 uM over class1 HDAC inhibition in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 1 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1566820Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1281848Inhibition of full length His6-tagged GST-fused recombinant human HDAC3 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID663333Growth inhibition of human HepG2 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1548286Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID1863168Inhibition of HDAC7 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID663475Efflux ratio, ratio of apparent permeability from basolateral to apical side over apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID352520Inhibition of human recombinant HDAC102009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1482166Cytotoxicity against human THP1 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID420320Binding affinity to Bordetella / Alcaligenes strain FB188 HDAC by FRET assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1785344Inhibition of full length human CDK2 (1 to 298 end residues)/N-terminal GST-tagged CyclinA2 (1 to 432 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay
AID239792Selectivity for class I HDACs as ratio of IC50 for maize histone deacetylase 1-A and 1-B2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID1897397Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 0.1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.02%)
AID1127324Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1164191Inhibition of HDAC6 in human U937 cells assessed as hyperacetylation of tubulin at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1164909Inhibition of HDAC4 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1754771Inhibition of HDAC in human MCF7 cells assessed as increase in histone H4 acetylation at 1 to 3 uM incubated for 24 hrs by Western blot analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1917541Inhibition of HDAC8 (unknown origin) measured by fluorescence based assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID1469311Induction of apoptosis in human T47D cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 6.16%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID420634Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 4 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID246077Effective Concentration of compound to inhibit the growth of human SK-OV-3 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1572355Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1826601Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1451831Inhibition of human recombinant HDAC3/GST tagged NCOR1 (397 to 503 residues) expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1739581Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated tubulin/GAPDH at 0.1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1826598Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1856988Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by substrate addition and measured after 30 mins by multimode microplate reader analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID663381Growth inhibition of human MDA-MB-435 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1515910Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1704067Inhibition of c-MET(unknown origin) using FAM labelled peptide substrate preincubated for 10 mins followed by substrate addition and measured by microplate reader method2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID1784976Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1576456Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID1205628Growth inhibition of human MDA-MB-231 cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1251321Growth inhibition of human NB4 cells after 72 hrs2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1600729Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins me2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1355713Antifungal activity against FLC resistant Candida albicans 0710922 after 48 hrs in presence of fluconazol by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1751992Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1206752Cell cycle arrest in human HEL cells assessed as accumulation at G2 phase at 0.5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.28%)2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1476149Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1525780Inhibition of HADC8 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID274018Half life after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1659653Antiproliferative activity against human MOLT4 cells incubated for 24 hrs by CCK8 assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID316944Inhibition of mouse SC9 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID753165Cytotoxicity against human HCT116 cells2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID628285Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1893824Inhibition of HDAC in human HeLa nuclear extract measured after 30 mins by fluorescence based assay2021European journal of medicinal chemistry, Jan-15, Volume: 2102-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.
AID322416Cell cycle arrest in human LNCap cells assessed as accumulation at G1 phase relative to control at 1 uM2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID723150Potentiation of 8 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID659493Inhibition of HDAC1 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1478584Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 4.78%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1503841Inhibition of recombinant human full length HDAC6 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluoresce2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
AID1742741Genotoxicity in Salmonella typhimurium TA98 by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1485126Cell cycle arrest in human U373 cells assessed as accumulation at sub-G1 phase at 2 uM after 24 to 48 hrs by propidium iodide staining-based flow cytometry2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1821343Toxicity in mouse xenografted with human HepG2 cells assessed as lung edema at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1206739Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1688035Induction of apoptosis in human HL-60 cells assessed as early apoptotic cells at 1 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 2.46 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID348792Inhibition of human recombinant C-terminally flag tagged HDAC12008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID1280267Inhibition of HDAC6 in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1486300Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1784988Inhibition of HDAC8 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1816711Inhibition of HDAC8 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID748985Inhibition of HDAC3 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1857036Antitumor activity against human MV4-11 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ip administered for 20 days by vernier caliper analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1168914Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif.
AID1600731Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins mea2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1821349Toxicity in mouse xenografted with human HepG2 cells assessed as necrosis in liver at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID327544Increase in p21waf1 re-expression in human HCT116 cells at 10 uM after 24 hrs relative to control2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID619192Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID84278Concentration required for the antiproliferation of Human HT1080 fibrosarcoma cells2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).
AID1600658Inhibition of recombinant human full length C-terminal Flag-tagged HDAC2 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID1234892Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin)2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1282245Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1677493Cytotoxicity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID308652Increase in p27kip1 gene expression in PANC1 cells after 48 hrs relative to control2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID619161Oral bioavailability in nude BALB/c mouse at 50 mg/kg2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1206740Cytotoxicity against human U937 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1848626Cytotoxicity against human 786-0 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1897469Inhibition of HDAC in human HCT-116 cells assessed as reduction in phosphorylated STAT3 level at 0.11 to 1 uM incubated for 36 hrs by Western blot analysis
AID1545831Antiproliferative activity against human HepG2 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1282230Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID473180Induction of HDAC-mediated histone hyperacetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1266085Inhibition of human HDAC in HeLa cells nuclear extract at 12.5 uM by fluorimetric assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID723462Inhibition of human HDAC6 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID328799Inhibition of HDAC6 at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1826628Synergistic antiproliferative effect on HEL cells assessed as combination index at 10 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1418669Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent at 10 to 100 uM preincubated for 10 mins followed by AAPH addition and measured every minute for 120 mins by ORAC-FL assay2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID1439349Inhibition of full length recombinant human GST fused His6-tagged HDAC3 expressed in baculovirus infected High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate measured after 24 hrs2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID1597938Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID605535Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1775566Inhibition of full length human N-terminal GST-tagged HDAC6 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1702065Inhibition of recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID374821Inhibition of wild type His-tagged HDAC7 catalytic domain T515-L952 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1201648Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1126992Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 1 uM after 12 hrs by flow cytometry analysis (Rvb = 96.42%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1599792Inhibition of HDAC6 in human A549 cells assessed as upregulation of p21 mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID538413Selectivity index, ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC62010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1775563Inhibition of full length human C-terminal His-tagged/C-terminal Flag-tagged HDAC1 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID274067AUC after i.p. dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID545853Inhibition of HDAC in Plasmodium falciparum 3D7 by fluorescent activity assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1861256Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1065967Inhibition of HDAC8 catalytic domain (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID476827Toxicity in FVB mouse assessed as effect on number of RBC at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test (Rvb = 8.1 +/- 0.2 10^6/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1441692Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as TGF-beta1 level at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 by ELISA (Rvb = 75.39 pg/ml)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1434359Inhibition of HDAC in HEK293 cells assessed as myc-tagged RUNX3 acetylation by measuring ratio of acetylated-RUNX3 level to beta-actin level at 1 uM measured after 24 hrs by Western blot analysis relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1764799Inhibition of recombinant human HDAC6 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1851614Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1401371Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 2.5 x 10'-8 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1431818Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID605536Antiproliferative activity against human A549 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID732153Inhibition of HDAC4 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1864680Inhibition of full length recombinant human HDAC6 expressing in mouse J774.A1 cells assessed as upregulation of acetylated histone H4 at 1 uM measured after 0.1 to 24 hrs by western blot analysis
AID1900934Toxicity in mouse bearing intracranial tumor assessed as last day of survival at 25 mg/kg, ip in presence of clorgyline for 10 days (Rvb=16 days)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID476643Antiproliferative activity against human U937 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1623538Selectivity index, ratio of IC50 for human recombinant HDAC11 to IC50 for human recombinant HDAC62019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1833061Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID1518787Antiproliferative activity against human MOLM14 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID274032Inhibition of HCT116 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID488276Inhibition of HDAC62010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1401544Antiproliferative activity against human L428 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1449329Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 expressed in insect cells using Boc-K(Ac)-AMC as substrate by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID411253Inhibition of HDAC1/2 from human HeLa cells nuclear extract by cell free fluorimetric assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1888582Inhibition of recombinant HDAC6 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay
AID420652Toxicity in athymic nude Swiss mouse bearing human H460 cells assessed as body weight loss at 100 mg/kg, po QD administered 5 days a week for 2 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1535346Growth inhibition of human U266 cells after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.
AID1915585Inhibition of HDAC3 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1614137Inhibition of recombinant full length N-terminal GST-tagged human HDAC11 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID723455Potentiation of cisplatin-induced toxicity in cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1566808Inhibition of recombinant N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1785348Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
AID1816184Inhibition of HDAC6 (unknown origin) incubated for 60 mins by microplate reader analysis
AID669762Inhibition of human recombinant HDAC2 after 30 mins by fluorometric assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1545761Inhibition of HDAC in human K562 cell extracts using (QSY-7)-RGGRGLGK(Ac)-GGARRHRK(TAMRA)NH2 as substrate preincubated for 30 mins followed by addition of endoproteinase Lys-C and measured after 2 hrs by fluorescence assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Indole: A privileged scaffold for the design of anti-cancer agents.
AID1890351Antitumor immunity in C57BL/6 mouse xenografted with mouse CT26 cells assessed as increase in CD3+ cytotoxic T cells at 50 mg/kg, po administered once daily for 21 days measured by flow cytometry analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1861654Inhibition of HDAC2 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1515882Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 500 nM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.33%)2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1898938Induction of DNA damage in human A2780 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID631668Inhibition of human recombinant full-length HDAC3 using fluorophore conjugated substrate by fluorescence assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).
AID1697198Cytotoxicity against human PC3 cells by colorimetric method2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID395034Antitumor activity against human HCT116 cells xenografted in athymic mouse assessed as tumor growth inhibition at 200 mg/kg, ip qd for 21 days measured on day 222009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
AID723138Potentiation of 3.16 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1164924Induction of cell differentiation in human BE(2)-C cells assessed as increase in TrkA expression at 2 to 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID492801Inhibition of human recombinant HDAC1 at 5 uM after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1174683Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID760497Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1599777Inhibition of HDAC6 in human Meso163 cells assessed as upregulation of E-cadherin mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1861657Inhibition of HDAC8 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID622260Inhibition of HDAC6 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1702200Toxicity in Ncr nude mouse xenografted with human HepG2 cells assessed as change in body weight at 60 mg/kg, po QD with 5 days on and 2 days off dosing schedule for 2 weeks cotreated with 75 mg/kg pictilisib and measured at day 14 (Rvb = -0.8%)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1865270Inhibition of HDAC in human MV4-11 cells assessed as upregulation of acetylated alpha-tubulin level incubated for 24 hrs by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1754779Downregulation of RELA (p65 ) gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1280268Inhibition of HDAC6 in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 0.1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1655902Inhibition of EZH2 in human RH4 cells assessed as H3K27me3 level at 0.15 uM incubated for 96 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1282242Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1566810Inhibition of recombinant full length HDAC6 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1556028Inhibition of SIRT1 in human MCF7 cells assessed as H3K9Ac expression at 0.1 uM measured after 24 hrs by Western blot analysis relative to H32019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD
AID704015Inhibition of human recombinant HDAC8 using fluor de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 25 mins by microplate reader analysis2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.
AID1469373Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID288450Growth inhibition of LOX-IMVI cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID723438Potentiation of 10 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.25 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID732446Inhibition of human ES2 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID482940Inhibition of HDAC1 in human COLO205 cells assessed as induction of histone H3 acetylation2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID492811Inhibition of HDAC in human NB4 cells assessed as increase in acetylate tubulin level at 5 uM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID461250Inhibition of HDAC in human HeLa cell nuclear extract2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID723130Potentiation of 50 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1917529Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID1688024Inhibition of recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID672026Inhibition of human recombinant HDAC3 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins at 10 uM measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID663384Growth inhibition of human SK-MEL-5 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID420321Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 by fluorescence polarization assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1702086Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1864243Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated alpha-tubulin level at 1.25 to 5 uM by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1321730Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 100 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1550118Induction of apoptosis in HEL cells assessed as viable cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 87.5%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID476644Antiproliferative activity against human Jurkat JA16 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID593547Inhibition of human HDAC1 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID414986Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1308521Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
AID1762495Inhibition of HDAC1 (unknown origin)2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1200974Solubility of the compound in PBS measured after overnight incubation by LYSA assay2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1246513Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1248351Inhibition of human full length MMP9 using Mca-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to testing measured for 15 mins by fluorometric analysis2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID1649504Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability measured after 72 hrs by tryphan blue assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
AID1487001Inhibition of HDAC3 (unknown origin) by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1433294Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs by SYBR gold staining based alkaline comet assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1537559Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID90212Inhibitory activity against histone deacetylase (HDAC1 and HDAC2) isolated from K562 erythroleukemia cells2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
AID1390963Inhibition of HDAC6 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).
AID343694Inhibition of HDAC in human HeLa cells assessed as induction of histone H3 hyperacetylation after 24 hrs2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
AID1126985Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID748112Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1439348Inhibition of full length recombinant human GST fused His6-tagged HDAC1 expressed in baculovirus infected High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate measured after 24 hrs2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID616002Inhibition of HDAC1 using KI-177 as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1901163Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1401475Selectivity ratio of IC50 for HDAC2 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1451822Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1235115Cytotoxicity against human KG1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1280283Selectivity index, ratio of HDAC6 inhibition in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 0.1 uM over class1 HDAC inhibition in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 0.1 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID316909Inhibition of human DU145 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID663397Growth inhibition of human BT549 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1709348Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1398820Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MKI67 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1348937Effect on CDH1 gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID619056Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID420516Inhibition of HDAC in human IGROV1 cells assessed as histone-H4 acetylation at IC50 after 4 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1832800Inhibition of human recombinant HDAC6 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID329921Inhibition of human HDAC1 in U937 cells at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1514597Antiproliferative activity against human HCCLM3 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1578478Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1833060Anticancer activity against human SK-HEP1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID329931Induction of apoptosis in human U937 cells at 5 uM after 30 hrs2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID269673Antiproliferative activity against human MDA-MB-231 cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1409641Inhibition of HDAC in human A549 cells using Boc-K(Ac)-AMC as substrate by fluorescence assay2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.
AID1875507Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID1380947Antiproliferative activity against human KG1 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID605531Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1599780Inhibition of HDAC6 in human Meso163 cells assessed as upregulation of semaphorin 3F mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID613341Inhibition of human ERG by automated Q-patch assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1765323Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1848559Inhibition of HDAC in human HCT-116 cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1407000Induction of cell cycle arrest in human NB4 cells assessed as accumulation at G1 phase after 30 hrs by propidium iodide-based FACS analysis2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID723152Potentiation of 8 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.25 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1622962Inhibition of HDAC3 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID350719Inhibition of human recombinant HDAC6 by fluorimetry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1742678Induction of cell cycle arrest in human MDA-MB-231 cells assessed as G0/G1 phase accumulation at 2 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 29.10 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1401546Antiproliferative activity against human DG75 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1126984Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID545855Antimalarial activity against Plasmodium falciparum 7G8 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1441633Inhibition of recombinant human cPLA2alpha expressed in Sf9 cells assessed as formation of 7-hydroxycoumarin from of 7-hydroxycoumarinyl-gamma-linolenate by fluorospectrometer analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID328829Toxicity against human HCT116 cells xenografted BALB/c mouse assessed as body weight loss at 100 mg/kg, ip administered 5 days per week for 2.5 weeks2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1742184Inhibition of recombinant human full-length N-terminal GST-tagged HDAC9 (1 to 1069 residues) expressed in wheat germ expression system using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID659641Inhibition of HDAC in human DU145 cells assessed as histone H4 acetylation at 2.5 to 5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1622914Inhibition of HDAC6 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1655889Inhibition of HDAC in human U937 cells assessed as Ac-H3 level at 0.5 uM incubated for 120 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1742658Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1848620Cytotoxicity against human HCC 2998 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1406992Inhibition of HDAC6 in human SH-SY5Y cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1548248Inhibition of HDAC4 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID605620Cell cycle arrest in human HCT116 cells assessed as accumulation at G1 phase at 300 nM after 15 hrs by propidium iodide staining based flow cytometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1763816Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID753149Inhibition of HDAC3 (unknown origin)2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID1897365Inhibition of HDAC1 (unknown origin)
AID1690833Inhibition of class 1 HDAC in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1165110Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID420317Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID274065Clearance after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1245686Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1576453Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID1739572Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated tubulin/GAPDH at 1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1901227Half life in rat liver microsomes by LC-MS/MS analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1433260Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID541651Inhibition of human HDAC9 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1129784Cell cycle arrest in human Jurkat cells assessed as accumulation at G0/G1-phase at 10 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 1.80%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1164192Inhibition of HDAC in human MCF7 cells assessed as hyperacetylation of histone H1 at Lys 9/4 residues at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1742183Inhibition of HDAC7 (unknown origin) using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1848616Cytotoxicity against human DU-145 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1727741Inhibition of HDAC4 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID482945Inhibition of HDAC52010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1566041Inhibition of full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 240 mins by fluorescence based assay2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID1293565Inhibition of full length human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/human recombinant N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescenc2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1832805Inhibition of human HDAC3 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID1861263Selectivity index, ratio of IC50 for inhibition of HDAC2 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID753148Inhibition of HDAC2 (unknown origin)2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID1650415Inhibition of HDAC in human Cal27 cells2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID753146Inhibition of HDAC6 (unknown origin)2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID1361646Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1614128Inhibition of recombinant full length HDAC3 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID511062Inhibition of HDAC in human HeLa cells at 1 uM after 15 mins2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1550129Induction of apoptosis in human K562 cells assessed as necrotic apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 0.827%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1775547Inhibition of HDAC3 (unknown origin)2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1832799Binding affinity to human BRD4 domain 1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID1737143Induction of cell cycle arrest in human HCT116 cells assessed as cell accumulation at G2/M phase at 3 uM after 24 hrs by Rnase/PI staining based flow cytometric analysis (Rvb = 26.4%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID781047Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID1487015Inhibition of HDAC1 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1873402Inhibition of HDAC1 (unknown origin) preincubated for 90 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID90663Inhibition of Histone deacetylase 1 (HDAC1) of HeLa nuclear extracts2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID414980Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID663360Growth inhibition of human HT-29 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1591715Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1826626Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 0.014 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID404450Antimalarial activity against Plasmodium falciparum TM91C235 by hypoxanthine uptake2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID385229Inhibition of HDAC12008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
AID1771455Antiproliferative activity against human U-937 cells assessed as cell growth inhibition after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID544096Selectivity index, ratio of LC50 for mouse RAW264.7 cells to IC50 for Plasmodium falciparum2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID605396Inhibition of human recombinant HDAC6 using fluor de Lys as substrate by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1832797Cytotoxicity against human TALL-1 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
AID90197Inhibitory concentration against histone deacetylase activity2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors.
AID1339567Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID717824Inhibition of HDAC3 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1578898Induction of apoptosis in human Bel7402 cells assessed as annexin-V positive cells at 5 uM after 72 hrs by Annexin-V/PI staining based flow cytometry relative to control2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1742175Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1764801Inhibition of recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID499814Inhibition of Plasmodium falciparum HDAC12010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1421602Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1439773Inhibition of Pseudomonas aeruginosa PA3774 using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by trypsin-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa.
AID1476119Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells using RHKKAc as substrate in presence of ATP2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID274034Microsome stability: percent compound remaining2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1709361Induction of apoptosis in human Jurkat cells assessed as necrotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 0.23%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID527319Growth inhibition of human HeLa cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
AID1825926Inhibition of recombinant human full length N-terminal GST tagged HDAC6 (1 to 1215 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
AID308648Increase in p21WAF1/CIP1 gene expression in PANC1 cells after 24 hrs relative to control2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID663398Growth inhibition of human T47D cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID747252Inhibition of human recombinant HDAC1 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1737146Induction of apoptosis in human HCT-116 cells assessed as viable cells at 3 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 90.34%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1742762Induction of apoptosis in mouse 4T1 cells implanted in BALB/c mouse assessed as increase in caspase-3 cleavage by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1690840Disaggregation of self-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 10 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID329922Inhibition of human HDAC4 in U937 cells at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1578480Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1764800Inhibition of recombinant human HDAC1 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID618017Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c nu mouse assessed as tumor growth inhibition at 90 mg/kg, po qd for 19 days relative to control2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1384231Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 1000 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID384317Inhibition of maize histone deacetylase 1A2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID446336Metabolic stability in human liver microsomes assessed as half life2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID350731Growth inhibition of human RXF631L cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1321700Inhibition of HDAC1 (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1739584Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated H3/GAPDH at 0.1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID300834Growth inhibition of human ACHN cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID1486676Inhibition of HDAC6 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1543954Induction of apoptosis in human Bel7402/5-FU cells assessed as late apoptotic cells at 5.0 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 1.01%)2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1915602Cytotoxicity against human A2780P cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID652749Inhibition of recombinant human HDAC5 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1566816Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID710837Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID1599722Inhibition of HDAC in human MeT-5A cells assessed as increase in transfected YFP fused histone H3 acetylation treated at 8 hrs after YFP fused H3 transfection measured after 24 hrs incubation by BRET assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1865263Inhibition of recombinant his-tagged human HDAC3 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1886181Inhibition of HDAC in human HeLa cells using BOC-K(Ac)-AMC as substrate at 10 uM measured after 30 mins by fluorescence based microtiter plate reader assay relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1518782Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1812445Inhibition of human recombinant HDAC6 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1129772Increase in p21 protein expression in human Jurkat cells at 10 uM after 24 hrs by FACS flow cytometric analysis2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID526536Growth inhibition of human HCT15 cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1336947Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G1 phase at 2.5 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 69.5%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1365022Inhibition of recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1533327Inhibition of full length human N-terminal FLAG-tagged HDAC8 (1 to 377 residues) expressed in HEK293 cells preincubated for 15 mins followed by Boc-[trifluoroacetyl-Lys]-AMC substrate addition measured after 30 mins by fluorimetric method2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
AID1515908Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1469335Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1622986Inhibition of HDAC8 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1742229Antimetastatic activity against CM-Dil labeled human MDA-MB-231 cells xenografted in Zebrafish AB assessed as reduction in tail metastasis at 2.5 ug/ml measured after 5 days by fluorescence microscopic analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1873381Inhibition of HDAC1 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1476158Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1294805Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate by fluorometric assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors.
AID760508Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1282275Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumor mass change at 50 mg/kg, ip q2d for 12 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1406988Inhibition of HDAC6 in human U87 cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1597937Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1547248Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1177043Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1848627Cytotoxicity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID621737Inhibition of HDAC1 by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors.
AID1202593Cytotoxicity against human HeLa cells after 72 hrs by MTS assay2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID90691Inhibition of maize Histone deacetylase 22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID1275638Inhibition of recombinant human HDAC4 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1478601Induction of apoptosis in human K562 cells after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric method2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1702100Inhibition of HDAC in human PC-3 cells assessed as increase in acetylation of histone H3 at K9 residue at 10 uM incubated for 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID604082Inhibition of JMJD2E2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Inhibitors of histone demethylases.
AID303347Inhibition of HDAC in HeLa nuclear extract in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID421216Inhibition of HDAC1 from human HeLa cells at 5 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID605527Inhibition of HDAC1 in human HCT116 cells assessed as induction of histone H3K9 acetylation after 30 hrs by Western blot analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID717820Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 1.25 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1439352Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter 96 AQueous Non-Radioactive assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID747253Growth inhibition of human DU145 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1215092Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 up to 46 uM after 24 hrs by luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1398819Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of E2F1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1543945Inhibition of human recombinant HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID499812Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum D62010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1206754Antitumor activity against human HEL cells xenografted in BALB/c-nu mouse assessed as inhibition of tumor growth at 120 mg/kg/day, po administered for 21 days measured every 3 days during compound dosing relative to control2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1594438Inhibition of C-terminal GST-tagged full-length human HDAC1 expressed in Sf9 cells at 10 uM pre-incubated for 10 mins before substrate addition and measured after 20 mins by fluorescence assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors.
AID622256Inhibition of HDAC3 after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1514599Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H3 levels at 1.25 uM by Western blot analysis relative to beta-actin (Rvb = 0.5 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID672034Ratio of IC50 for human HDAC2 preincubated for 24 hrs to IC50 for human HDAC2 preincubated for 5 mins2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1202585Inhibition of His-tagged HDAC8 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID1466062Inhibition of recombinant human full length HDAC4 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID655474Restoration of CFTR deltaF508 mutant trafficking to cell surface as glycoforms in human CFBE41o cells at 1 uM after 24 hrs by Western blotting2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1240552Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 1 uM after 24 hrs using Annexin V-FITC and propidium iodide staining by flow cytometry (Rvb = 4.04%)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID492803Inhibition of human recombinant HDAC1 after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1548290Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID1326528Toxicity in nude mouse xenografted with human HCT116 cells assessed as change in body weight at 200 mg/kg, po qd2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1865261Inhibition of recombinant his-tagged human HDAC1 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1469299Induction of apoptosis in human NCI-H460 cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.29%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1890310Inhibition of HDAC3 (unknown origin)2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1897466Inhibition of HDAC in human HCT-116 cells assessed as upregulation of acetyl-histone 3 level at 1.25 to 5 uM incubated for 36 hrs by Western blot analysis
AID1363797Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID310186Antitumor activity against MDA-MB-231 cells xenografted BALB/c nude mouse at 30 mg/kg, ip for 15 days2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID526533Growth inhibition of human MDA-MB-231 cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1273873Metabolic stability in mouse liver microsomes assessed as compound remaining at 1 uM preincubated for 10 mins measured after 30 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1739587Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated tubulin/GAPDH at 0.1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1900917Induction of apoptosis in mouse GL26 cells assessed as caspase-mediated PARP1 cleavage at 1.25 to 5 uM incubated for 48 hrs by Western blot analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID352524Antiproliferative activity against human Panc 04.03 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID347807Inhibition of human HDAC8 at 0.50 uM2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1486294Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID593548Inhibition of human HDAC3 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID652764Inhibition of HDAC8 in human HeLa cells nuclear extract using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1141761Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorimetric analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1890323Inhibition of HDAC1 in mouse CT26 cells assessed as accumulation of acetylated H3 level at 6 uM after 24 hrs by Western blotting analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1426428Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID663358Growth inhibition of human HCT116 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID775834Inhibition of human recombinant MMP-2 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2.AcOH as substrate at 10 uM preincubated for 30 mins prior to substrate addition measured for 30 mins by fluorescence assay relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1355714Synergistic antifungal activity against FLC resistant Candida albicans 0304103 assessed as FIC index after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1742223Cmax in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1769653Inhibition of ALK G1202R mutant (unknown origin)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1141783Inhibition of HDAC in human HCT116 cells assessed as increase in histone-H3 acetylation after 3 hrs by Western blotting analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID353354Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
AID1622904Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1676594Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1633416Inhibition of human recombinant GSK3beta up to 50 uM using GSM as substrate incubated for 30 mins by luminescence based assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID1383985Inhibition of HDAC1/2 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1704064Inhibition of human C-terminal Flag tagged HDAC1 (1 to 482 residues) expressed in SF9 cells using Ac-peptide substrate at 100 nM preincubated for 15 mins followed by substrate addition and measured after 60 mins by microplate reader method2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID1811364Inhibition of HDAC4 (unknown origin)2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID1864238Stabilization of FAM-labeled DNA Pu22 (unknown origin ) double strand assessed as G4-quadruplex formation incubated for 30 mins in presence of potassium ions by electrophoresis mobility shift assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1826596Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1547282Inhibition of HDAC in human HCT116 cells assessed as increase in acetylated histone H3 expression level measured after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1653143Cytotoxicity against human PC3 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID481554Cytotoxicity against human KB cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1380954Inhibition of HDAC3 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1383988Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1410014Selectivity index, ratio of CC50 for human U937 cells to EC50 for reactivation of latent HIV1 infected in human U1 cells2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
AID1337293Therapeutic index, ratio of IC50 for mouse TAMH cells to IC50 for human cancer cells2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1848583Inhibition of full length C-terminal his6-tagged human recombinant HDAC2 (1 to 488 residues)2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1702067Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1415668Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP expression at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID446345Clearance in CD1 mouse at 15 mg/kg, po2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID1415646Inhibition of HDAC1 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1433291Induction of apoptosis in p53 null human U937 cells at 2 uM preincubated with NAC for 3 hrs followed by compound addition measured after 24 hrs by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1821965Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
AID1890332Stability in mouse liver microsomes assessed as half-life and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID780580Inhibition of Topoisomerase 2 (unknown origin) assessed as impairment of pBR322 DNA decatenation at 100 uM after 30 mins by agarose gel electrophoresis2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
AID1487042Inhibition of HDAC in human HeLa-S3 cells lysates assessed as remaining enzyme activity at 5 x 10'-8 M pre-incubated for 15 mins before HDAC-Glo I/II substrate addition and measured after 30 mins post substrate addition2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID384316Inhibition of maize histone deacetylase 1B2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID90682Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID1240549Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID1487046Inhibition of HDAC3 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1326518Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1312876Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as change in tumor mass at 50 mg/kg, ip administered every 2 days for 11 days measured every 2 days of compound dosing relative to control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1783062Antifungal activity against fluconazole-resistant Candida tropicalis 5008 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1898953Induction of cell cycle arrest in human NCI-H460 cells assessed as accumulation of cells at S phase at 4.2 uM after 72 hrs by flow cytometry (Rvb = 32.1%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID541653Inhibition of human HDAC10 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID476832Toxicity in FVB mouse assessed as effect on number of WBC at 50 mg/kg, po administered 5 times per week for 2 weeks (Rvb = 9.1 +/- 0.2 10^3/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1548268Induction of cell cycle arrest in human KM3 cells assessed as reduction in cell cycle progression in G2/M phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry
AID1578505Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 4 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 19.46 to 22.17 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1861653Inhibition of HDAC1 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1422514Inhibition of HDAC in MEF assessed as increase in histone H3K18 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1431817Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID274099Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 50% of isolates after 48h.2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID1497923Induction of CRBN ubiquitin ligase-mediated HDAC6 degradation in human MCF7 cells assessed as decrease in HDAC6 levels at 10 uM after 12 hrs by immunoblotting analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Development of the first small molecule histone deacetylase 6 (HDAC6) degraders.
AID1200973Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac)AMC as substrate2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1848594Induction of cell cycle arrest in human NCI-H522 cells assessed as accumulation at G2/M phase 5 uM incubated for 24 to 72 hrs by PI staining based flow cytometric analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1383989Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1751984Inhibition of HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID1826650Antitumor activity against HEL cells xenografted in BALB/C mouse assessed as tumor growth inhibition at 10 mg/kg, po qd for 14 days consecutively by caliper method relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1203896Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1816212Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 2.5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 85.7%)
AID663391Growth inhibition of human SN12C cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1282240Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1597930Inhibition of HDAC in human HeLa cell nuclear extracts at 1 uM2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1515914Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID304373Inhibition of HDAC2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
AID1441662Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta mRNA level at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1547300Inhibition of HDAC in human HCT116 cells assessed as induction of autophagy at marginal level by measuring LC3-I cleavage to LC3-II at 10 uM measured after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1550084Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID411259Cytotoxicity against human NCI-H69 cells after 72 hrs by trypan blue exclusion assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1614131Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1816206Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 2.5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.09%)
AID1384230Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1599728Cytotoxicity against human Meso163 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1702199Toxicity in Ncr nude mouse xenografted with human HepG2 cells assessed as animal survival at 60 mg/kg, po QD with 5 days on and 2 days off dosing schedule for 2 weeks cotreated with 75 mg/kg pictilisib and measured at day 122018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1436790Growth inhibition of human NCI-H292 cells in FBS containing medium after 72 hrs using compound after sonication in presence of LDL by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity.
AID1855261Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 1.5 uM incubated for 48 hrs by PI and annexin V-FITC staining based flow cytometry (Rvb = 3.4%)2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1742719Induction of apoptosis in mouse 4T1 cells assessed as viable cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 91.1 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID496801Inhibition of human HDAC12010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1126966Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC1 (unknown origin)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1825927Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs followed by trypsin addition and further incubated for 2 hrs
AID761585Inhibition of HDAC in human HeLa cell extract using fluor de Lys as substrate at 1 uM after 15 mins by fluorometric analysis2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID90351Concentration required to inhibit human Histone deacetylase (HDAC) enzyme by 50%2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1164178Cell cycle arrest in human U937 cells assessed as block at G1 phase at 5 uM after 24 to 96 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1399809Clearance in human hepatocytes assessed per million cells at 1 uM after 5 to 90 mins by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
AID374827Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID274063Half life after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID404449Antimalarial activity against Plasmodium falciparum W2 by hypoxanthine uptake2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID255818Inhibitory concentration against Histone deacetylase 1B in maize2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
AID1543929Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID525021Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 5 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1487045Inhibition of HDAC2 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1127007Induction of apoptosis in human U937 cells assessed as necrotic cells using annexin-V/propidium iodide staining at 0.125 uM after 24 hrs by flow cytometry analysis (Rvb = 0.06%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1821345Toxicity in mouse xenografted with human HepG2 cells assessed as kidney edema at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID748114Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1901229Half life in human liver microsomes by LC-MS/MS analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID473191Growth inhibition of human BJ cells after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1503585Inhibition of C-terminal His-tagged human recombinant full-length HDAC8 expressed in baculovirus expression system assessed as reduction in 7-amino-4-methylcoumarin by fluorescence based assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design.
AID637888Inhibition of recombinant human HDAC1 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases.
AID1234893Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1543930Antiproliferative activity against human SMMC7721 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1887681Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1550325Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as combination index after 48 hrs in presence of ruxolitinib by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1848601Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1502981Antiproliferative activity against human MGC803 cells incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1702058Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1885672Synergistic antiproliferative activity against human HFL1 cells at 2.5 to 12.5 uM measured after 72 hrs in presence of CDDO-Me by MTT assay2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy.
AID473190Growth inhibition of human MUF cells at 0.05 to 100 uM after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID618087Toxicity in athymic nu/nu Harlan mouse xenografted with human HCT116 cells assessed as body weight loss at 200 mg/kg, po QD for 21 days measured on day 82011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID246081Effective Concentration of compound to inhibit the growth of human NCI-H226 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1469491Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as reduction in tumor weight at 130 mg/kg, ip administered daily for 18 days measured after 8 to 25 days2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1421902Antiplasmodial activity against drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID732874Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1293562Antiproliferative activity human HCT116 cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1459948Antiproliferative activity against human PC3 cells measured after 48 hrs by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1549141Antifungal activity against azole-sensitive Cryptococcus neoformans H99 after 72 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1481749Antiproliferative activity against human Raji cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors.
AID1901171Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM preincubated for 6 hrs followed by compound washout and measured after 12 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1511969Selectivity index, ratio of IC50 for full length recombinant FLAG/His-tagged C-terminal human HDAC1 expressed in baculovirus infected Sf9 insect cells to IC50 for full length recombinant GST-tagged N-terminal human HDAC6 expressed in baculovirus infected 2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
AID1848301Induction of apoptosis in human MV4-11 cells assessed as viable cells at 1 uM incubated for 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 96.5%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID632973Cytotoxicity against human PC3 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1702062Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins b2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1848624Cytotoxicity against human KM12 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1888416Inhibition of fungal filamentation in azole-resistant Candida albicans 0304103 assessed as reduction in yeast-hypha transition at 64 ug/ml by inverted microscopic analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID1127008Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining at 0.125 uM after 24 hrs by flow cytometry analysis (Rvb = 96.24%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1614127Inhibition of recombinant full length human HDAC2 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1312869Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1389951Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 4 uM after 24 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID347868Growth inhibition of human Colon cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1732193Cytotoxicity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1873383Inhibition of HDAC3 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID761582Inhibition of full length His-tagged human recombinant HDAC6 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID208381Concentration required to reassume their usual morphology of T/5 cells1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID1476146Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1547350Antitumor activity against human HCT116 cells xenografted in BALB/cAnNCrl mouse assessed as tumor growth inhibition at 30 mg/kg, po administered on day 1 to day 192020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1401376Inhibition of human recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID297482Cytotoxicity against human SKBR3 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1518783Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID347875Growth inhibition of human CNS cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1361651Induction of apoptosis in human A549 cells assessed as viable cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1515913Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1545842Antiproliferative activity against human A549 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID297472Inhibition of HDAC in HeLa cells assessed as induction of human histone H3 hyperacetylation2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1861305Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at S phase measured by flow cytometry analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1550324Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs in presence of ruxolitinib by MTT assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID527043Cytotoxicity against human NCI-H522 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1901174Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM treated for 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1816966Cytotoxicity against human CEM cells assessed as cell death incubated for 20 hrs measured by DNS assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their
AID1864216Inhibition of HDAC in human HeLa nuclear extract incubated for 30 mins by fluorescence-based Glo-luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1689773Inhibition of human recombinant HDAC1 at 10 uM preincubated for 10 mins followed by addition of substrate fluor De Lys SIRT1 deacetylase measured after 30 mins by fluorescent plate reader analysis relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID1164902Inhibition of HDAC6 in human A549 cells assessed as tubulin acetylation after 17 to 18 hrs by cytoblot assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1482120Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1707507Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID1816200Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
AID605538Antiproliferative activity against doxorubicin-resistant human COR-L23 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1355706Antifungal activity against FLC resistant Candida albicans 0304103 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1677515Binding affinity to full length His-tagged Bcl2 (unknown origin) preincubated for 30 min followed by 5-FAM Bid-BH3 addition and measured after 20 mins by fluorescence polarization assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1888590Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay
AID1164906Inhibition of HDAC1 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1336944Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at lesser G1 phase at 2.5 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.59%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1742221Half life in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1901172Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM preincubated for 6 hrs followed by compound washout and measured after 12 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID732876Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1639365Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1898906Antiproliferative activity against human Z138 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1515911Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID313734Inhibition of HDAC62008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID324949Inhibition of HDAC3 in HEK293 cells2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID717817Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 5 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1390025Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID482957Half life in rat liver microsome2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1205630Growth inhibition of human HCT15 cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1467240Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured after 30 mins by fluorometri2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1129779Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M-phase at 10 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 10%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID476641Antiproliferative activity against human SK-BR-3 cells after 48 hrs by cell titer-glo assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID525019Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR protein level at 1 uM after 1 hr by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1269319Cytotoxicity against human A2780S cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID1240548Inhibition of HDAC1/2 in human HeLa cells nuclear extracts using acetylated histone peptide as substrate after 30 mins by Color de Lys assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID765198Cytotoxicity against human MDA-MB-231 cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID1466065Inhibition of HDAC in human PC3 cells assessed as increase in histone H3 acetylation at 1 uM after 24 hrs by Western blot analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1742657Cytotoxicity against human B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID663388Growth inhibition of human A498 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID482966Clearance in mouse at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1141768Cytotoxicity against human A549 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1337288Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutant after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1730888Inhibition of EGFR in human NCI-H1975 cells assessed as reduction in EGFR phosphorylation at Tyr-1068 residues at 1 uM after 48 hrs by Western blot analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1887685Cytotoxicity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1141797Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin)2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID670513Inhibition of EGFR derived from human A431 cell membrane assessed as inhibition of poly-Glu-Tyr phosphorylation after 30 mins by ELISA assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.
AID1623533Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1863441Inhibition of HDAC9 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1454032Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate by fluorimetric method2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1066163Cytotoxicity against human HCT116 cells at 50 uM after 72 hrs2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
AID609498Half life in human liver microsomes2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1548288Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID1742704Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 5.57 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID623020Inhibition of human HDAC1 expressed in Escherichia coli using fluorogenic substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group.
AID1466058Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID672023Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1764252Inhibition of recombinant human N-terminal GST-fusion tagged/C-terminal GST-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measu2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID269674Antiproliferative activity against human NCI-H23 cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID524991Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1702155n-Octanol/water distribution coefficient, logD of the compound at pH 7.42018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1769654Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID663347Growth inhibition of human MOLT4 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID90350Inhibitory activity against histone deacetylase (HDAC) enzyme obtained from H1299 human lung carcinoma cell lysates2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID1141243Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys (acetyl)-AMC as fluorogenic substrate after 30 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Design, synthesis and preliminary evaluation of α-sulfonyl γ-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors.
AID1897805Inhibition of recombinant full length C-terminal His/Flag-tagged human HDAC1 (1 to 482 residues) using Z-Lys(Ac)-AMC as substrate preincubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based microplate reader anal2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.
AID1742684Induction of cell cycle arrest in mouse 4T1 cells assessed as G0/G1 phase accumulation at 2 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 42.06 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1170740Inhibition of human recombinant HDAC1 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID443645Binding affinity to pyridoxal-5'-phosphate assessed as formation of PLP-aldoxime at 5 mM after 1 hr by UV/vis spectroscopy2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.
AID1178599Inhibition of human HDAC4 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1487096Inhibition of HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID1164196Inhibition of HDAC6 in human MCF7 cells assessed as hyperacetylation of tubulin at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1486299Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1155329Antimalarial activity against asexual blood stage of Plasmodium falciparum 3D7 infected in human serum assessed as [3H]hypoxanthine incorporation incubated for 48 hrs prior to 3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1487008Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1732191Cytotoxicity against human HuT78 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1401543Antiproliferative activity against human OCI-LY3 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID414981Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID1751986Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID243634In vitro inhibition against human Histone deacetylase2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors.
AID1401368Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 2 x 10'-7 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1164926Effect on p21 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1227043Stability in human plasma assessed as compound remaining after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1303631Potentiation of 1 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1515883Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 500 nM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.87%)2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1671983Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase measured after 24 hrs2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID1273877Inhibition of human CYP2C19 using 3-cyano-7-ethoxycoumarin as substrate at 10 uM after 30 mins by fluorimetric analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1399812Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
AID1861656Inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1849167Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1164785Inhibition of HDAC10 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1622942Cytotoxicity against human AML cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID420506Antiproliferative activity against cisplatin-resistant human IGROV1 cells after 72 hrs2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID663341Inhibition of HDAC in human MDA-MB-231 cells assessed as stimulation of histone H3 acetylation incubated for 24 hrs by Western blot2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1832681Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1312868Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID316895Inhibition of human MCF7 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID544399Antimalarial activity against Plasmodium falciparum infected in mouse RAW264.7 cells2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID723424Potentiation of 5 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1754780Downregulation of RELB gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1864242Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated H4 level at 1.25 to 5 uM by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID329916Induction of histone H4 hyperacetylation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1876462Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence plate reader assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID759309Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1599723Cytotoxicity against human Meso13 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID297486Cytotoxicity against human proliferating RKOp21 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1164028Inhibition of human recombinant HDAC4 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID732447Inhibition of human PC3 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1155335Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1541450Cytotoxicity against human CAL27 cells assessed as reduction in cell survival measured after 72 hrs by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1821967Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
AID1587864Inhibition of recombinant full-length C-terminal His-tagged human HDAC2 expressed in baculovirus infected Sf9 insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1816207Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 2.5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.8%)
AID1418670GPx-like activity of the compound assessed as velocity for H2O2 reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID1441635Inhibition of recombinant human N-terminal His-tagged 12-LOX expressed in Escherichia coli assessed as conversion of arachidonic acid to HETEs measured for 300 secs by UV-visible spectrophotometric analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1915538Inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID328801Inhibition of HDAC8 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1312925Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of acetylated histone H3 level at 2 uM after 6 hrs by Western blot method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1279130Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
AID1605977Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1821342Toxicity in mouse xenografted with human HepG2 cells assessed as heart edema at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1614226Induction of apoptosis in human MM1S cells assessed as early apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.38%)
AID1848625Cytotoxicity against human SW620 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1469326Induction of apoptosis in human MDA-MB-231 cells assessed as live cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.1%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1548258Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay
AID1832682Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID670012Inhibition of human recombinant HDAC6 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID781051Inhibition of HDAC in human HeLa cell nuclear extracts using Fluor de Lys as substrate by fluorescence assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID1296346Inhibition of recombinant Schistosoma mansoni HDAC8 expressed in Escherichia coli using Fluor de Lys as substrate preincubated for 90 mins followed by BML-KI176 addition measured after 45 mins by fluorescence assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.
AID1653119Cytotoxicity against human MCF7 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1816381Inhibition of JAK2 (unknown origin) assessed as inhibition rate at 10 nM incubated for 60 mins by microplate reader analysis relative to control
AID1647330Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as ratio of cerebral blood flow in right parietal area at 25 mg/kg, ip administered post surgery measured2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID329928Inhibition of human HDAC4 in U937 cells assessed as residual activity at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID760518Therapeutic index, ratio of GI50 for human HMEC to GI50 for human SK-BR-3 cells2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1622931Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1856998Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1365026Selectivity ratio of IC50 for recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 for recombinant human HDAC22017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1415653Inhibition of HDAC8 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1774968Inhibition of HDAC in human HeLa nuclear extract at 10 uM using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors.
AID1819504Inhibition of HDAC2 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1361631Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1482100Inhibition of HDAC 8 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1396961Antiproliferative activity against human MCF7 cells2018Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
AID1898903Antiproliferative activity against human Ramos cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1915568Cytotoxicity against human PC-3 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1502978Antiproliferative activity against human PC3 cells incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1566804Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID760504Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1166496Inhibition of human recombinant full length HDAC1 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1502987Inhibition of C-terminal His-tagged full length human HDAC2 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID526535Growth inhibition of human NUGC3 cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1337289Antiproliferative activity against human NKYS cells after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1709352Selectivity index, ratio of IC50 for human HS5 cells to IC50 for human NAMALVA cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID524994Inhibition of HDAC9 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1578156Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1742176Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1742750Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 150 mg/kg, po administered for 34 days and measured on day 342020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1482098Inhibition of HDAC 2 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1234906Antitumor activity against human H7402 cells xenografted in mouse assessed as tumor increment ratio at 100 mg/kg/day, po for 16 days relative to control2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID609507Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect High5 cells using Boc-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
AID374822Inhibition of C-terminal His-tagged HDAC8 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1437239Inhibition of HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID1702060Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID545858Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID618013Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 5 uM after 48 hrs using propidium iodide staining by flow cytometric analysis2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1380956Inhibition of HDAC8 (unknown origin) using fluorogenic Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1384207Inhibition of HDAC2 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID503688Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 5 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID652757Down regulation of HDAC7 in human CFBE41o cells at 0.2 to 5 uM by Western blot analysis2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1269317Cytotoxicity against mouse NIH/3T3 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID1742739Inhibition of human ERG2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID374811Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1431811Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1888584Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay
AID519587Toxicity in neonatal foreskin fibroblasts2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1355708Antifungal activity against FLC resistant Candida albicans 100 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1449327Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1415667Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase3 expression at 5 uM after 48 hrs by Western blot analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1336948Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at S phase at 2.5 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 27.1%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1859937Antiproliferation activity against human U-937 cells assessed as reduction in cell viability at 5 to 50 uM measured after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1205629Growth inhibition of human ACHN cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1127331Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1173502Inhibition of N-terminal GST-tagged human HDAC4 (627 to 1085 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID717819Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1401504Cytotoxicity against human Jurkat cells assessed as cell viability at 1 uM after 44 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID488273Inhibition of HDAC12010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID373085Antitumor activity in mouse P388 cells xenografted B6D2F1 mouse assessed as increase in life span at 60 mg/kg/day, ip administered 3 to 7 days postxenografting2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID781048Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID404448Antimalarial activity against Plasmodium falciparum D6 by hypoxanthine uptake2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID392408Induction of histone H3 acetylation in human T24 cells after 3 hrs by ELISA2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Sulfamides as novel histone deacetylase inhibitors.
AID1487090Increase in SMN2 mRNA expression in induced pluripotent stem cell derived from human GM03813 cells isolated from SMA patient homozygous for deletion of exons 7 and 8 in SMN1 gene and containing 3 SMN2 gene copies at 0.1 uM by PCR assay relative to untreat2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID420511Cell cycle arrest in human IGROV1 cells assessed as accumulation at sub-G1 phase at IC90 after 24 hrs using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID482953Antiproliferative activity against human PC3 cells2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1129787Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M-phase at 10 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.20%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1336924Cytotoxicity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1384209Inhibition of HDAC6 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1511156Inhibition of HDAC6 in human HL60 cells assessed as increase in acetylation of alpha tubulin at 0.08 to 1.6 uM incubated for 24 hrs by western blot analysis2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1702135Inhibition of PI3K/AKT/mTOR signaling in human HuH-7 cells assessed as AKT S473 phosphorylation level at 10 uM incubated for 4 hrs including last 12 mins stimulation with 20 ng/ml growth factor VEGF by Western blot analysis (Rvb = 100 %)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1812467Antiplasmodial activity against Plasmodium falciparum stage IIb-III gametocytes assessed as abnormal morphology by measuring rounded/swollen at highest concentration measured after 72 hrs using Geimsa staining based assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1605974Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID310126Growth inhibition of human H460 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.
AID1275641Growth inhibition of human HCT116 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1390811Antiproliferative activity against human Raji cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
AID1478582Induction of apoptosis in human K562 cells assessed as necrotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.035%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1386685Inhibition of HDAC in human GM18453 cells harboring NPC1 mutant assessed as increase in 250 kDa NPC1 protein expression at 5 uM measured after 48 hrs by Western blot analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1547257Inhibition of human recombinant His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1591854Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells at 10 nM using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay relative to contro2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID1266812Antiproliferative activity against human LoVo cells assessed as cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1348932Upregulation of TNFalpha gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1487091Increase in SMN2 mRNA expression in induced pluripotent stem cell derived from human GM03813 cells isolated from SMA patient homozygous for deletion of exons 7 and 8 in SMN1 gene and containing 3 SMN2 gene copies at 1 uM by PCR assay relative to untreated2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID1485125Cell cycle arrest in human Hs683 cells assessed as accumulation at sub-G1 phase at 2 uM after 24 to 48 hrs by propidium iodide staining-based flow cytometry2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1164927Effect on acetylated histone H3 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID90690In vitro for anti-HD2 (Histone deacetylase 2) activity in maize2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID1337285Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1764815Inhibition of Nanoluc-fused HDAC1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1164918Antiproliferative activity against human BE(2)-C cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1784985Inhibition of HDAC1 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1764298Inhibition of class-1 HDAC in human CAL-27 cells assessed as induction of histone H-3 acetylation at 1 uM for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1173499Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1785342Inhibition of recombinant human SIRT2 measured after 30 mins by fluorescence microplate reader assay
AID525032Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 1 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1383993Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1639367Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID603540Toxicity in human MDA-MB-231 cells xenografted athymic nude mouse assessed as signs of toxicity at 90 mg/kg, ip qd for 21 days2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1690839Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation after 24 hrs by thioflavin-T fluorescence method2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1848584Inhibition of full length C-terminal FLAG-tagged human recombinant HDAC6 expressed inSf9 insect cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1275640Growth inhibition of human MCF7 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1688034Induction of apoptosis in human HL-60 cells assessed as live cells at 1 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 89.29 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID503692Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 16 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1390010Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1578496Induction of apoptosis in human MV4-11 cells assessed as viable cells at 0.25 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 53.01 to 53.07 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID619142Apparent permeability from apical to basolateral side of human Caco2 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID663383Growth inhibition of human SK-MEL-28 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1816186Inhibition of HDAC1 (unknown origin) incubated for 60 mins using microplate reader analysis
AID1174705Antitumor activity against human U937 cells xenografted in athymic nude mouse at 120 mg/kg/day, po after 16 days relative to control2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1403179Inhibition of Akt phosphorylation in human HepG2 cells at 2 uM after 48 hrs by Western blot analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1576461Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by PI/RNaseA staining based flow cytometry analysis relative to control
AID1200982AUC (0 to infinity) in ICR mouse at 10 mg/kg, iv2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1623528Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID670971Inhibition of human recombinant His6-tagged and GST-fuses HDAC3 expressed in insect High5 cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
CCLab--a multi-objective genetic algorithm based combinatorial library design software and an application for histone deacetylase inhibitor design.
AID313730Inhibition of HDAC22008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1449321Antiproliferative activity against human ONS76 cells after 72 hrs by Celltiter-Glo assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID297471Inhibition of recombinant HDAC1 in HeLa cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1373250Inhibition of HDAC6 (unknown origin) at 1 uM preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
AID1451829Inhibition of recombinant HDAC2 (unknown origin) using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1511151Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1174684Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID619264Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 200 mg/kg, po qd for 21 days2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1688044Upregulation of acetylated H3 level in human HL-60 cells at 2 uM measured after 12 hrs by Western blot analysis2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID274077Inhibition of HCT116 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1537566Cell cycle arrest in human G55T2 cells assessed as accumulation in G0/G1 phase at 3 uM incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 49.9 %)2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID373076Inhibition of human recombinant HDAC32009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1384210Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID316935Inhibition of HDAC52008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1164783Inhibition of HDAC6 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1205632Growth inhibition of human NUGC3 cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1336926Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1600656Inhibition of recombinant human full length C-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID1514603Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H4 levels at 2.5 uM by Western blot analysis relative to beta-actin (Rvb = 1 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID348802Inhibition of HDAC72008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID628436Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1677512Inhibition of HDAC1 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1234909Toxicity in human H7402 cells xenografted mouse assessed as change in body weight at 100 mg/kg/day, po for 16 days2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1578500Induction of apoptosis in human MV4-11 cells assessed as viable cells at 1 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 53.01 to 53.07 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID246062Effective Concentration of compound to inhibit the growth of human St-4 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1785335Inhibition of HDAC4 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID1572359Inhibition of human HDAC6 in human T24 cells assessed as up-regulation of PDL1 by measuring volume intensity at 10 uM after 48 hrs by Western blot analysis relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID447579Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.
AID607635Inhibition of HDAC6 in human Hela cells assessed as increase in alpha-tubulin acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
AID1355745Antitumor activity against human HEL cells xenografted in BALB/C nude mouse assessed as tumor growth at 10 mg/kg, ip bid treated for 21 consecutive days relative to control2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1410327Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1737150Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 4.01%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1890518Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID659634Antiproliferative activity against human DU145 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1821265Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1848615Cytotoxicity against human PC-3 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1861335Inhibition of HDAC in human OCILY3 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1164036Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1549163Inhibition of HDAC in HUVEC using Boc-Lys(Ac)-AMC as substrate preincubated for 12 hrs followed by substrate addition and measured after 4 hrs by fluorimetry2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1321732Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 1000 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1421915Inhibition of HDAC in synchronized trophozoite stage Plasmodium falciparum 3D7 infected in human erythrocytes assessed as increase in acetylated H2A.Z level at 5 times IC50 after 3 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID348803Inhibition of HDAC82008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID1413067Inhibition of nuclear HDAC in human SKOV3 cells assessed as increase in acetylated histone H3 levels at 10 uM after 1 hr by immunoblot method2018MedChemComm, Jun-01, Volume: 9, Issue:6
Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition.
AID1599765Inhibition of HDAC6 in human Meso163 cells assessed as increase in histone H3 acetylation at 2.5 uM measured after 6 to 20 hrs by Western blot analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1127328Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID628286Antiproliferative activity against human HeLa cells after 24 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1060989Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1326513Antiproliferative activity against human A549 cells after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1410330Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1441678Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as TGF-beta1 level at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 by by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1235110Cytotoxicity against human U937 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1861254Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1173501Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID208382Concentration required to reduce cell proliferation of T/5 cells1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID1274872Inhibition of HDAC2 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1897369Inhibition of FGFR1 (unknown origin) at 10 nM relative to control
AID1206756Antitumor activity against human HEL cells xenografted in BALB/c-nu mouse assessed as decrease in tumor volume at 120 mg/kg/day, po administered for 21 days measured every 3 days during compound dosing relative to control2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1126981Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1401556Antiproliferative activity against human MM487 cells at 10 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1599725Cytotoxicity against human A549 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID628211Antiproliferative activity against human HeLa cells after 72 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1699970Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1819523Induction of apoptosis in human KG-1 cells assessed as total apoptotic cells at 1 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry analysis relative to control2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1128978Inhibition of human HDAC-1 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1339569Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID760509Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID663354Growth inhibition of human NCI-H322M cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1164913Inhibition of HDAC8 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1482099Inhibition of HDAC 3 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1330947Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1547261Inhibition of human recombinant His-tagged BRD2 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1548289Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID663348Growth inhibition of human SR cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID723120Potentiation of 20 uM cisplatin-induced toxicity in 5 uM cisplatin resistant human A2780 cells at 0.25 uM pretreated for 48 hrs followed by 5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1245687Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID297494Cytotoxicity against human Saos2 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1771456Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1861266Selectivity index, ratio of IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID420329Inhibition of HDAC from RT extract2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1462219Inhibition of human BRD4 bromo domain 2 at 0.5 uM2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1890312Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1361653Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1587866Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1819533Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as glomerular structure damage in kidney at 60 mg/kg, IG administered for 12 days H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1655789Inhibition of human recombinant HDAC3 using AMC-K(Ac)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1873400Inhibition of HDAC1 (unknown origin) preincubated for 30 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1515906Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID527317Inhibition of HDAC in human HeLa cell nuclear extracts by fluorimetric assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
AID1487038Inhibition of HDAC in human HeLa-S3 cells lysates assessed as remaining enzyme activity at 2 x 10'-7 M pre-incubated for 15 mins before HDAC-Glo I/II substrate addition and measured after 30 mins post substrate addition2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1550105Inhibition of HDAC1 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID348801Inhibition of HDAC52008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID760491Cytotoxicity against human SW620 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1702057Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID673992Inhibition of recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1361649Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1234894Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1482101Inhibition of HDAC 4 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1785021Metabolic stability in rat liver microsomes assessed as parent compound remaining at 10 ug/ml measured after 1 hr in the presence of NADPH by HPLC analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1865298Toxicity in BALB/c mouse allografted with mouse 4T1 cells assessed as body weight loss at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1511134Inhibition of HDAC4 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1597970Induction of cell cycle arrest in human A549 cells assessed as accumulation at S phase at 10 uM incubated for 36 hrs by propidium iodide staining based flow cytometry (Rvb = 16.66%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1486672Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1848579Inhibition of HDAC6 in human NCI-H522 cells assessed as increase in acetylation of tubulin at 2.5 to 10 uM measured for 3 days by Western blot analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1174691Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1336949Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G2 phase at 2.5 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.08%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID269668Inhibition of HeLa cell HDAC2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID663335Growth inhibition of human SW620 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1605968Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1246507Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1825923Inhibition of recombinant human full length C-terminal His/FLAG tagged HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
AID1784981Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1784978Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1630599Inhibition of recombinant full length C-terminal His-tagged human HDAC3/GST-tagged human Ncor2 (395 to 489 residues) expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID316907Inhibition of human RFX631L cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1623532Inhibition of HDAC10 (unknown origin) by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1847777Inhibition of HDAC1 in human HeLa cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID1282279Antitumor activity against human HCT116 cells xenografted in Balb/c nude mouse assessed as tumor mass change at 100 mg/kg, po q2d for 8 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID269671Antiproliferative activity against human LOX-IMVI cells by SRB assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1433234Induction of cell death in p53 null human U937 cells at 1 to 4 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID420517Inhibition of HDAC in human IGROV1 cells assessed as histone-H4 acetylation at IC80 after 4 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1380955Inhibition of HDAC6 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1421921Selectivity index, ratio of IC50 for human HepG2A16 cells to IC50 for exo-erythrocytic stage of GFP-Luc-fused Plasmodium berghei ANKA infected in human HepG2 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID385231Inhibition of HDAC92008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
AID775828Inhibition of TPCK-treated trypsin (unknown origin) at 10 uM preincubated for 10 mins prior to substrate addition measured for 30 mins by spectrophotometric analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1339570Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID1493592Inhibition of human recombinant full-length C-terminal GST-tagged HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID1783108Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.
AID1861344Inhibition of HDAC in human DOHH-2 cells assessed as effect on pS6 levels at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID1865266Inhibition of recombinant human HDAC7 using Ac-LeuGlyLys (TFA)-AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1464876Anti-proliferative activity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID603218Inhibition of HDAC in human HeLa cell extracts assessed as conversion of dithiothreitol to dithiol after 1 hr by Flour-de-Lys assay2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.
AID1441647Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in TNFalpha mRNA level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1476148Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID481560Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1864227Inhibition of full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID482955Thermodynamic solubility at pH 7.42010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID663373Growth inhibition of human SF295 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1275591Inhibition of human recombinant HDAC2 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
AID749389Inhibition of human recombinant HDAC3 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
The discovery of colchicine-SAHA hybrids as a new class of antitumor agents.
AID1697196Inhibition of HDAC in human HeLa nuclear extract using fluoroscence-labeled acetylated peptide as substrate by fluorometric assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID1600661Antiproliferative activity against human OE19 cells assessed as reduction in cell viability incubated for 72 hrs by presto blue assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID300832Inhibition of HDAC in HeLa cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID673998Growth inhibition of human HL60 cells after 72 hrs by XTT assay2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID753166Cytotoxicity against human K562 cells2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID618100Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as mouse survival at 200 mg/kg, po QD for 21 days measured on day 222011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1533326Inhibition of full length human N-terminal FLAG-tagged HDAC6 (1 to 1215 residues) expressed in HEK293 cells preincubated for 15 mins followed by acetyl-Gly-Ala-[acetyl-Lys]-AMC substrate addition measured after 30 mins by fluorimetric method2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
AID476648Therapeutic ratio, EC50 for human PBMC to EC50 for human 937 cells2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1821274Inhibition of HDAC8 (unknown origin) incubated for 30 mins by microplate reader assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID525009Inhibition of HDAC7 in human CFBE41o- cell line assessed as increase in stabilization of Fdelta508 CFTR protein at 1 uM after 5 days pretreatment by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1266819Inhibition of HDAC6 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID663394Growth inhibition of human MCF10A cells after 48 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1248349Inhibition of human full length MMP2 using Mca-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to testing measured for 15 mins by fluorometric analysis2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID1709358Induction of apoptosis in human Jurkat cells assessed as viable cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 85.2%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1855246Binding affinity to calf thymus DNA at 50 uM incubated for 30 mins and measured by UV-vis absorption spectroscopy2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1566812Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1337292Antiproliferative activity against mouse TAMH cells after 24 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1201652Antiproliferative activity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1848280Inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID622259Inhibition of HDAC3 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID1655791Inhibition of human recombinant HDAC5 using AMC-K(TFA)GL as substrate by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID465150Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID297492Cytotoxicity against human A431 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1600730Inhibition of C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further 2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1126991Induction of apoptosis in human U937 cells assessed as necrotic cells using annexin-V/propidium iodide staining at 1 uM after 12 hrs by flow cytometry analysis (Rvb = 0.17%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID366643Inhibition of HDAC8 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1454056Growth inhibition of human A2780 cells after 3 days by WST1 assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1861261Inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1401474Selectivity ratio of IC50 for HDAC1 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1127010Induction of apoptosis in human U937 cells assessed as early apoptotic cells using annexin-V/propidium iodide staining at 0.125 uM after 24 hrs by flow cytometry analysis (Rvb = 1.57%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1890341Antitumor immunity in C57BL/6 mouse xenografted with mouse CT26 cells assessed as decrease in number of CD4+CD25+ CD127- T regulatory cells at 100 mg/kg, po administered once daily for 21 days measured by flow cytometry analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1915551Antiproliferative activity against non-small cell lung cancer cell line (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1825804Toxicity in ip dosed BALB/c mouse assessed as maximum tolerated dose measured after 2 weeks2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of a Novel, Small-Molecule Brain-Penetrant Histone Deacetylase Inhibitor That Enhances Spatial Memory Formation in Mice.
AID350730Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID1566825Antiproliferative activity against human AML patient derived primary leukemia cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1235112Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1280278Inhibition of class1 HDAC in human HL60 cells assessed as ratio of acetylated histone H3 to GAPDH level at 10 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1227029Inhibition of human recombinant HDAC1 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1548271Induction of cell cycle arrest in human RPMI8226 cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 48.6%)
AID1819527Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID414720Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1459945Inhibition of HDAC activity in human HeLa cell nuclear extract using fluorometric substrate measured after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1200988Oral bioavailability in ICR mouse at 50 mg/kg2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1600728Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation fo2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID525007Inhibition of HDAC7 in Fdelta508 CFTR-expressing human CFBE41o- cell line assessed as increase in cAMP-stimulated iodide efflux in at 5 uM after 24 hrs relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID632971Cytotoxicity against human SW620 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1739583Inhibition of HDAC6 in human THP-1 cells assessed as ratio of acetylated H3/GAPDH at 1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1336954Inhibition of HDAC in human BEAS2B cells assessed as reduction of NTHi-induced NFkappaB activation at 1 uM preincubated for 1 hr followed by NTHi stimulation for 5 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID618181Antitumor activity against human A2780 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 200 mg/kg, po qd for 21 days measured on day 92011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID613295Antiproliferative activity against human HCT116 cells assessed as growth inhibition2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1848633Cytotoxicity against human UO-31 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1466060Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID619260Antitumor activity against human HCT116 cells xenografted in athymic nu/nu Harlan mouse assessed as tumor growth inhibition at 200 mg/kg, po qd for 21 days measured on day 222011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1686358Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
AID1292166Induction of apoptosis in human HCT116 cells assessed as apoptotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometric analysis2016European journal of medicinal chemistry, Jun-10, Volume: 115Novel spiropyrazolone antitumor scaffold with potent activity: Design, synthesis and structure-activity relationship.
AID1898908Antiproliferative activity against human THP-1 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID605395Inhibition of human recombinant HDAC5 using fluor de Lys as substrate by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1293571Inhibition of human HDAC10 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1826622Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 1.11 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID481569Antitumor activity against mouse S180 cells xenografted in ICR mouse assessed as inhibition of tumor weight at 100 mg/kg, ig administered 2 days after tumor inoculation qd for 7 days relative to control2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1227050Cytotoxicity against mouse NIH/3T3 cells assessed as cell proliferation after 70 hrs by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1739590Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated H3/GAPDH at 0.1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1578484Cytotoxicity against human MRC9 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1599768Inhibition of HDAC6 in human Meso163 cells assessed as increase in alpha tubulin acetylation at 2.5 uM measured after 6 to 20 hrs by Western blot analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1421910Selectivity index, ratio of IC50 for human HepG2A16 cells to IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1550095Inhibition of recombinant human JAK2 at 10 uM using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1848281Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID1275647Cytotoxicity against HEK293 cells assessed as growth inhibition after 96 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID420510Cell cycle arrest in human IGROV1 cells assessed as accumulation at sub-G1 phase at IC80 after 24 hrs using propidium-iodide staining by flow-cytometry2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1275639Inhibition of recombinant human HDAC11 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID274110Inhibition of HDAC1 (mean IC50)2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
A series of novel, potent, and selective histone deacetylase inhibitors.
AID1915574Inhibition of HDAC1 in human HeLa cell nuclear extract using Bos-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition incubated for 30 mins2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1401541Antiproliferative activity against human JeKo1 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1129797Inhibition of HDAC in human Jurkat cells assessed as perforin expression after 48 hrs by FACS flow cytometric analysis relative to control2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1355691Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1282298Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1421625Antiproliferative activity against human HEL 92.1.7 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1865251Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SHP099 by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID765206Cytotoxicity against human H69 cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID619042Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1128555Inhibition of human HDAC-2 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1280306Inhibition of human KDAC12016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1623527Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1379289Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
AID1704066Inhibition of human C-terminal Flag tagged HDAC1 (1 to 482 residues) expressed in SF9 cells using Ac-peptide substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by microplate reader method2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID461268Antiproliferative activity against human SCC25 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1769655Antiproliferative activity against human SKNBE2 cells harboring wild type ALK assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1633676Neuroprotective activity against low serum/K+ deprivation-induced toxicity in rat CGN cells assessed as increase in cell viability at 5 to 25 uM pre-treated for 6 hrs followed by 24 hrs co-treatment with serum/K+ starvation and measured after 24 hrs by MT2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1337280Antiproliferative activity against human Jurkat cells2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1875508Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID1464875Anti-proliferative activity against human HCT116 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID375039Toxicity in ip dosed BALB/c nu/nu mouse assessed as maximum tolerated dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1339578Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID1614253Antitumor activity against human MM1S cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 50 mg/kg, iv qd administered for 10 days and measured every 2 days post last dose by caliper method relative to control
AID1655896Inhibition of HDAC6 in human RH4 cells assessed as acetylated alpha-tubulin level at 0.15 uM incubated for 72 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1752942Selectivity index, ratio of IC50 for cytotoxicity against human HepG2-A16-CD81EGFP cells to IC50 for antiplasmodial activity against drug-sensitive asexual intraerythrocytic stage of Plasmodium falciparum 3D7 infected in human O+ erythrocytes
AID1486324Genotoxicity in Salmonella typhimurium TA1535 at 50 times antiproliferative IC50 by Ames test2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1511139Inhibition of HDAC10 (unknown origin) using Ac-ArgThr- Lys(Ac)Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID322420Cell cycle arrest in human LNCap cells assessed as accumulation at G2/M phase relative to control at 1 uM2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID1441645Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in neutrophil infiltration by measuring MPO activity at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1215095Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay relative to SR128132011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1690103Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID1462221Inhibition of recombinant human HDAC1 after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1128556Inhibition of human HDAC-3/NCOR-2 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID347808Inhibition of human HDAC12008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1535340Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.
AID546546Inhibition of HDAC assessed as histone H3K'9+14 acetylation levels by cell based histone H3 hyperacetylation assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID105421Inhibitory concentration against MDA-435 cells proliferation2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1248354Inhibition of porcine kidney microsomal APN using L-Leu-para-nitroanilide as substrate at 10 uM incubated for 2 hrs prior to substrate addition measured after 30 mins by plate reader analysis relative to control2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
AID1263143Antagonist activity at ERalpha in human T47D-KBLuc cells assessed as inhibition of E2-induced transcriptional activity by luciferase reporter gene assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1066166Cytotoxicity against human LNCAP cells at 50 uM after 72 hrs2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
AID1897384Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID1503842Selectivity index, ratio of IC50 for recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells to IC50 for recombinant human full length HDAC6 expressed in baculovirus infected Sf9 insect cells2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
AID1742745Genotoxicity in Salmonella typhimurium WP2 uvrA (pKM 101) by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1383991Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1454679Decrease in alcohol intake in C57BL/6J mouse at 50 mg/kg, ip relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1487017Inhibition of HDAC3 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID527321Growth inhibition of human HUT78 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
AID1434357Growth inhibition of human NCI-H23 cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1821961Inhibition of full length recombinant human C-terminal His tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-GlyLys (Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluo
AID1849166Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1547256Inhibition of human recombinant His-tagged BRDT BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1885254Inhibition of KDM4E (unknown origin)2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID1832688Inhibition of human HDAC4 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID637887Inhibition of Bordetella FB188 HDAH using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases.
AID1164034Inhibition of human recombinant HDAC11 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1677495induction of apoptosis in siRNA-induced BAX knock down human HeLa cells at 0.3 to 3 uM after after 48 hr by annexin V FITC and propidium iodide staining based flow cytometric analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1165105Antileishmanial activity against axenic amastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1707466Synergistic antifungal activity against Candida albicans 0304103 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = >64 ug/ml)2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID420638Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC80 after 24 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1065635Inhibition of human recombinant HDAC9 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1529549Induction of apoptosis in human BL2 cells assessed as late apoptotic cells at 10 nM after 48 hrs by annexin V-FITC/propidium iodide double staining-based flow cytometry (Rvb = 2.1%)2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1819546Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as fold increase in CD86 expression by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1578903Induction of apoptosis in human Bel7402 cells assessed as increase in cleaved caspase-3 level at 5 uM after 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1401555Antiproliferative activity against human MM473 cells at 10 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID481567Antitumor activity against mouse S180 cells xenografted in ICR mouse assessed as reduction of tumor weight at 100 mg/kg, ig administered 2 days after tumor inoculation qd for 7 days2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1653098Antiproliferative activity against human PC3 cells by CCK8 assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1266811Antiproliferative activity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1775564Inhibition of full length human C-terminal His-tagged HDAC2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1250643Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1380968Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1380949Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1873384Inhibition of HDAC4 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID373084Antitumor activity in mouse P388 cells xenografted B6D2F1 mouse assessed as increase in life span at 20 mg/kg/day, ip administered 3 to 7 days postxenografting2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1441649Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 mRNA level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1280277Inhibition of HDAC6 in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 0.1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1898904Antiproliferative activity against human L-428 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID274037Hepatocyte stability2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID90680Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID1727731Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1709353Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human Jurkat cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1865242Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID352518Inhibition of human recombinant HDAC62009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1702089Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID613340Antiproliferative activity against human H1299 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1697200Inhibition of HDAC2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID1865244Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID343690Inhibition of HDAC in human HeLa cells2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
AID1401554Antiproliferative activity against human MM432 cells at 10 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1234891Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC1 (unknown origin)2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1591853Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1413071Antiproliferative activity against human SKOV3 cells at 10 uM measured every 2 hrs for 200 hrs by IncuCyte ZOOM cell confluence assay2018MedChemComm, Jun-01, Volume: 9, Issue:6
Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition.
AID1864219Binding affinity to 5' FAM-labeled c-myc G4-quadruplex DNA Pu22 (unknown origin) at 50 uM by fluorescence quench assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1707464Antifungal activity against Candida albicans 0304103 incubated for 48 hrs by microdilution assay2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID1326519Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1702061Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1811362Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID545890Specificity index, ratio for IC50 for human HDAC in HeLa cells to IC50 for HDAC in Plasmodium falciparum 3D72009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1543951Induction of apoptosis in human Bel7402/5-FU cells assessed as early apoptotic cells at 5.0 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 3.60%)2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1861262Inhibition of HDAC8 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID482965Apparent permeability from apical to basolateral side of Caco-2 cells2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1415657Binding affinity to calf thymus DNA assessed as decrease in maximum absorption wavelength by UV-Vis spectroscopic titration method2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1764256Induction of histone H-3 expression in human CAL-27 cells for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1469310Induction of apoptosis in human T47D cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.8%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1548261Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay
AID1336927Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1126963Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC3 (unknown origin)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1697203Induction of apoptosis in human SW620 cells assessed as early apoptotic cells by flow cytometry2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID134163Antitumor activity against HT1080 cell line in mouse xenograft model after orally dosed once every other day at 100 mg/kg2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
AID1542185Inhibition of HDAC7 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1873409Inhibition of HDAC3 (unknown origin) preincubated for 5 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1873408Inhibition of HDAC2 (unknown origin) preincubated for 120 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID669759Growth inhibition of human PC3 cells after 48 hrs by SRB assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1073051Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
AID1688036Induction of apoptosis in human HL-60 cells assessed as late apoptotic cells at 1 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 7.24 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1742685Induction of cell cycle arrest in mouse 4T1 cells assessed as S phase accumulation at 2 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 19.43 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1702063Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 (627 to 1084 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1060990Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors.
AID1141770Cytotoxicity against human TSGH cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1177047Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID300835Growth inhibition of human NCI-H23 cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID438216Inhibition of HDAC1/2 from human HeLa cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
AID605541Antiproliferative activity against human U937 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1164031Inhibition of human recombinant HDAC9 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1898981Induction of cell cycle arrest in human H460-R9A cells assessed as accumulation of cells at S phase at 1.9 uM after 72 hrs by flow cytometry (Rvb = 34.5%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID723463Inhibition of human HDAC5 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1605969Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1251322Growth inhibition of human H460 cells after 72 hrs2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1518780Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1848623Cytotoxicity against human HT-29 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID591326Inhibition of HDAC in human HeLa cells at 0.1 uM by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.
AID1547260Inhibition of human recombinant His-tagged BRD3 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1348936Effect on TIMP3 gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1401484Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1861259Inhibition of HDAC3 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1384232Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level after 2 hrs by Western blot analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1401373Inhibition of HDAC2 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1127318Inhibition of HDAC2 in human HeLa cells using KI-104 as substrate after 40 mins by fluorescence analysis2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1126988Inhibition of HDAC3 in human U937 cells assessed as increase of intracellular acetylated histone H4 level at 1 uM after 24 hrs by Western blot analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1067346Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1704069Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID1821957Inhibition of HDAC in human HeLa nuclear extracts using fluorometric substrate incubated for 30 mins by fluorescence plate reader analysis
AID1478600Inhibition of Class 2a histone deacetylase in human K562 cells using Boc-Lys-(epsilon-trifluoromethylacetyl)-AMC as substrate preincubated with compound for 3 hrs followed by substrate addition measured after 3 hrs by fluorometric analysis2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1622977Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 3 hrs and measured after 35 min2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1915572Inhibition of EGFR (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID288453Growth inhibition of human MDA-MB-231 cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID1246526Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human U937 cells2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1487013Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC8 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1282290Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as death at 50 mg/kg, ip q2d for 12 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1751996Inhibition of HDAC8 (unknown origin)2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
AID366648Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1260646Inhibition of human recombinant HDAC10 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1260639Inhibition of human recombinant HDAC3 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1550126Induction of apoptosis in human K562 cells assessed as viable cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 85.7%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1754768Downregulation of SIRT1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID373082Inhibition of human recombinant HDAC92009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1898979Induction of cell cycle arrest in human H460-R9A cells assessed as accumulation of cells at sub-G1 phase at 1.9 uM after 72 hrs by flow cytometry (Rvb = 1.5%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1129008Inhibition of human HDAC-6 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1466063Inhibition of recombinant human full length HDAC6 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID482958Half life in mouse liver microsome2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1547246Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1848634Cytotoxicity against human Hs578Bst cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1901161Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1164770Antitumor activity against human A2780 cells xenografted in athymic nude mouse assessed as tumor volume inhibition at 100 mg/kg, po qd for 5 days a week for 2 weeks2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1141798Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin)2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID404451Antimalarial activity against Plasmodium falciparum TM90C2A by hypoxanthine uptake2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1326512Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID734728Inhibition of HDAC6 in human LNCAP cells assessed as increase in tubulin polymerization after 4 hrs by Western blotting analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1349724Inhibition of HDAC2 (unknown origin)2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID615999Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.
AID1784969Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1826632Synergistic antiproliferative effect on HEL cells assessed as combination index at 0.12 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1742648Induction of apoptosis in human MDA-MB-231 cells xenografted in BALB/c mouse assessed as increase in caspase-3 cleavage by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1731758Inhibition of recombinant human HDAC7 using Ac-LGK(TFA)-AMC as substrate pre-incubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
AID1873412Inhibition of HDAC3 (unknown origin) preincubated for 90 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1181306Inhibition of HDAC1 in human U937 cells assessed as increase in acetyl-histone H3 level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1225987Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 8%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1225989Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.03%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID765377Inhibition of recombinant human HDAC5 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1206743Cytotoxicity against human ES2 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID605539Antiproliferative activity against human MOLT4 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID274069Bioavailability after i.p. dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID672032Ratio of IC50 for human HDAC1 preincubated for 3 hrs to IC50 for human HDAC1 preincubated for 5 mins2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1449322Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID366650Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID80246Inhibitory activity against HCT116 human colon cell growth2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID1699974Inhibition of recombinant human HDAC8 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1737153Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 5.14%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1861252Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 7 days2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID1056037Antiproliferative activity against human A549 cells after 48 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Total synthesis of schizocommunin and revision of its structure.
AID1164175Cell cycle arrest in human K562 cells assessed as block at G2-M phase at 40 uM after 24 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1250653Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1162218Cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 1 uM by propidium iodide staining-based flow cytometry (Rvb = 58.9%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID1389960Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.
AID1234900Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1266835Induction of caspase-3 cleavage in human HCT116 cells at 1 to 5 uM after 48 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1737135Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in sf9 insect cells using Boc-Lys(TFA)-AM as substrate incubated for 60 mins by fluorescence assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID519583Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID382343Viability of human DU145 cells after 72 hrs by trypan blue staining2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
AID90520Inhibition of in vitro enzyme activity measured in partially purified rat liver Histone deacetylase preparation2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID1281854Antiproliferative activity against human LP-1 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1542179Inhibition of HDAC1 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1762492Inhibition of N-terminal GST-tagged full length human HDAC6 expressed in baculovirus-infected Sf9 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based 2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1401533Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1821959Inhibition of recombinant human His-tagged HDAC3 expressed in baculovirus insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader ass
AID1848566Ratio of IC50 for cytotoxicity against human RPE cells to IC50 for cytotoxicity against human HCT-116 cells2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1898924Antiproliferative activity against human NCI-H460 cells at 7.4 uM assessed as reduction in p-ERK1/2 level and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID90665Inhibitory activity against human Histone deacetylase 12004Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
On the function of the 14 A long internal cavity of histone deacetylase-like protein: implications for the design of histone deacetylase inhibitors.
AID1915525Antiproliferative activity against human PC-3 cells incubated for 48 hrs by Sulforhodamine B staining method2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID760520Cytotoxicity against human SK-BR-3 cells after 72 hrs by WST1 assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1282232Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1384234Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1449217Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID1898982Induction of cell cycle arrest in human H460-R9A cells assessed as accumulation of cells at G2/M phase at 1.9 uM after 72 hrs by flow cytometry (Rvb = 15.4%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID473029Ex vivo inhibition of human HDAC1 in human Caco-2 cells by fluorometric cellular activity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1549139Antifungal activity against azole-resistant Candida albicans 4108 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID525022Inhibition of HDAC in human CFBE41o- cell line assessed as increase in total CFTR protein level including CFTR glycoform at 0.1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1901765Selectivity ratio of IC50 for full length human recombinant HDAC8 to IC50 for full length human recombinant HDAC62022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1550150Antitumor activity against HEL cells xenografted in BALB/c nu mouse assessed as reduction in tumor volume at 100 mg/kg/day, ip administered for 16 days and measured every 3 days during compound dosing by caliper method relative to control2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1848592Induction of cell cycle arrest in human NCI-H522 cells assessed as accumulation at S phase 5 uM incubated for 24 to 72 hrs by PI staining based flow cytometric analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1459955Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1459956Selectivity ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC62017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1742758In vivo inhibition of STAT-3 in tumor of human MDA-MB-231 cells xenografted in BALB/c mouse assessed as decrease in STAT-3 phosphorylation by immunohistochemistry method2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1832684Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1401591Resistance index, ratio of IC50 for human A2780/DX cells to IC50 for human A2780 cells2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID618184Toxicity in nude BALB/c mouse xenografted with human A2780 cells assessed as maximum body weight loss at 200 mg/kg, po QD for 21 days measured on day 132011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1055355Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID723154Potentiation of 1 uM cisplatin-induced toxicity in 0.5 uM cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by 0.5 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID90672Inhibitory activity against maize Histone deacetylase 1-B2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1548727Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID765204Cytotoxicity against human Hep3B cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID273180Cell cycle arrest in U937 cells by accumulation at S/G2/M phase at 5 uM after 48 hrs2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID663474Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1260640Inhibition of human recombinant HDAC4 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID328797Inhibition of HDAC4 gain-of-function phenotype expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1139706Inhibition of HDAC in human HeLa cell nuclear extract using acetylated lysine as substrate after 30 mins by spectrophotometric analysis2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.
AID1067344Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1765322Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1454681Decrease in alcohol intake in C57BL/6J mouse at 100 mg/kg, ip relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1548275Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay
AID1811393Toxicity in Balb/c mouse xenografted with human MCF7 cells assessed as change in organ morphology at 50 mg/kg, po administered 3 times week for 21 days by H and E staining based analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID1282277Antitumor activity against human HCT116 cells xenografted in Balb/c nude mouse assessed as tumor mass change at 50 mg/kg, ip q2d for 9 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1250642Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1141767Cytotoxicity against human HONE1 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID663363Growth inhibition of human IGROV1 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1777025Inhibition of HDAC in human A549 cells assessed as reduction in fluorescent APS probe fluorescence intensity at 10 uM preincubated with compound for 2 hrs followed by co-incubation with APS probe for 1 hr by flow cytometry2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase.
AID481570Antitumor activity against mouse S180 cells xenografted in ICR mouse assessed as inhibition of tumor weight at 200 mg/kg, ig administered 2 days after tumor inoculation qd for 7 days relative to control2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID273173Inhibition of mouse HDAC12006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1251315Inhibition of human HDAC2 after 40 mins by fluorescence analysis2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1783092Inhibition of HDAC in Candida tropicalis 5008 using Boc-Lys(Ac)-AMC as substrate preincubated with protoplast for 12 hrs followed by incubation with substrate for 6 hrs by fluorimetric assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1699971Resistance index, ratio of of IC50 for human K562/A02 cells to IC50 for human K562 cells2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID603530Cytotoxicity against human A549 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1514600Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H3 levels at 2.5 uM by Western blot analysis relative to beta-actin (Rvb = 0.5 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1549164Inhibition of HDAC1 (unknown origin) after 30 mins by fluorescence based assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1819517Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1856995Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1266834Induction of PARP cleavage in human HCT116 cells at 1 to 5 uM after 48 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1398808Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin expression after 8 hrs by Western blot analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID316873Inhibition of human HT1080 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1821960Inhibition of recombinant human N-terminal GST tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence mic
AID316925Inhibition of human HepG2 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1168915Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif.
AID1274880Inhibition of HDAC10 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1653144Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID331900Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID1833070Antiangiogenesis activity in human Endothelial progenitor cell assessed as inhibition of cell growth measured for 48 hrs2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID1861651Antiproliferative activity against human A549 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1337308Inhibition of HDAC6 in HEL 92.1.7 cells harboring JAK2 V617F mutant assessed as increase in acetylated tubulin level at 0.1 uM after 1 hr by immunoblot method2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1406989Inhibition of HDAC6 in human U87 cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1482123Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1707467Synergistic antifungal activity against Candida albicans 0304103 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID1888588Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
AID395031Toxicity in ip dosed athymic mouse assessed as maximum tolerated dose2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
AID1263061Inhibition of NTHi-induced NF-kappaB activation in human BEAS-2B cells at 1 uM treated 1 hr before NTHi stimulation measured after 5 hrs by luciferase assay relative to control2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.
AID1707508Inhibition of human HDAC6 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.
AID1566815Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID619053Competitive inhibition of HDAC8 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1688041Induction of apoptosis in human HL-60 cells assessed as necrotic cells at 2 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 1.01 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1206751Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 0.5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 47.87%)2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1550106Inhibition of HDAC3 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1266100Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID723468Inhibition of HDAC in cisplatin sensitive human KYSE-510 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1280260Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID456798Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID755621Cytotoxicity against human GBC-SD cells assessed as growth inhibition after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1269325Cytotoxicity against human A549 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID775831Inhibition of HDAC2 (unknown origin)-mediated deacetylation at 10 uM preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1622932Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf21 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID461263Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1065971Inhibition of HDAC1 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID499803Selectivity ratio IC50 for HDAC6 to IC50 for HDAC in human HeLa cells nuclear extract2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1379285Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as increase in acetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
AID1819532Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as lung damage at 60 mg/kg, IG administered for 12 days H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID609494Inhibition of CYP3A42011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1398812Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYC mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1547284Effect on histone H3 expression level in human HCT116 cells measured after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1861342Inhibition of HDAC in human DOHH-2 cells assessed as effect on pS6 levels at 2.5 uM measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID527040Cytotoxicity against human NCI-H1299 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1765332Selectivity index, ratio of IC50 for human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1558002Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
AID1811392Toxicity in Balb/c mouse xenografted with human MCF7 cells assessed as body weight loss at 50 mg/kg, po administered 3 times week for 21 days in presence of fulvestrant2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID755618Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1441643Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in total number of leucocytes in BALF at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID273176Induction of granulocytic differentiation of U937 cells measured as CD11c expression level after 48 hrs at 1 uM2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1394884Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1401538Antiproliferative activity against human A2780/DX cells after 72 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1572344Inhibition of recombinant human HDAC8 expressed in baculovirus expression system using fluorogenic Arg-His-Lys(Ac)-Lys(Ac) as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1275635Inhibition of recombinant human HDAC2 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID324950Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1775565Inhibition of full length human C-terminal His-tagged HDAC3/human N-terminal GST-agged NCOR2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID1399813Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
AID1431822Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1466066Inhibition of HDAC in human PC3 cells assessed as increase in alpha-tubulin acetylation at 1 uM after 24 hrs by Western blot analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1863435Inhibition of HDAC3 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID723433Potentiation of 2.5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1330944Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1547333Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in LIF mRNA level at 10 uM after 24 hrs by RT-PCR analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1439350Inhibition of full length recombinant human GST fused His6-tagged HDAC6 expressed in baculovirus infected High5 cells using Boc-Lys(epsilon-acetyl)-AMC as substrate measured after 3 hrs2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID316927Inhibition of human CCD1059SK cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID499809Antimalarial activity against Plasmodium falciparum D6 after 72 hrs by alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID669756Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID90696Inhibition of maize histone deacetylase 22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID1127006Induction of apoptosis in human U937 cells assessed as early apoptotic cells using annexin-V/propidium iodide staining at 0.25 uM after 24 hrs by flow cytometry analysis (Rvb = 1.57%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1164177Cell cycle arrest in human MCF7 cells assessed as block at G2-M phase at 5 uM after 24 to 96 hrs using propidium iodide staining by FACScan flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1622985Inhibition of HDAC6 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID748981Inhibition of HDAC6 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1819548Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as fold reduction in Treg cells in spleen by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID618016Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c nu mouse assessed as tumor growth inhibition at 90 mg/kg, ip qd for 19 days relative to control2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1633426Cytotoxicity against human SH-SY5Y cells at 10 uM incubated for 24 hrs by MTS assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID274095Inhibition of mouse HDAC1 (mean)2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID663402Lipophilicity, log D of the compound in pH 7.4 PBS buffer2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID723147Potentiation of 40 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human MDA-MB-231 cells at 0.5 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1282302Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1754764Downregulation of HDAC7 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID723464Inhibition of human HDAC4 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1550119Induction of apoptosis in HEL cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 12.5%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1281855Antiproliferative activity against human Mino cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1177046Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1129790Induction of apoptosis in human Jurkat cells assessed as late apoptotic cells at 10 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based FACS flow cytometric analysis (Rvb = 0.0401%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1451830Inhibition of human recombinant HDAC6 expressed in Baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID1754790Downregulation of HDAC8 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1898910Antiproliferative activity against human MDA-MB-436 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1846147Inhibition of HDAC (unknown origin) incubated for 30 mins by ELISA method2021Bioorganic & medicinal chemistry letters, Apr-15, Volume: 38Current status in the discovery of dual BET/HDAC inhibitors.
AID499810Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID420639Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC80 after 48 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1784979Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1141765Cytotoxicity against human HCT116 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1720111Cytotoxicity against human MCF7 cells assessed as reduction in cell viability in presence of erlotinib by MTT assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
AID1759726Fraction unbound in rat plasma2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
AID1482170Cytotoxicity against human Caco2 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1550101Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1890512Inhibition of HDAC3 (unknown origin)2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1467235Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 0.02 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured within 30 mins by fluorom2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID503691Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 8 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1771457Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID519597Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-resistant Plasmodium falciparum Dd22008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1469298Induction of apoptosis in human NCI-H460 cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1572353Ratio of inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 10 uM to inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 10 uM2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1421914Inhibition of HDAC in synchronized trophozoite stage Plasmodium falciparum 3D7 infected in human erythrocytes assessed as increase in acetylated H2B/H2Bv level at 5 times IC50 after 3 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1890321Inhibition of HDAC1 in mouse B16 cells assessed as accumulation of acetylated H3 level at 6 uM after 24 hrs by Western blotting analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID541648Inhibition of human HDAC4 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1869147Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
AID352521Antiproliferative activity against human BxPC3 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1164903Inhibition of HDAC1/2/3 in human HeLa cells assessed as p21 gene expression at 3 uM after 15 hrs by luciferase reporter gene assay relative to SNDX-2752014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1605967Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1622933Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID461265Antiproliferative activity against human MDA-MB-468 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1655900Inhibition of EZH2 in human RH4 cells assessed as H3K27me3 level at 0.15 uM incubated for 72 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1758463Phototoxicity in human A549 cells assessed as reduction in cell viability irradiated 10 j/cm2 for 24 hrs followed by incubated for 24 hrs by CCK8 assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID395023Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
AID1855253Downregulation of SSRP-1 expression in human HCT-116 cells at 1.5 uM measured after 24 hrs by Western blot analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID461301Antitumor activity against human HepG2 cells xenografted in nude CD1 mouse at 72 mg/kg, iv daily relative to control2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1380939Inhibition of VEGFR-2 (unknown origin) at 0.2 uM after 40 mins by kinase-Glo assay relative to control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1543957Induction of apoptosis in human Bel7402/5-FU cells assessed as necrotic cells at 5.0 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 2.27%)2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1762491Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus-infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic 2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1396990Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
AID1126983Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1462025Antiproliferative activity against human U266 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability.
AID1758468Inhibition of human recombinant HDAC6 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1702139Inhibition of PI3K/AKT/mTOR signaling in human HuH-7 cells assessed as PS6 Ser240/244 phosphorylation level at 10 uM incubated for 4 hrs including last 12 mins stimulation with 20 ng/ml growth factor VEGF by Western blot analysis (Rvb = 100 %)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1901766Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1865268Inhibition of recombinant his-tagged human HDAC10 using Ac-ArgHisLys (Ac) Lys (Ac)-AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1441658Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction MPO activity at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID465155Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID723469Inhibition of HDAC in cisplatin resistant human CAL27 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1677517Binding affinity to recombinant human full length His-tagged BAX expressed in Escherichia coli BL21 (DE3) cells preincubated for 30 min followed by FITC-BIM addition and measured after 20 mins by fluorescence polarization assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1174699Induction of apoptosis in human U937 cells assessed as early apoptotic cells at 1.5 uM after 24 hrs by annexin-V/propidium iodide staining-based flow cytometry (Rvb = 3.81%)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID618024Inhibition of MMP22011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1825881Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay
AID274022AUC after i.p. dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1256444Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.
AID1785347Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
AID1816698Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability at 10 uM after 72 hrs by CellTiter-Glo assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1667066Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1783109Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.
AID1897806Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 (1 to 1215 residues) using Z-Lys(Ac)-AMC as substrate preincubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.
AID1282237Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1394883Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID481548Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1164908Inhibition of HDAC3 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1742679Induction of cell cycle arrest in human MDA-MB-231 cells assessed as S phase accumulation at 2 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 43.82 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1890436Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID1606020Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 1 to 2 uM after 72 hrs by tryphan blue assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID310127Growth inhibition of human HCT116 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.
AID1365024Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID303349Inhibition of HDAC6 in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID1441646Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in pulmonary edema by measuring lung wet and dry ratio at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1869149Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
AID1690843Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1545756Inhibition of HDAC3 (unknown origin)2019European journal of medicinal chemistry, Dec-01, Volume: 183Indole: A privileged scaffold for the design of anti-cancer agents.
AID1753646Inhibition of HDAC6 in human SH-SY5Y cells assessed as fold increase in ratio of acetylated histone H3 to histone H3 at 1 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1227033Inhibition of human recombinant HDAC8 using MAZ1675 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID316934Inhibition of HDAC42008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1459957Selectivity ratio of IC50 for recombinant human HDAC2 to IC50 for recombinant human HDAC62017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1177044Inhibition of human HDAC3 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1337196Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1897381Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID1128563Inhibition of human HDAC-11 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1201647Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay2015European journal of medicinal chemistry, May-05, Volume: 95Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
AID1275077Inhibition of recombinant human HDAC12016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID1164188Inhibition of HDAC in human U937 cells assessed as hyperacetylation of histone H1 at Lys 9/4 residues at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1545944Antiproliferative activity against human K562 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1572350Inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 10 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID546559Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1336940Inhibition of HDAC in human LNCAP cells assessed as down regulation of COX2 expression at 10 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1764253Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1282243Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1622984Inhibition of HDAC2 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1566814Antiproliferative activity against human A2780S cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1614247Inhibition of HDAC6 in human MV4-11 cells assessed as increase in alpha-tubulin acetylation at 1 uM after 6 hrs by Western blot analysis
AID1752947Selective index, ratio of IC50 for human HepG2-A16-CD81EGFP cells to IC50 for antiplasmodial activity against liver stage exo-erythrocytic forms of Plasmodium berghei sporozoites infected in human HepG2-A16-CD81EGFP cells
AID348804Antiproliferative activity against human HCT116 cells after 72 hrs by celltiter-blue viability assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID297491Cytotoxicity against human Cal27 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1422520Inhibition of HDAC in human HeLa cell extract at 2 uM after 15 to 30 mins by COLOR DE LYS-based colorimetric method2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID525001Inhibition of HDAC2 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID503668Cytotoxicity against human GM15850 cells at 5 uM after 96 hrs by trypan blue exclusion assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1515917Antitumor activity against human HCT116 cells xenografted in athymic nude BALB/c mouse assessed as tumor growth inhibition at 100 mpk, ip measured 2 times every week relative to control2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1671981Cytotoxicity against human MCF7/ADR cells after 72 hrs by SRB assay2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID499813Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W22010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1600734Antiproliferative activity against human A2780 cells after 72 hrs by microplate reader based MTT assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.
AID1065633Inhibition of human recombinant full length HDAC6 after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1406987Inhibition of class 1 HDAC in human U87 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1550128Induction of apoptosis in human K562 cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin-V/propidium iodide staining-based flow cytometric analysis (Rvb = 5.87%)2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID750106Cytotoxicity against human MCF7 cells after 48 hrs by Sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
AID1816201Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
AID1688032Induction of apoptosis in human HL-60 cells assessed as late apoptotic cells at 0.5 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 7.24 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1282256Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1897379Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID1225975Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 2.27%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1349726Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1784986Inhibition of HDAC2 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1246515Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1511137Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1464871Inhibition of HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID663376Growth inhibition of human SNB75 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1434355Growth inhibition of human ACHN cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1759721Inhibition of class 1 HDAC in human Jurkat 2C4 model of HIV latency assessed as reactivation of HIV latency incubated for 18 to 24 hrs in presence of 0.1 % heat inactivated NHS by Steady-Glo luciferase assay2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
AID1293554Inhibition of human recombinant HDAC2 using Fluor de Lys Green as substrate incubated for 30 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1917542Inhibition of HDAC11 (unknown origin) measured by fluorescence based assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID672025Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 24 hrs measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1478583Induction of apoptosis in human K562 cells assessed as late apoptotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2.83%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1406986Inhibition of class 1 HDAC in human U87 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1537569Cell cycle arrest in human G55T2 cells assessed as accumulation in subG0 phase at 3 uM incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 4.5 %)2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1897403Induction of apoptosis in human SNU-16 cells assessed as dead cells at 0.3 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 2.65%)
AID482943Inhibition of HDAC32010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1321713Inhibition of HDAC in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 50 nM in presence of >400 nM sildenafil after 2 hrs by AlphaLisa assay relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1245684Cytotoxicity against human U937 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID652755Inhibition of recombinant human HDAC11 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1280284Cytotoxicity against human HL60 cells after 72 hrs by cell titre 96 aqueous cell proliferation assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID723432Potentiation of 2.5 uM cisplatin-induced toxicity in 1 uM cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by 1 uM cisplatin treatment by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1251320Growth inhibition of human HCT116 cells after 72 hrs2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1274874Inhibition of HDAC4 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID496808Activity of human HDAC82010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1348935Effect on TNFalpha gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID481553Cytotoxicity against human KB cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1485111Inhibition of SIRT1 in human U373 cells assessed as increase of histone H4 acetylation at 2 uM after 8 hrs by Western blotting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID488239Inhibition of HDAC6 after 10 mins by fluorometric assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1873399Inhibition of HDAC1 (unknown origin) preincubated for 5 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1548249Inhibition of HDAC6 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID288447Inhibition of LPS-stimulated TNFalpha production in RAW264.7 cells after 24 hrs by ELISA2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID1280264Selectivity ratio of IC50 for human HDAC6 to IC50 for human HDAC82016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID628450Induction of apoptosis in human HepG2 cells assessed as cleavage of caspase 3 at 1 to 10 uM after 14 hrs by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1728925Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 5 days by beckman coulter counting method2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1380950Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1876340Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID1174702Induction of apoptosis in human U937 cells assessed as viable cells at 1.5 uM after 24 hrs by annexin-V/propidium iodide staining-based flow cytometry (Rvb = 92.47%)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1478595Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1576451Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID663349Growth inhibition of human A549/ATCC cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1260653Inhibition of human recombinant HDAC1 by microplate reader assay
AID1622938Inhibition of recombinant human N-terminal FLAG-tagged HDAC10 (2 to 631 residues) expressed in baculovirus infected using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1848613Cytotoxicity against human LOX IMVI cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1810049Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay
AID1206766Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1709365Induction of apoptosis in human NAMALVA cells assessed as viable cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 90.4%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1816193Inhibition of JAK3 (unknown origin) preincubated for 60 mins followed by reagent A addition and measured after 60 mins in presence of ATP by using microplate reader method
AID663364Growth inhibition of human OVCAR3 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1401539Antiproliferative activity against human Mino cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID352751Inhibition of His-tagged HDAC8 catalytic domain expressed in Escherichia coli2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1330945Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1383995Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1652197Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1401375Inhibition of HDAC6 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1449326Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID744876Cytotoxicity against human NCI-H460 cells by MTT assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Discovery of adamantane based highly potent HDAC inhibitors.
AID621738Antiproliferative activity against human HCT116 cells by MTT assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors.
AID628448Induction of apoptosis in human HepG2 cells assessed as cleavage of caspase 3 at 1 to 10 uM after 24 hrs by Western blot analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1566811Inhibition of recombinant N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID605534Antiproliferative activity against human MG63 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1266820Inhibition of HDAC8 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID300837Growth inhibition of human LOX-IMVI cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID755625Inhibition of HDAC in human HL60 cells using Boc-Lys(Ac)-pNA as substrate at 5 umol/L incubated for 24 hrs prior to substrate addition measured after 90 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1897383Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
AID1623530Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2A by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID732151Inhibition of HDAC8 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1280263Selectivity ratio of IC50 for human HDAC6 to IC50 for human HDAC12016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1355730Toxicity in BALB/C nude mouse xenografted with human HEL cells assessed as reduction in body weight at 10 mg/kg, ip bid treated for 21 consecutive days2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID717657Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 1.25 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID747260Growth inhibition of human HT1080 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1225985Inhibition of recombinant full length human HDAC1 (1 to 482) expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID594123Inhibition of full length HDAC3/NCoR2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Discovery of histone deacetylase 8 selective inhibitors.
AID1396958Antiproliferative activity against human MDA-MB-231 cells2018Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
AID1396986Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
AID1630589Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTS-PMS assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1548274Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay
AID775827Binding affinity to human holo-transferrin assessed as pseudo-first-order rate constant measured as removal of ferric ion at 1 mM measured for 1 hr by UV-vis spectrophotometric analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID1783065Antifungal activity against fluconazole-sensitive Candida albicans SC5314 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1515907Antiproliferative activity against human U87 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1578481Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1856997Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1164190Inhibition of HDAC in human U937 cells assessed as hyperacetylation of p21 at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1380953Inhibition of HDAC2 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1441660Inhibition of LTB4 biosynthesis in LPS-induced C57BL/6 mouse model of acute lung injury BLAF at 25 mg/kg, ip by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1548285Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID1816220Induction of apoptosis in mouse 4T1 cells assessed as viable cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 89.5%)
AID1742748Antitumor activity against mouse 4T1 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 150 mg/kg, po administered for 22 days and measured on day 222020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID373083Antiproliferative activity against human HeLa cells after 4 hrs by WST-1 assay2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1263144Inhibition of human recombinant HDAC3 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1534485Inhibition of HDAC6 in mouse LL/2 cells assessed as reduction in PD-L1 expression at 10 uM after 24 hrs by Western blot analysis2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer.
AID1819500Antitumor activity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as reduction on tumor weight at 60 mg/kg, IG administered for 12 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID373087Antitumor activity in mouse P388 cells xenografted B6D2F1 mouse assessed as increase in life span at 100 mg/kg/day, ip administered 3 to 7 days postxenografting2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID1890435Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID1181314Induction of apoptosis in human U937 cells assessed as accumulation at pre-G1 phase at 5 uM after 48 hrs by propidium iodide staining based FACS method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1882978Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID492802Inhibition of human recombinant HDAC4 at 5 uM after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1821348Toxicity in mouse xenografted with human HepG2 cells assessed as necrosis in lung at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1126977Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1737145Induction of apoptosis in human HCT-116 cells assessed as viable cells at 10 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 90.34%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1622981Cytotoxicity against African green monkey Vero cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1754774Induction of apoptosis in human MCF7 cells assessed as downregulation of c-Myc protein expression at 1 to 3 uM measured after 48 hrs western blot analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1282261Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1784991Selectivity index, ratio of IC50 for cytotoxicity against human L02 cells to IC50 for antiproliferative activity against human HepG2 cells2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID414721Inhibition of wild-type c-Abl by liquid scintillation counting2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1384215Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1502984Inhibition of MAOB (unknown origin) using beetle luciferin as substrate by MAO-Glo assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1339571Inhibition of full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID1785343Inhibition of recombinant human SIRT5 measured after 30 mins by fluorescence microplate reader assay
AID1876465Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1622936Inhibition of recombinant full-length human C-terminal HDAC8 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID84266Antiproliferative activity against HT1080 (human fibrosarcoma) cell line.2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
AID1865240Induction of apoptosis in human MV4-11 cells incubated for 24 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1597953Induction of apoptosis in human A549 cells assessed as live cells at 10 uM incubated for 72 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometric analysis (Rvb = 89.8%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1849157Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1422515Inhibition of HDAC in MEF assessed as increase in histone H3 acetylation at 2 uM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Nov-05, Volume: 159In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1256443Inhibition of human HDAC in HeLa cell nuclear extract by fluorometric assay using Fluor de Lys substrate2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.
AID637891Inhibition of recombinant human HDAC8 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases.
AID1227044Stability in human plasma assessed as compound remaining after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID753167Inhibition of HDAC in human Hela cell nuclear extract after 15 mins2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.
AID1753833Inhibition of recombinant human HDAC1 at 100 nM using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay relative to control2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1266091Cytotoxicity against human MeT-5A cells2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1702103Inhibition of PI3K/AKT/mTOR signaling in human PC-3 cells assessed as reduction in phosphorylation of Akt at S473 residue at 10 uM incubated for 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID755616Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID316904Inhibition of human NCI-H226 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1816215Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 2.5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.38%)
AID1478597Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID525014Inhibition of HDAC7 in human CFBE41o- cell line assessed as increase in rate of maturation of CFTR protein to its glycoform at 5 uM after 24 hrs by pulse chase analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1502980Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1063057Inhibition of recombinant HDAC2 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1917543Selectivity index, ratio IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID1487092Inhibition of HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID519582Antimalarial activity against Plasmodium falciparum2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1272258Cytotoxicity against human MCF7 cells after 72 hrs by CCK8 assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Novel hydroxyamides and amides containing D-glucopyranose or D-fructose units: Biological assays in MCF-7 and MDST8 cell lines.
AID1676602Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1469379Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1754789Downregulation of HDAC3 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID316899Inhibition of HDAC62008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1380967Inhibition of HDAC6 in human HeLa cells assessed as increase in intracellular acetyl-tubulin levels at 100 nM after 6 hrs by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID273166Inhibition of maize HD22006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID780585Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
AID1174680Inhibition of HDAC in human HeLa cell extract using Boc-Lys (acetyl)-AMC as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by fluorescence assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID546561Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID710835Cytotoxicity against human HCT15 cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID1764288Inhibition of HDAC in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.7 uM pretreated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay (Rvb = 3.57 uM)2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1303622Potentiation of 0.05 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.25 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1406990Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID1684872Toxicity in mouse LL/2 cells inoculated C57BL/6J mouse assessed as effect on body weight by measuring end body weight at 25 mg/kg, ip administered for 12 days and measured for every 2 days (Rvb = 18.1 +/- 0.2 g)
AID628453Antiproliferative activity against human SH-SY5Y cells after 72 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID347806Inhibition of human HDAC1 at 0.50 uM2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1383990Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1418666Inhibition of recombinant human HDAC6 using fluorogenic HDAC substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence analysis2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID1597969Induction of cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 10 uM incubated for 36 hrs by propidium iodide staining based flow cytometry (Rvb = 72.51%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID519598Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID663369Growth inhibition of human SKOV3 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1055351Cytotoxicity against human HUT78 cells after 72 hrs by MTS-PMS assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID1873391Inhibition of HDAC11 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1677510Inhibition of HDAC8 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID482949Inhibition of HDAC102010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1614190Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 10.7%)
AID1421925Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1273874Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM preincubated for 10 mins measured after 30 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1502982Inhibition of recombinant LSD1 (157 to 852 amino acids) (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 substrate by amplex red and horseradish peroxidase based fluorescence assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1355716Synergistic antifungal activity against FLC resistant Candida albicans 0710922 assessed as FIC index after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1486675Inhibition of HDAC2 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1487007Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1363799Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID378556Induction of P21WAF1 gene expression in human ARP1 cells2005Journal of natural products, Mar, Volume: 68, Issue:3
4-Hydroxybenzoyl derivative from the aqueous extract of the hydroid Campanularia sp.
AID1056038Antiproliferative activity against human HeLa cells after 48 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Total synthesis of schizocommunin and revision of its structure.
AID1433251Antiproliferative activity against human CMS cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID619058Half life in mouse liver microsomes2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1065957Cytotoxicity against human Jurkat gamma1 cells assessed as growth inhibition at 20 uM after 72 hrs by MTS assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID1126965Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC1 (unknown origin)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1486293Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1578149Inhibition of HDAC1 (unknown origin)2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID683277Antiproliferative activity against human BE(2)-C cells after 72 hrs by Alamar blue assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects.
AID297473Cytotoxicity against HeLa cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1164183Inhibition of human recombinant HDAC4 using (S)-[5-Acetylamino-1-(2-oxo-4-trifluorometyl-2Hchromen-7-ylcarbamoyl)pentl]carbami acid tert-Butyl Ester as substrate at 5 uM after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1855252Downregulation of SPT16 expression in human HCT-116 cells at 1.5 uM measured after 24 hrs by Western blot analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID456800Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D62010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID618015Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 1 uM after 48 hrs using propidium iodide staining by flow cytometric analysis2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
AID1537555Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1065628Inhibition of human recombinant full length HDAC2 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1206762Inhibition of full length human recombinant HDAC1 expressed in baculovirus using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID473174Ex vivo inhibition of human HDAC6 in human Caco-2 cells by fluorometric cellular activity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1386681Inhibition of HDAC in human GM18453 cells harboring NPC1 mutant assessed as restoration of cholesterol trafficking at 5 uM after 48 hrs by filipin-staining based fluorescence microscopic analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1622979Cytotoxicity against human MCF7 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1065961Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID1514612Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 3.2 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1274876Inhibition of HDAC6 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
AID1482117Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1671979Cytotoxicity against human HCT-116 cells after 72 hrs by SRB assay2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID1548300Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 42%)
AID1355712Antifungal activity against FLC resistant Candida albicans 0710922 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1356282Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability at 0.05 to 0.5 uM cotreated with up to 500 nM of 4-CPA measured after 72 hrs by MTT assay
AID1826599Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID526531Inhibition of HDAC2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Property based optimization of δ-lactam HDAC inhibitors for metabolic stability.
AID1449218Inhibition of human recombinant HDAC8 expressed in Escherichia coli using Z-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate measured after 90 mins by fluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID1764249Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1873411Inhibition of HDAC3 (unknown origin) preincubated for 60 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1649884Inhibition of HDAC8 (unknown origin)2019European journal of medicinal chemistry, Feb-15, Volume: 164Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview.
AID1548247Inhibition of HDAC3 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1754798Downregulation of SIRT5 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1901762Inhibition of full length human recombinant HDAC6 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1742740Genotoxicity in Salmonella typhimurium TA97a by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID308646Antiproliferative activity against human PANC1 cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1174704Antitumor activity against human U937 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 120 mg/kg/day, po after 16 days2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID304371Inhibition of human IMPDH 12007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
AID461261Antiproliferative activity against human MCF7 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1533328Selectivity ratio of IC50 for full length human N-terminal FLAG-tagged HDAC8 (1 to 377 residues) expressed in HEK293 cells to IC50 for full length human N-terminal FLAG-tagged HDAC6 (1 to 1215 residues) expressed in HEK293 cells2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
AID619057Half life in human liver microsomes2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1164912Inhibition of HDAC7 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1280273Selectivity index, ratio of HDAC6 inhibition in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 1 uM over class1 HDAC inhibition in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 1 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID328802Inhibition of HDAC5 at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1515912Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1605970Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1898905Antiproliferative activity against human U2932 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID492812Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1864266Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c-nu/nu mouse assessed as reduction in tumor volume at 10 mg/kg, ip measured for 31 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1864252Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1897367Inhibition of FGFR1 (unknown origin)
AID1597955Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 10 uM incubated for 72 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometric analysis (Rvb = 5.69%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1897373Inhibition of HDAC2 (unknown origin)
AID1704070Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.
AID1487004Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1410013Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.
AID609725Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors.
AID1578507Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells incubated for 18 hrs by annexin V FITC and PI based flow cytometry2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1876467Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1276240Inhibition of HDAC1/HDAC2 in human HeLa cells nuclear extract preincubated for 5 mins before Boc-Lys (acetyl)-AMC substrate addition for 30 mins by microplate reader analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.
AID461256Antiproliferative activity against human HepG2 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1275656Toxicity in athymic nude mouse xenografted with human HCT116 cells assessed as reduction in body weight at 40 mg/kg, ip qd administered for 14 days measured every other day during compound dosing2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1599771Inhibition of HDAC6 in human A549 cells assessed as increase in histone H3 acetylation at 2.5 uM measured after 6 to 20 hrs by Western blot analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1518828Antimalarial activity against ring stage Plasmodium falciparum K1 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1890517Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1742706Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 0.330 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID274075Inhibition of MCF7 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID511067Inhibition of HDAC102010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1275247Inhibition of HDAC in human HeLa cell nuclear extracts preincubated for 15 mins followed by addition of Fluor de Lys as substrate for 1 hr by fluorometric assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.
AID1529548Induction of apoptosis in human BL2 cells assessed as early apoptotic cells at 10 nM after 48 hrs by annexin V-FITC/propidium iodide double staining-based flow cytometry (Rvb = 8.2%)2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1819529Antitumor activity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as reduction on tumor volume at 60 mg/kg, IG administered for 12 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID503687Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 14 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1434353Growth inhibition of human PC3 cells measured after 5 days by sulforhodamine-B assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1649503Cytotoxicity against mouse L929 cells assessed as reduction in cell viability measured after 72 hrs by tryphan blue assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
AID411261Cytotoxicity against human primary lung fibroblasts after 72 hrs by trypan blue exclusion assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1399543Inhibition of recombinant human HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID1379288Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
AID1876464Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1622934Inhibition of recombinant human HDAC6 using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1321725Passive membrane permeability of the compound at 50 uM after 18 hrs by PAMPA2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID445125Inhibition of human recombinant his tagged HDAC4 expressed in baculovirus assessed as residual activity at 5 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group.
AID348797Inhibition of HDAC22008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID620531Reactivation of MeCp2 mutant expression in human GM11272 cells at 10 to 100 nM by PCR method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression.
AID1762500Cytotoxicity against mouse Neuro2a cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo 2.0 Luminescent cell assay2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1739566Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 20 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1742181Inhibition of recombinant human N-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus infected Sf9 insect cells using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1859953Cytotoxicity against mouse NIH3T3 cells assessed as inhibition of cell growth by neutral red uptake assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1901158Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1063059Inhibition of HDAC in human K562 cell extract using Fluor-de-Lys deacetylase as substrate preincubated for 45 mins measured after 15 mins by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID90675In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID613298In vitro cardiac safety index, ratio of IC50 for human ERG to IC50 for human HCT116 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1549140Antifungal activity against azole-resistant Candida tropicalis 5008 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1312892Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as mortality at 50 mg/kg, ip administered every 2 days for 11 days2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1215094Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1321734Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1355728Antitumor activity against human HEL cells xenografted in BALB/C nude mouse assessed as tumor growth inhibition at 10 mg/kg, ip bid treated for 21 consecutive days relative to control2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1511149Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID288448Inhibition of LPS-stimulated NO production in RAW264.7 cells after 24 hrs by ELISA2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID482956Half life in human liver microsome2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID482947Inhibition of HDAC72010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID750107Cytotoxicity against human HCT116 cells after 48 hrs by Sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
AID1566807Inhibition of recombinant full length N-terminal GST-tagged human HDAC5 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1599727Cytotoxicity against human Meso13 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1816227Induction of apoptosis in mouse 4T1 cells assessed as necrotic cells at 5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.35%)
AID352749Inhibition of His-tagged HDAC4 catalytic domain expressed in Escherichia coli2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1899585Inhibition of HDAC class 1 in human HT-29 cells using Boc-Lys-Ac as substrate incubated for 3 hrs by microplate reader assay
AID1296348Inhibition of recombinant human HDAC1 using Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition measured after 20 mins by fluorescence assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.
AID603539Toxicity in human MDA-MB-231 cells xenografted athymic nude mouse assessed as change in body weight at 90 mg/kg, ip qd for 21 days2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1181331Potentiation of doxorubicin-induced cytotoxicity against human U937 cells assessed as inhibition of cell proliferation at 2.5 uM after 24 hrs by Cell Titer GLo Assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1633669Neurotoxicity against rat CGN cells assessed as cell viability at 25 uM incubated for 24 hrs by MTT assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1917536Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID408880Inhibition of HDAC12008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1165113Cytotoxicity against human DU145 cells2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID1742654Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1454053Growth inhibition of human MCF7 cells after 3 days by WST1 assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID541644Inhibition of human HDAC1 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1371075Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1907399Inhibition of HDAC1 (unknown origin) using trypsin and LGK(Ac)-AMC as substrates incubated for 1 hr and measured by fluorescence assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Dual-acting antitumor agents targeting the A
AID1876466Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID90347Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells.2002Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23
Trifluoromethyl ketones as inhibitors of histone deacetylase.
AID1155336Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1677509Up regulation of BAX protein in human HeLa cells at 0.3 to 3 uM after 6 to 12 hrs by Western blot analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1206764Inhibition of full length human recombinant HDAC3 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID603535Cytotoxicity against human HL60 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1888586Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay
AID1446915Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy.
AID1326514Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID347870Growth inhibition of human ovarian cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1550115Inhibition of JAK in human MDA-MB-231 cells assessed as decrease in upregulation of p-STAT3-Tyr705 level at 5 uM after 12 hrs in presence of ruxolitinib by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID674001Growth inhibition of human MCF7 cells after 72 hrs by XTT assay2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1898954Induction of cell cycle arrest in human NCI-H460 cells assessed as accumulation of cells at G2/M phase at 4.2 uM after 72 hrs by flow cytometry (Rvb = 21.1%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID760495Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID780586Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect high5 cells using Boc-Lys (epsilon-acetyl)-AM) as substrate after 3 to 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
AID1200981Plasma clearance in ICR mouse2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1469372Cytotoxicity against human Hep3B cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID619055Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1280307Inhibition of human KDAC32016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1739565Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 100 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1864264Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c-nu/nu mouse assessed as reduction in tumor growth at 10 mg/kg, ip measured for 31 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1486670Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID670101Antitumor activity against human A549 cells xenografted in nude mouse assessed as tumor growth delay at 200 mg/kg, po administered QD till end point2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1426427Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID347871Growth inhibition of human Leukemia cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1825925Inhibition of human C-terminal His tagged HDAC3 (1 to 428 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
AID1727732Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1441673Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in number of lymphocytes in BALF at 10 and 25 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID420644Antitumor activity against human H460 cells athymic nude Swiss mouse assessed as tumor volume inhibition at 100 mg/kg, po QD administered 5 days a week for 2 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID755627Inhibition of HDAC isolated from human HeLa cell nuclear extract after 30 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
AID1606018Induction of necrosis in human HEK293 at 1 to 2 uM after 72 hrs by propidium iodide/Annexin-V staining based flow cytometry2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1659236Inhibition of human HDAC6 after 30 mins by microplate reader analysis2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
AID1482134Induction of mitochondrial membrane potential loss in human HL60 cells assessed as intact mitochondrial membrane potential at 1 uM measured after 48 hrs by Rh123 dye-based flow cytometric analysis (Rvb = 91.3%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1556035Inhibition of SIRT2 in human MCF7 cells assessed as accumulation of acetylated-alpha tubulin at 0.1 uM measured after 24 hrs by Western blot analysis relative to alpha-tubulin2019Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD
AID1901054Inhibition of HDAC1 (unknown origin) using trypsin and Ac-peptide as substrates2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID637889Inhibition of recombinant human HDAC6 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases.
AID1819506Inhibition of HDAC8 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1572342Inhibition of recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1250650Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID717795Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 1.25 x 10'-7 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID749388Inhibition of human recombinant HDAC6 expressed in High5 insect cells using Boc-Lys (-acetyl)-AM) as substrate after 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
The discovery of colchicine-SAHA hybrids as a new class of antitumor agents.
AID1917544Selectivity index, ratio IC50 for inhibition of HDAC11 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
AID527046Inhibition of AKT phosphorylation in human A549 at 5 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID350726Growth inhibition of human SNB78 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID545859Antimalarial activity against Plasmodium falciparum HB3 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1321735Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 1000 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1469312Induction of apoptosis in human T47D cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 7.7%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1898900Antiproliferative activity against human MM432 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1200980Inhibition of HDAC6 in human NCI-H929 cells assessed as induction of tubulin acetylation after 24 hrs by Western blot analysis2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1266808Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID544090Antimalarial activity against drug-resistant Plasmodium falciparum D6 infected in Aotus lemurinus lemurinus monkey2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1548260Antiproliferative activity against human KM3 cells incubated for 48 hrs by MTT assay
AID1373247Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
AID1572345Selectivity ratio of IC50 for recombinant human HDAC8 to IC50 for N-terminal GST-tagged human HDAC62019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1861670Induction of apoptosis in human HCT-116 cells at 2000 nM measured after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1659646Inhibition of HDAC in human HeLa cell extracts assessed as inhibition of substrate deacetylation using Boc-Lys (acetyl)-AMC as substrate by fluorescence based assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID1203894Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1469178Downregulation of HDAC6 protein expression in human MV4-11 cells at 5 uM after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Class I HDAC Inhibitors Display Different Antitumor Mechanism in Leukemia and Prostatic Cancer Cells Depending on Their p53 Status.
AID1861336Inhibition of HDAC in human DOHH-2 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 2.5 uM in presence of 10 uM piclitisib measured by Western blot analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID328810Antiproliferative activity against human renal epithelial cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1178593Inhibition of rat liver HDAC at 10 uM pre-incubated for 15 mins before Boc-Lys(Ac)-AMC substrate addition and measured after 30 mins by fluorometry2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID1758495Antiproliferation activity against human U-87 MG cells assessed as growth inhibition measured after 1 hr by MTT assay2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID446342AUC (0 to infinity) in CD1 mouse at 5 mg/kg, iv2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID328794Inhibition of HDAC22008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1250644Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1355689Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1275637Inhibition of recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
AID1371052Antilieshmanial activity against amastigote stage of Leishmania donovani by fluorimetric assay2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1742659Cytotoxicity against human PLC cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID90343In vitro inhibitory activity against histone deacetylase (HDAC) isolated from HeLa nuclear extract at a concentration of 100 uM2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.
AID1821322Antitumor activity against human HepG2 cells xenografted in mouse assessed as upregulation of histone H3 at 12 mg/kg, ip administered every 2 days for 4 weeks by western blot analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1273868Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID673999Growth inhibition of human Jurkat cells after 72 hrs by XTT assay2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1667067Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1821340Toxicity in mouse xenografted with human HepG2 cells assessed as cellular inflammation in kidney at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1206765Inhibition of human recombinant HDAC4 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID274012Percent inhibition of CYP450 2D6 at 1uM concentration2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID525002Inhibition of HDAC3 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1469288Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.88%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1659658Induction of apoptosis in human MOLT4 cells assessed as increase in apoptotic cells at 5 uM incubated for 24 hrs by Annexin V and PE staining based flow cytometric analysis relative to control2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID1898951Induction of cell cycle arrest in human NCI-H460 cells assessed as accumulation of cells at sub-G1 phase at 4.2 uM after 72 hrs by flow cytometry (Rvb = 1.1%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1245690Inhibition of Class 2a histone deacetylase in human PC3 cells using Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1251318Growth inhibition of human IGROV1 cells after 72 hrs2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1754784Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 1 uM incubated for 24 hrs by PI staining based flow cytometric analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1758466Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1591851Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system at 10 nM using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay relative to contro2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID760374Half life in mouse liver microsomes at 0.4 ug/mL by HPLC-MS analysis in presence of NADPH2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1266841Induction of p53 activation in human HCT116 cells assessed as upregulation of p21 expression at 0.1 to 5 uM after 12 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1441694Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as TGF-beta1 level at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 14 by ELISA (Rvb = 99.30 pg/ml)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1769650Inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1873407Inhibition of HDAC2 (unknown origin) preincubated for 90 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1433258Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1352478Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID1441642Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in alveolar vascular permeability at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by Evans blue dye based micro2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID737908Selectivity index, ratio of IC50 for mouse MEF cells to IC50 for human A549 cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1170749Cytotoxic activity against human EB3 cells after 3 days by MTT assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1129792Induction of apoptosis in human Jurkat cells assessed as caspase 8 activation at 10 uM after 24 hrs by FACS flow cytometric analysis relative to control2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID297496Cytotoxicity against human WM 266-4 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1898495Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer.
AID1901162Antiproliferative activity against human SGC-7901 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1181304Inhibition of human recombinant HDAC4 using non-histone trifluoroacetyl lysine substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1441656Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in total number of leucocytes in BALF at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID482942Inhibition of HDAC22010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1462023Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability.
AID1819859Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype.
AID1600660Antiproliferative activity against human OE33 cells assessed as reduction in cell viability incubated for 72 hrs by presto blue assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
AID1578910Induction of autophagy in human Bel7402 cells assessed as upregulation of LC3-2 level at 5 uM after 24 to 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1303628Potentiation of 0.05 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.25 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID459821Inhibition of HDAC in human HeLa cell nuclear extract by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors.
AID1684874Antitumor activity against mouse LL/2 cells inoculated in C57BL/6J mouse assessed as tumor growth inhibition at 25 mg/kg, ip administered for 12 days
AID476654Toxicity in FVB mouse assessed as effect on mean platelet volume at 50 mg/kg, po administered 5 times per week for 2 weeks (Rvb = 8.8 +/- 0.1 microm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1066165Antimigratory activity against human LNCAP cells at 50 uM after 72 hrs2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
AID1900903Cytotoxicity against mouse GL26 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID482948Inhibition of HDAC92010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1170744Inhibition of human recombinant HDAC6 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1898952Induction of cell cycle arrest in human NCI-H460 cells assessed as accumulation of cells at G0/1 phase at 4.2 uM after 72 hrs by flow cytometry (Rvb = 46.8%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1330927Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1515902Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID274070Half life after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID408883Inhibition of HDAC82008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1591717Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1722281Inhibition of human recombinant HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate incubated for 24 hrs measured after 30 mins by microplate reader based spectrophotometric analysis2020Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
AID1545859Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1659654Antiproliferative activity against human K562 cells incubated for 24 hrs by CCK8 assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID1622954Inhibition of HDAC in human HeLa nuclear extract2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1177055Cytotoxicity against rat L6 cells2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1873404Inhibition of HDAC2 (unknown origin) preincubated for 5 mins2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID605540Antiproliferative activity against human HUT78 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1543662Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID1281849Inhibition of full length His6-tagged GST-fused recombinant human HDAC4 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1676595Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1688042Induction of HDAC3 degradation in human HL-60 cells assessed as decrease in HDAC3 level at 2 uM incubated for 12 hrs by Western blot analysis2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID297479Cytotoxicity against human MCF7 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID708275Growth inhibition of human QGY7701 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1622908Inhibition of HDAC in human HeLa cytosolic extract using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1753832Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells at 100 nM using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay relative to control2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1676589Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID352750Inhibition of C-terminal FLAG tagged HDAC62009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1303692Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 5000:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM)2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1418671GPx-like activity of the compound assessed as velocity for tert-butyl hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.
AID1876463Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1578907Induction of autophagy in human Bel7402 cells assessed as accumulation of autophagic vacuoles at 5 uM after 24 hrs by acridine orange staining based fluorescence microscopic method2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1897470Inhibition of HDAC in human SNU-16 cells assessed as reduction in phosphorylated STAT3 level at 0.11 to 1 uM incubated for 36 hrs by Western blot analysis
AID1260655Binding affinity to Zn2+ assessed as Zn2+/compound complex formation by ITC analysis
AID481545Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1653096Antiproliferative activity against human HepG2 cells by CCK8 assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID222292Compound was tested for anti-proliferative activity in human hepatocytes2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1659648Inhibition of HDAC2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID487875Inhibition of HDAC in human A549 cells assessed as induction of histone H4 hyperacetylation at IC50 concentration after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
AID1173495Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1777022Inhibition of HDAC6 (unknown origin)2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase.
AID1129010Inhibition of human HDAC-8 using RHKK(Ac) as substrate by fluorescence assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
AID1437552Inhibition of human HDAC1 using H3(1-21)K9 after 60 mins by fluorescence assay2017Journal of natural products, 01-27, Volume: 80, Issue:1
Monascustin, an Unusual γ-Lactam from Red Yeast Rice.
AID1055715Antiproliferative activity against human AsPC1 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1441690Protection against BLM-induced lung fibrosis in C57BL/6 mouse assessed as reduction in deposition of collagen fibers at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 by Massons trichrome staining based method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1452275Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID626563Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 1 uM by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
AID1178601Inhibition of human HDAC6 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.
AID511069Inhibition of HDAC in human HeLa cells at 10 uM after 15 mins2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1401374Inhibition of HDAC3 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1865304Antitumor immunity against mouse 4T1 cells xenografted in BALB/c syngeneic mouse model assessed as fold increase in proportion of CD4+ T cells in spleen at 40 mg/kg, po qd for 12 days by flow cytometry analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID473183Growth inhibition of human Caco-2 cells after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID748980Inhibition of HDAC5 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1434361Inhibition of HDAC in HEK293 cells expressing Myc-tagged RUNX3 assessed as histone-3 acetylation by measuring ratio of histone-3 acetylation level to beta-actin level at 1 uM measured after 24 hrs by Western blot analysis relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1205631Growth inhibition of human NCI-H23 cells after 5 days by sulforhodamine B assay2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID586606Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1065636Inhibition of human recombinant HDAC7 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1367349Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Synthesis and biological evaluation of Santacruzamate-A based analogues.
AID539709Inhibition of human HDAC after 30 mins2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.
AID1897392Induction of apoptosis in human SNU-16 cells assessed as live cells at 0.03 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 90.92%)
AID288452Growth inhibition of ACHN cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID1647329Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as reversal of hippocampal atrophy by measuring increase in ratio of size of hippocampus to lateral ventr2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1514610Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 2.5 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 3.2 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1545755Inhibition of HDAC1 (unknown origin)2019European journal of medicinal chemistry, Dec-01, Volume: 183Indole: A privileged scaffold for the design of anti-cancer agents.
AID1605981Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1206767Inhibition of full length human recombinant HDAC8 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1690844Inhibition of human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residus) expressed in baculovirus infected Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by s2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1348914Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID609506Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
AID1164905Solubility of the compound in phosphate buffer at pH 6.5 after 1 to 2 hrs by LYSA2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1322165Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of novel HDAC8 inhibitory 2,5-disubstituted-1,3,4-oxadiazoles containing glycine and alanine hybrids with anti cancer activity.
AID1449681Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID1819503Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1888426Toxicity in ICR mouse infected with azole-resistant Candida albicans 0304103 assessed as reduction in survival time at 10 mg/kg, ip administered once daily for 5 days2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID605530Antiproliferative activity against human A2780 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID408889Cytotoxicity against human Hup T3 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1578506Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 4 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 9.2 to 9.63 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1785328Inhibition of full length human CDK2 (1 to 298 end residues)/N-terminal GST-tagged CyclinA2 (1 to 432 residues) expressed in baculovirus expression system at 100 nM preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay re
AID1541453Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1898980Induction of cell cycle arrest in human H460-R9A cells assessed as accumulation of cells at G0/1 phase at 1.9 uM after 72 hrs by flow cytometry (Rvb = 50.1%)2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID604137Inhibition of histone acetyltransferase in human U937 cells assessed as increase of acetylation of histone H3 at K9 at 5 uM after 24 hrs by Western blotting2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
AID780587Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
AID1885698Toxicity in ICR mouse assessed as effect on AST level at 12 umol/kg, ip measured after 12 hrs in presence of CDDO-Me2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy.
AID1282258Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1547273Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1898907Antiproliferative activity against human NB-4 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1647339Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as reversal of hippocampal atrophy by measuring increase in hippocampal volume at 25 mg/kg, ip administer2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID446335Metabolic stability in mouse liver microsomes assessed as half life2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID1206741Cytotoxicity against human 3AO cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1250646Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1783068Antifungal activity against fluconazole-sensitive Candida albicans 4108 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1349732Toxicity in BALB/C nude mouse xenografted with human HCT116 cells assessed as body weight loss at 25 mg/kg, ip bid administered for 21 consecutive days measured every 3 days2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1482172Cytotoxicity against human PC3 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1702137Inhibition of PI3K/AKT/mTOR signaling in human HuH-7 cells assessed as p70S6K Thr389 phosphorylation level at 10 uM incubated for 4 hrs including last 12 mins stimulation with 20 ng/ml growth factor VEGF by Western blot analysis (Rvb = 100 %)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1907401Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Dual-acting antitumor agents targeting the A
AID1293578Antitumor activity against human HCT116 cells xenografted in athymic Swiss nude mouse assessed as tumor growth inhibition at 175 mg/kg, po for 5 days a week for 4 weeks relative to control2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1863436Inhibition of HDAC4 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1587863Inhibition of recombinant full-length C-terminal FLAG-fused/His-tagged human HDAC1 expressed in baculovirus infected Sf9 insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1848614Cytotoxicity against human IGROV-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1865239Inhibition of recombinant his-tagged human HDAC11 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID473181Induction of HDAC-mediated alpha-tubulin acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID683274Inhibition of HDAC1 by fluorometric assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects.
AID1821277Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1614251Antitumor activity against human MM1S cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 50 mg/kg, iv qd administered for 10 days and measured every 2 days post last dose in presence of 25 mg/kg RAPA by caliper method relative to c
AID1431813Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1898897Antiproliferative activity against human A2780 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1888587Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
AID1576452Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay
AID1361645Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1742228Antitumor activity against CM-Dil labeled human MDA-MB-231 cells xenografted in Zebrafish AB assessed as tumor growth inhibition at 2.5 ug/ml measured after 5 days by fluorescence microscopic analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID300838Growth inhibition of human HCT15 cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID1326517Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated alpha-tubulin after 48 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1401901Inhibition of HDAC in human HeLa cell extract using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1578492Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 19.46 to 22.17 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1415637Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 60 mins by fluorescence assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1399542Inhibition of recombinant human HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID1454057Growth inhibition of human OVCAR5 cells after 3 days by WST1 assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1515839Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1819536Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as spleen damage at 60 mg/kg, IG administered for 12 days H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID240505Inhibitory concentration against histone deacetylase of HeLa cells2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.
AID1361634Inhibition of HDAC6 (unknown origin) after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1119182Cytotoxicity against human MCF10A cells after 96 hrs by MTA reduction assay2012MedChemComm, , Volume: 3, Issue:1
Polyamine-based small molecule epigenetic modulators.
AID414717Inhibition of human recombinant HDAC1 expressed in HEK293 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID482941Inhibition of HDAC82010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1441707Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in number of lymphocytes in BALF at 25 and 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1162226Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential in P5 quadrant at 1 uM by Rhodamine123 assay (Rvb = 3.4%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID541647Inhibition of human HDAC8 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1550158Toxicity in BALB/c nu mouse xenografted with HEL cells assessed as injury to internal organs at 60 mg/kg/day, ip administered for 16 days and measured post-last dose in presence of ruxolitinib2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1139708Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.
AID392409Induction of alpha tubulin acetylation in human T24 cells after 3 hrs by ELISA2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Sulfamides as novel histone deacetylase inhibitors.
AID1384224Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1753837Antiproliferative activity against human MGC803 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID274025Half life after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1380940Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1614140Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay
AID525017Inhibition of HDAC in human CFBE41o- cell line assessed as increase in mutant Fdelta508 CFTR mRNA level at 5 uM after 8 hrs by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1355711Antifungal activity against FLC resistant Candida albicans 0710922 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1401382Inhibition of HDAC2 in human HeLa-S3 cell lysates assessed as remaining activity at 1 uM preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1664945Inhibition of class 1 HDAC in human Jurkat model of HIV latency assessed as reactivation of HIV latency incubated for 20 hrs in presence of 5% NHS by Steady-Glo luciferase assay2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
AID1239050Inhibition of recombinant His6-tagged GST-fused human HDAC6 expressed in baculovirus infected insect High5 cells using Boc-Lys-(epsilon-acetyl)-AMC as substrate after 3 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID749696Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 expression at 2.5 to 5 uM after 24 hrs by Western blot analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1623534Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID1762490Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus-infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic a2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1566802Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1462030Half life in rat plasma at 200 uM by HPLC analysis2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability.
AID1469377Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.41%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1702085Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1355688Inhibition of full length human recombinant HDAC1 expressed in baculovirus expression system using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID723472Inhibition of HDAC in cisplatin sensitive human MDA-MB-231 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1737151Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 10 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 5.14%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1890343Antitumor immunity in C57BL/6 mouse xenografted with mouse CT26 cells assessed as decrease in number of CD8+IFNgamma+ T cells at 100 mg/kg, po administered once daily for 21 days measured by flow cytometry analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1816194Inhibition of TYK2 (unknown origin) incubated for 40 min in presence of ATP by microplate reader analysis
AID420509Induction of apoptosis in human IGROV1 cells at IC90 after 72 hrs by TUNEL assay2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID781049Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID292437Antiproliferative activity against HeLa cells by alamar blue assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
AID1785340Inhibition of recombinant human HDAC9 measured after 30 mins by fluorescence microplate reader assay
AID1266086Inhibition of HDAC in human MeT-5A cells assessed as hisone H3 acetylation at 5 uM after 16 hrs by BRET assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1390013Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1758526Permeability of compound by PAMPA-BBB assay2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID1702069Inhibition of N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID710838Cytotoxicity against human ACHN cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID1482171Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1246514Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1441672Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in number of neutrophils in BALF at 10 and 25 mg/kg, ip qd for 7 days post BLM challenge measured on day 72017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1754800Downregulation of SIRT7 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1754796Downregulation of SIRT3 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID525023Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 5 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1614193Induction of apoptosis in human MV4-11 cells assessed as viable cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 84.1%)
AID1774970Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate at 10 uM preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors.
AID1890336Antitumor activity against mouse CT26 cells xenografted in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po administered once daily for 21 days2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID619140Kinetic solubility of the compound at pH 7 with 2.5% DMSO2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1421912Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate measured after 90 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1337260Antiproliferative activity against human MCF7 cells up to 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1578885Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1897396Induction of apoptosis in human SNU-16 cells assessed as live cells at 0.1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 90.92%)
AID1898899Resistance index, ratio of IC50 for human A2780 cells to IC50 for A2780-DX cells2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID503690Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 9 acetylation of FXN gene at 2.5 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1810052Inhibition of HDAC6 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader
AID511064Inhibition of HDAC22010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1865259Inhibition of wild type SHP2 (unknown origin) using DiFMUP as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by microplate reader method2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID461264Antiproliferative activity against human NCI-H2122 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID663370Growth inhibition of human PC3 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1373248Inhibition of HDAC1 (unknown origin) at 1 uM preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
AID1816191Inhibition of recombinant HDAC10 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis
AID350717Inhibition of human recombinant HDAC2 by fluorimetry2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID366651Cytotoxicity against HMEC after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID663385Growth inhibition of human UACC257 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID762189Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.
AID623098Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group.
AID1141762Cytotoxicity against human KB cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1421926Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1630628Inhibition of HDAC in human MOLT4 cells assessed as H3K9 acetylation at 2.5 uM after after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID352752Antiproliferative activity against human HCT116 cells after 72 hrs by celltiter-blue cell viability assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
AID1240551Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID1065631Inhibition of HDAC4 in human Jurkat E6.1 cells using Boc-Lys-TFA as substrate incubated for 2 hrs prior to substrate addition measured after 3 hrs by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1576464Induction of apoptosis in human A549 cells assessed as viable cells at 5 uM after 72 hrs by Annexin V-phycoerythrin/7-AAD staining based flow cytometric analysis (Rvb = 96.57%)
AID744874Cytotoxicity against human HCT116 cells by MTT assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Discovery of adamantane based highly potent HDAC inhibitors.
AID481568Antitumor activity against mouse S180 cells xenografted in ICR mouse assessed as reduction of tumor weight at 200 mg/kg, ig administered 2 days after tumor inoculation qd for 7 days2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1901170Inhibition of HDAC6 in human HCT-116 cells assessed as increase in alpha-tubulin acetylation at 5 uM measured after 6 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID544400Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation after 3.5 hrs by SDS-PAGE2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1639363Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1361629Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1864678Inhibition of full length recombinant human HDAC6 in expressing in mouse J774.A1 cells assessed as accumulation of acetylated alpha-tubulin at 0.1 to 1 uM measured upto 24 hrs by western blot analysis
AID1239056Inhibition of HDAC in human RPMI8226 cells assessed as upregulation of acetylated alpha-tubulin level at 1 uM after 24 hrs by Western blot analysis2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID1486322Genotoxicity in Salmonella typhimurium TA100 at 50 times antiproliferative IC50 by Ames test2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID626565Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
AID1865294Antitumor activity against human MV4-11 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 40 mg/kg, po qd administered for 20 days in presence of SHP0992022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1548246Inhibition of HDAC2 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID134164Antitumor activity against HT1080 cell line in mouse xenograft model after orally dosed once every other day at 30 mg/kg2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
AID749705Inhibition of HDAC in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1848283Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID1127011Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining after 12 to 24 hrs by flow cytometry analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID541656Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID619051Competitive inhibition of HDAC6 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID723460Inhibition of human HDAC11 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1464867Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate after 15 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1697197Cytotoxicity against human SW620 cells by colorimetric method2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID1816197Inhibition of JAK in human BT-549 cells assessed as reduction in activation of p-STAT3 at 3 uM incubated for 12 hrs by chemiluminescence based western blotting analysis
AID1215090Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1421614Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
AID1537558Antiproliferative activity against human IMR32 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID765212Cytotoxicity against human MiaPaCa cells2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents.
AID328793Inhibition of HDAC12008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID717804Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1467238Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 0.02 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured after 30 mins by fluorome2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1605971Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1205634Induction of myc-tagged RUNX3 acetylation in human HEK293 cells assessed as RUNX3 level at 1 uM after 24 hrs by immunoprecipitation analysis relative to TSA2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.
AID1380938Inhibition of HDAC in human HeLa cell nuclear extract using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID663336Growth inhibition of human COLO205 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1476161Antiproliferative activity against human KHYG cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1698865Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID329927Inhibition of human HDAC1 in U937 cells assessed as residual activity at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1667090Inhibition of STAT3 in human MDA-MB-231 cells assessed as downregulation of cyclinD1 expression at 5 to 25 uM after 24 hrs by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1808546Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using fluorometric substrate measured after 60 mins by FRET 2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1482103Inhibition of HDAC 9 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1164173Induction of apoptosis in human K562 cells using annexin-V/PI staining by flow cytometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1202600Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation after 24 hrs by Western blotting analysis2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID1126962Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID482968Elimination half life in mouse at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1861309Induction of apoptosis in human DOHH-2 cells measured by flow cytometry analysis2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
AID473193Growth inhibition of human HepG2 cells after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1702101Inhibition of HDAC6 in human PC-3 cells assessed as increase in acetylation of alpha-tubulin at Lys40 residue at 10 uM incubated for 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1164922Cytotoxicity against human BE(2)-C cells at 2 uM after 3 to 9 days by CCK-8 assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1765328Inhibition of human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assa2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1393285Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
AID1825882Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
AID1174689Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1899584Inhibition of HDAC class 2a in human HT-29 cells using Boc-Lys-TFA as substrate incubated for 3 hrs by microplate reader assay
AID1390014Inhibition of full length recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Boc-Lys-(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1816198Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
AID1482105Inhibition of HDAC 11 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1487010Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1518839Resistance ratio of IC50 for antimalarial activity against ring stage Plasmodium falciparum K1 to IC50 for antimalarial activity against ring stage Plasmodium falciparum 3D72019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID663379Growth inhibition of human MALME-3M cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1832670Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1865254Inhibition of human HDAC in human MV4-11 cells assessed as downregulation of ERK phosphorylation at 1 uM measured after 24 hrs by in presence of SHP099 Western blot assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1888404Antifungal activity against azole-resistant Candida albicans 0304103 assessed as fungal growth inhibition incubated for 48 hrs by CLSI based checkerboard microdilution assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.
AID313736Inhibition of HDAC82008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID603531Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID1730889Inhibition of EGFR in human NCI-H1975 cells assessed as reduction in EGFR phosphorylation at Tyr-1173 residues at 1 uM after 48 hrs by Western blot analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID593546Inhibition of human HDAC2 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1739586Inhibition of HDAC6 in human HL-60 cells assessed as ratio of acetylated tubulin/GAPDH at 1 uM incubated for 4 hrs by Western blot analysis relative to DMSO2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1898911Antiproliferative activity against human U-87 MG cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1572379Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter blue-reagent based assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1547334Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in CTF1 mRNA level at 10 uM after 24 hrs by RT-PCR analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1572378Ratio of inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 10 uM to inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 0.1 uM2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID404443Cytotoxicity against human Mia Paca2 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID663350Growth inhibition of human EKVX cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID674002Growth inhibition of human HEK293 cells after 72 hrs by XTT assay2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1155337Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for exo-erythrocytic form of Plasmodium berghei2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID482969Oral bioavailability in mouse at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1312930Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of acetylated alpha-tubulin level at 2 uM after 6 hrs by Western blot method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1591855Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells at 100 nM using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay relative to contr2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
AID546550Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1250641Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1486673Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1832690Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1441682Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as protein concentration in BALF at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 (Rvb = 2.39 mg/ml)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID605619Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 300 nM after 15 hrs by propidium iodide staining based flow cytometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID605392Inhibition of human recombinant HDAC1 using fluor de Lys as substrate by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1599786Inhibition of HDAC6 in human A549 cells assessed as upregulation of E-cadherin mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID708277Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1511132Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID274171Antiproliferative activity against HCT116 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID247946Concentration required to inhibit human LNCaP prostate carcinoma cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.
AID1282238Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1542186Inhibition of HDAC8 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1065632Inhibition of human recombinant full length HDAC8 using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1859928Inhibition of HDAC in human U-937 cells assessed as increase in acetylation level of alpha-tubulin at 10 uM measured after 24 to 48 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID1890307Inhibition of recombinant human HDAC1 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1518786Antiproliferative activity against human OPM2 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID765392Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID481571Cytotoxicity against mouse S180 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1293560Antiproliferative activity against human HT-29 cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1742629Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated alpha-tubulin incubated for 8 hrs by Western blot analysis2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1826631Synergistic antiproliferative effect on HEL cells assessed as combination index at 0.37 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1915537Inhibition of HDAC1 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1206736Inhibition of HDAC1/HDAC2 in human HeLa cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1915552Antiproliferative activity against breast cancer cell line (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1390016Antiproliferative activity against human A549 cells after 96 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1431815Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1441652Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-6 level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1816689Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1312926Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of acetylated histone H3 level at 2 uM after 6 hrs by Western blot method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID760505Inhibition of HDAC8 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHK(Ac)K(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1449675Inhibition of HDAC in human HeLa cell nuclear extracts using (Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID1466059Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID765391Inhibition of GST-tagged recombinant human HDAC3/NcoR1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1547258Inhibition of human recombinant His-tagged BRD4 BD1 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1476150Antiproliferative activity against human HL60 cells2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID663357Growth inhibition of human COLO205 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1752945Selectivity index, ratio of IC50 for C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 cells to IC50 for N-terminal GST-tagged full length human recombinant HDAC6 expressed in baculovirus infected
AID461254Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID652750Inhibition of recombinant human HDAC6 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1164915Inhibition of HDAC10 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1548730Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1633991Inhibition of HDAC3 in human HuH7 cells assessed as increase in histone H3 K9/K14acetylation at varying concentrations incubated for 24 hrs by Western blot analysis2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID1622910Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID652761Restoration of CFTR deltaF508 mutant trafficking to cell surface in human CFBE41o cells co-expressing halide-sensitive YFP-H148Q/I142L assessed as fluorescence quenching at 5 uM after 24 hrs relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1055352Selectivity ratio of IC50 for human recombinant HDAC6 to IC50 for human recombinant HDAC22013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID1763821Inhibition of human recombinant HDAC8 incubated for 15 mins by fluorogenic assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID1622900Cytotoxicity against human HCT116 cells after 72 hrs by CellTiter-Glo assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1737147Induction of apoptosis in human HCT-116 cells assessed as viable cells at 1 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 90.34%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1826641Induction of apoptosis in HEL cells assessed as apoptotic cells at 0.1 uM incubated for 48 hrs by annexin V-FITC/PI staining based flow cytometry (Rvb = 3.95%)2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID781046Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
AID1742664Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1876477Induction of cell cycle arrest in human HCT-116 cells assessed as decrease in accumulation of cells at S phase at 1 uM incubated for 24 hrs by flow cytometry analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1578499Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 0.5 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 19.46 to 22.17 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID348800Inhibition of HDAC42008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID1441632Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID297500Cytotoxicity against vincristine resistant human CCRF-CEM cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1543931Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.
AID1864223Cytotoxicity against human BT-549 cells assessed as reduction in cell viability measured after 48 hrs2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID366647Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1671970Retention time of the compound by HPLC method2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro.
AID734740Inhibition of HDAC6 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.
AID1486296Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1227053Cytotoxicity against african green monkey Vero cells cells assessed as cell proliferation after 70 hrs by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1785330Inhibition of full length human CDK6 (1 to 326 end residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system at 100 nM preincubated for 10 mins followed by substrate and ATP addition by mobility shift a
AID1863172Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID1478590Inhibition of HDAC1/2 in human HeLa cell nuclear extract using COLOR DE LYS as substrate pretreated for 5 mins followed by substrate addition measured after 30 mins by UV-absorption method2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID446344Half life in CD1 mouse at 15 mg/kg, po2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID1067345Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1832689Inhibition of human HDAC5 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID347874Growth inhibition of human prostate cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID1578501Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 9.2 to 9.63 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1819555Antitumor activity against mouse B16-F10 cells xenografted in C57BL/6J mouse assessed as change in tumor cell morphology into normal tissue at 60 mg/kg, IG administered for 12 days by H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1260644Inhibition of human recombinant HDAC8 at 20 uM using Ac-RHK(Ac)K(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1901768Cytotoxicity against human MRC9 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1901786Binding affinity to full length HDAC6-NanoLuc fusion protein (unknown origin) expressed in HeLa cells assessed as residence time by NanoBRET assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1525776Inhibition of HADC6 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1898894Antiproliferative activity against human NCI-H460 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID673990Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID750109Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
AID764219Inhibition of HDAC in human HeLa cell extract using Fluor deLys as substrate by fluorimetric assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1771459Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1848631Cytotoxicity against human SN12C cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1337253Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID208379Tested for morphological alterations in T/5 cells after administration along with DMSO (0.1%)1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID732143Inhibition of HDAC7 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.
AID1464873Anti-proliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1361659Antitumor activity against human A549 cells xenografted in BALB/C nude mouse assessed as inhibition of tumor growth at 100 mg/kg, po administered once daily for 21 days starting day 11 after tumor cells implantation2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1890330Stability in mouse plasma incubated for 6 hrs in presence of NADPH and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1742665Cytotoxicity against human NCI-1581 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1280269Inhibition of class1 HDAC in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 10 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID408885Inhibition of HDAC62008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1141764Cytotoxicity against human PC3 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1467236Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 0.2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition measured within 30 mins by fluorome2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID670514Inhibition of HDAC derived from human HeLa cell nuclear extract using Boc-Lys(acetyl)-AMC as substrate incubated for 5 mins prior to substrate addition measured after 30 mins by fluorimetry2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.
AID1762496Inhibition of HDAC2 (unknown origin)2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID1897807Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC62022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.
AID737909Cytotoxicity against human HS68 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1182316Antiproliferative activity against hTERT expressing immortalized human HPNE cells after 48 hrs by MTT assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
A potent HDAC inhibitor, 1-alaninechlamydocin, from a Tolypocladium sp. induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
AID1688022Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition after 72 hrs by trypan blue staining based cell counting assay2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1260645Inhibition of human recombinant HDAC9 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID760511Inhibition of HDAC2 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1128557Inhibition of human HDAC-4 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1371071Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID765390Inhibition of recombinant human HDAC8 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1189850Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID663386Growth inhibition of human UACC62 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1365023Inhibition of recombinant human HDAC2 preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID297481Cytotoxicity against human MDA-MB-231cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID544092Antimalarial activity against drug-resistant Plasmodium falciparum TM91C2352008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1164186Inhibition of human recombinant HDAC4 using (S)-[5-Acetylamino-1-(2-oxo-4-trifluorometyl-2Hchromen-7-ylcarbamoyl)pentl]carbami acid tert-Butyl Ester as substrate after 1 hr by fluorescent activity assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1383992Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1240550Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID1771458Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1597954Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 uM incubated for 72 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometric analysis (Rvb = 1.8%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID748979Inhibition of HDAC in human K562 cells2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID655476Inhibition of recombinant human HDAC1 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1380985Antitumor activity against human HT-29 cells xenografted in BALB/c nu mouse assessed as tumor growth level at 100 mg/kg, po administered for 25 consecutive days measured every 3 days during compound dosing relative to control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1698860Inhibition of HDAC1 (unknown origin) at 100 nM relative to control2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
AID1177048Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1452273Inhibition of HDAC1 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID1303632Potentiation of 5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 25 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1055350Cytotoxicity against human HCT116 cells after 96 hrs by MTS-PMS assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID1915598Inhibition of HDAC5 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID748978Inhibition of HDAC8 (unknown origin)2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
A cyclodextrin-capped histone deacetylase inhibitor.
AID1647327Anti-vascular cognitive impairment activity against bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model assessed as improvement in short-term non-spatial working memory by measuring increase in novel object recognition2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1550102Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1383998Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
AID1433303Induction of apoptosis in p53 null human U937 cells assessed as increase in Bim EL expression level by measuring ratio of Bim EL to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1730853Antiproliferation activity against human NCI-H838 cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1901764Inhibition of full length human recombinant HDAC11 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of HDAC6-Selective Inhibitor NN-390 with
AID1275076Inhibition of HDAC in human HeLa nuclear extract2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID1486677Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1597935Antiproliferative activity against human SGC7901 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID440823Inhibition of human recombinant N-terminal FLAG-tagged HDAC7 (438-915) expressed in baculovirus after 10 mins by fluorimetric analysis2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
AID1155330Cytotoxicity against human HepG2 cells after 48 hrs2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID619046Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1485113Inhibition of SIRT2 in human U373 cells assessed as increase of alpha-tubulin acetylation at 2 uM after 8 hrs by Western blotting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1514595Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1690838Inhibition of recombinant human full-length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence2020European journal of medicinal chemistry, Apr-15, Volume: 192Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
AID1864221Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1126997Induction of apoptosis in human U937 cells assessed as late apoptotic cells using annexin-V/propidium iodide staining at 1 uM after 24 hrs by flow cytometry analysis (Rvb = 2.13%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1356299Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay
AID1246524Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for imatinib resistant human IR-K562 cells2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1566036Selectivity index, ratio of IC50 for recombinant human HDAC6 to IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells2019European journal of medicinal chemistry, Nov-15, Volume: 182A fluorine scan on the Zn
AID1826630Synergistic antiproliferative effect on HEL cells assessed as combination index at 1.11 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1321728Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation after 2 hrs by Western blot analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1550152Drug level in BALB/c nu mouse xenografted with HEL cells at 100 mg/kg/day, ip administered for 5 days and measured after 0.5 to 4 hrs by LC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID414726Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
AID1597927Inhibition of HDAC8 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1897368Inhibition of FGFR1 (unknown origin) at 100 nM relative to control
AID593550Inhibition of human HDAC5 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1848578Inhibition of HDAC in human NCI-H522 cells assessed as increase in acetylation of H3 at 2.5 to 10 uM measured for 3 days by Western blot analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1173497Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1481748Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors.
AID1753639Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylated alpha-tubulin levels at 1 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1848282Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID1622930Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1753835Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1832692Inhibition of full length human C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1821264Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1742180Inhibition of recombinant human full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
AID1394900Inhibition of HDAC in human HL60 cells assessed as upregulation of acetylated histone H3 levels at 0.1 to 3 uM after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1737655Cytotoxicity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID1591716Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1633673Immunomodulatory activity in mouse N9 cells assessed as reduction in LPS-induced iNOS expression at 5 to 25 uM incubated for 24 hrs by Western blot analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.
AID1897467Inhibition of HDAC in human SNU-16 cells assessed as upregulation of acetyl-histone 3 level at 1.25 to 5 uM incubated for 36 hrs by Western blot analysis
AID438218Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC1/2 from human HeLa cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
AID297495Cytotoxicity against human U87MG cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1282253Cytotoxicity against human K562 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID717793Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 3.125 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1576465Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 5 uM after 72 hrs by Annexin V-phycoerythrin/7-AAD staining based flow cytometric analysis (Rvb = 1.13%)
AID1769657Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1129794Induction of apoptosis in human Jurkat cells assessed as caspase 3/7 activation at 10 uM after 12 hrs by luminescence assay (Rvb = 69,935 +/- 7003.63 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1303560Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 to 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID492804Inhibition of human recombinant HDAC4 after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1401392Inhibition of HDAC6 in human HeLa-S3 cell lysates assessed as remaining activity at 1 uM preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1250658Selectivity ratio of GI50 for human DU145 cells to GI50 for human HLF cells2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1431814Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1653145Cytotoxicity against human HepG2 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID286791Effect on alpha tubulin acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID1597929Antiproliferative activity against human NCI-H226 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1433284Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID711155Inhibition of HDAC6 by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID310180Inhibition of HDAC in HeLa cell lysates2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1515983Inhibition of HDAC in human MM1S cells assessed as increase in histone H3 acetylation at 100 nM measured after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity.
AID1676600Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID527206Inhibition of ERK phosphorylation in human A549 at 5 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1856994Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID329914Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID465151Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1723744Selectivity index, ratio of IC50 for inhibition of human recombinant HDAC1 to IC50 for inhibition of human recombinant HDAC62020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
AID1433239Induction of apoptosis in p53 null human U937 cells at 2 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1760292Antiproliferative activity against human A549 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
AID1525779Inhibition of HADC3 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1421908Cytotoxicity against human HepG2A16 cells expressing GFP-fused CD81 after 48 hrs by bioluminescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID708272Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1165106Selectivity ratio of IC50 for axenic amastigote stage of Leishmania donovani to IC50 for amastigote stage of Leishmania donovani infected in human THP1 cells2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
AID619261Antitumor activity against human HCT116 cells xenografted in athymic nu/nu Harlan mouse assessed as tumor growth inhibition at 300 mg/kg, po qd for 21 days measured on day 222011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1312903Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as body weight loss at 50 mg/kg, ip administered every 2 days for 8 days measured on day 8 post last dose2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1067343Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1245689Ratio of IC50 for Class 1 histone deacetylase in human PC3 cells to IC50 for Class 1 histone deacetylase isolated from human HeLa cell nuclear extracts2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID90211Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Heterocyclic ketones as inhibitors of histone deacetylase.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID652766Induction of CFTR deltaF508 mutant protein expression in cystic fibrosis patient lung cells relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1785333Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID1816224Induction of apoptosis in mouse 4T1 cells assessed as viable cells at 5 uM measured after 48 hrs in presence of ruxolitinib by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 89.5%)
AID1437251Inhibition of HDAC6 in mouse B16F10 cells assessed as accumulation of acetylated tubulin at 20 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID1141769Cytotoxicity against human MCF7 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1915569Cytotoxicity against human MCF7 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID499802Inhibition of HDAC62010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID605394Inhibition of human recombinant HDAC3 using fluor de Lys as substrate by fluorometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID675300Antiproliferative activity against human HCT116 cells after 5 days by Alamar Blue assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
AID1303686Inhibition of HDAC3 in human Jurkat cells extract after 30 mins by immunoprecipitation assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1826634Synergistic antiproliferative effect on HEL cells assessed as combination index at 0.014 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID780575Inhibition of HDAC in human HeLa cell nuclear extracts using Color de LysTM after 30 mins2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
AID1119181Cytotoxicity against human MCF7 cells after 96 hrs by MTA reduction assay2012MedChemComm, , Volume: 3, Issue:1
Polyamine-based small molecule epigenetic modulators.
AID358681Increase in REST/NRSF mRNA expression in rat ST14A cells after 72 hrs by RT-PCR relative to control2007The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators.
AID609493Inhibition of human ERG by automated patch clamp assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID637890Inhibition of recombinant human HDAC7 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases.
AID1630595Inhibition of HDAC in human MOLT4 cells assessed as H3K23 acetylation at 2.5 uM after after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID699752Inhibition of SIRT52012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Substrates for efficient fluorometric screening employing the NAD-dependent sirtuin 5 lysine deacylase (KDAC) enzyme.
AID1250666Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1655786Inhibition of human EZH2 using core histone as substrate incubated for 1 hr by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID1437244Cytotoxicity against human A375 cells assessed as growth inhibition after 72 hrs by MTS assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID1476166Cytotoxicity against human AC10 cells assessed as cell viability after 24 hrs by CellTiter-Glo assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1246521Cytotoxicity against human U937 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1462223Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1541464Inhibition of class 1 HDAC in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 0.5 uM preincubated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT 2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID303346Growth inhibition of MCF7 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID90199Experimental anti-HDAC (anti-histone deacetylase) activity of the compound2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors.
AID760506Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1702153Metabolic stability in mouse liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID748101Inhibition of HDAC6 in human HeLa cells assessed as increase in alpha tubulin acetylation at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1337278Antiproliferative activity against human HL60 cells2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1452276Antiproliferative activity against human U937 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID1901154Inhibition of HDAC8 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1730854Inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID663332Growth inhibition of human A549 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID90677Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID1478592Inhibition of HDAC6 (unknown origin) using substrate after 30 mins by fluorometric analysis2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1688039Induction of apoptosis in human HL-60 cells assessed as early apoptotic cells at 2 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 2.46 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1129781Cell cycle arrest in human Jurkat cells assessed as accumulation at G1-phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 60.90%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1808547Inhibition of recombinant human full length C-terminal His- tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1845459Inhibition of HDAC1 (unknown origin)2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?
AID1515927Antitumor activity against human HGC27 cells xenografted in athymic nude BALB/c mouse assessed as tumor growth inhibition at 100 mpk, po measured 2 times every week2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1542188Inhibition of HDAC10 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID1482116Cytotoxicity against human HL60 cells assessed as growth inhibition after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1702049Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1454052Growth inhibition of human K562 cells after 3 days by counting method2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID586615Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1415662Induction of apoptosis in human HepG2 cells at 5 uM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry relative to control2017MedChemComm, Jun-01, Volume: 8, Issue:6
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.
AID1888589Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
AID1897374Inhibition of HDAC8 (unknown origin)
AID1497926Induction of CRBN ubiquitin ligase-mediated HDAC4 degradation in human MCF7 cells assessed as decrease in HDAC4 levels at 10 uM after 12 hrs by immunoblotting analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Development of the first small molecule histone deacetylase 6 (HDAC6) degraders.
AID1897366Inhibition of HDAC6 (unknown origin)
AID1760296Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
AID1390023Antiproliferative activity against human HEL cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1848612Cytotoxicity against human SNB-75 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1898916Inhibition of HDAC6 in human NCI-H460 cells at 7.4 uM assessed as increase in alpha-tubulin acetylation measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1129771Inhibition of HDAC in human Jurkat cells assessed as increase in H3K9 acetylation at 10 uM after 12 hrs by FACS flow cytometric analysis relative to control2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1578895Inhibition of HDAC in human Bel7402 cells assessed as increase in acetylated histone h3 expression at 5 uM incubated for 72 hrs by Western blot analysis2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID1356296Inhibition of HDAC derived from human HeLa nuclear extract at 1 uM by fluorimetric assay relative to control
AID767621Cytotoxicity against human HT1080 cells2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Inhibitory effects of p-dodecylaminophenol on the invasiveness of human fibrosarcoma cell line HT1080.
AID1384228Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 1000 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1321703Inhibition of HDAC6 (unknown origin)2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1785332Inhibition of HDAC1 (unknown origin) measured after 30 mins by fluorescence microplate reader assay
AID1164030Inhibition of human recombinant HDAC7 after 60 mins by fluorimetric assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1181308Inhibition of HDAC1 in human U937 cells assessed as increase in p21WAF1/CIP1 level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID546563Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID524999Inhibition of HDAC6 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID628210Antiproliferative activity against human HeLa cells after 48 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1462226Inhibition of BRD4/HDAC1 in human OCI-AML3 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1763815Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID274064Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1398801Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1275078Inhibition of recombinant human HDAC62016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID465156Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID499801Selectivity ratio IC50 for HDAC8 to IC50 for HDAC in human HeLa cells nuclear extract2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID1630602Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID663400Growth inhibition of human MCF7 cells after 48 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID747255Growth inhibition of HUVEC by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1541456Inhibition of recombinant human N-terminal GST-fused and C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measu2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1566809Inhibition of recombinant C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID670014Selectivity index, ratio of IC50 for human recombinant HDAC6 to IC50 for human recombinant HDAC12012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID1202583Inhibition of His-tagged HDAC1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID1282250Cytotoxicity against human U266 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID748108Inhibition of HDAC7 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1162219Cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 1 uM by propidium iodide staining-based flow cytometry (Rvb = 17.3%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID525035Inhibition of CFTR transcription assessed as decrease of CFTR protein level at 50 uM by immunoblot method2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID764217Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1469396Induction of apoptosis in human Hep3B cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.25%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1487094Inhibition of HDAC3 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID1753636Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-based assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1771467Inhibition of HDAC (unknown origin)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1630629Inhibition of HDAC in human MOLT4 cells assessed as H4K12 acetylation at 2.5 uM after after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1055353Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID1202595Cytotoxicity against human A549 cells at 100 uM after 72 hrs by MTS assay2015European journal of medicinal chemistry, , Volume: 96Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.
AID1731759Inhibition of recombinant human HDAC1 using Ac-LGK(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 90 mins by fluorescence based assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
AID1614134Inhibition of recombinant full length N-terminal GST-tagged human HDAC5 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1652196Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1763818Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human MCF7 cells2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
AID1622939Inhibition of recombinant full-length human HDAC11 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1266856Antitumor activity against human HCT116 cells xenografted in BALB/c mouse assessed as tumor weight at 90 mg/kg, po measured twice per week over 22 days (Rvb = 1.38 +/- 0.13 g)2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1127332Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID732872Inhibition of HDAC6 in human MDA-MB-231 cells assessed as acetylation levels of tubulin at 1 uM after 3 to 24 hrs by Western blot analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1433296Induction of DNA damage in p53 null human U937 cells assessed as increase in gammaH2AX expression level by measuring ratio of gammaH2AX to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID659635Antiproliferative activity against human SKMES1 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1398805Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1623523Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate-3 by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID476650Toxicity in FVB mouse assessed as mortality at 50 mg/kg, po administered 5 times per week for 2 weeks measured up to 1 month2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1864228Inhibition of full length recombinant N-terminal GST-tagged human HDAC11 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1348916Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.
AID1816687Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1486301Antiproliferative activity against human U937 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID274031Inhibition of MCF7 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1245685Cytotoxicity against human U266 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID476649Toxicity in FVB mouse assessed as mortality at 50 mg/kg, po administered 5 times per week for 2 weeks2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1128559Inhibition of human HDAC-6 using RHKK(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID1233269Inhibition of human recombinant HDAC6 after 15 mins by fluorogenic assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
AID1845908Reversal of HIV-1 latency infected in GFP-fused human J-Lat C11 cells assessed as increase in GFP expression at 2 uM incubated for 3 hrs by flow cytometry2021European journal of medicinal chemistry, Mar-05, Volume: 213HIV latency reversal agents: A potential path for functional cure?
AID1848621Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID732443Inhibition of human HCT116 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1239057Inhibition of HDAC in human RPMI8226 cells assessed as upregulation of acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID420636Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC50 after 24 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID392399Inhibition of human recombinant N-terminal histidine-tagged HDAC6 expressed in baculovirus by fluorimetry2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Sulfamides as novel histone deacetylase inhibitors.
AID1702133Inhibition of HDAC6 in human HuH-7 cells assessed as alpha-tubulin Lys40 acetylation level at 10 uM incubated for 4 hrs including last 12 mins stimulation with 20 ng/ml growth factor VEGF by Western blot analysis (Rvb = 3.8 %)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1864222Cytotoxicity against human SUM159PT cells assessed as reduction in cell viability measured after 48 hrs2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1466402Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as relative tumor increment ratio at 100 mg/kg/day administered via oral gavage for 16 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1848588Induction of ferroptosis in human NCI-H522 cells assessed as viability at 5 uM incubated after 60 hrs by microscopic analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID1659652Inhibition of HDAC8 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID652747Inhibition of recombinant human HDAC3-NCoR2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1808550Inhibition of recombinant human full length N-terminal GST-tagged HDAC5 expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1181310Induction of cell cycle arrest in human U937 cells assessed as accumulation at S phase at 5 uM after 48 hrs by propidium iodide staining based FACS method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID404444Cytotoxicity against human Panc 04.03 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1865273Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 2.5 uM measured after 24 hrs by flow cytometry2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1225982Inhibition of recombinant N-terminal GST-tagged full length human HDAC6 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1627671Inhibition of HDAC in human HL60 cells assessed as upregulation of alphatubulin acetylation levels at 2 uM after 18 hrs by SDS-PAGE analysis2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Synthesis, biological evaluation and molecular modeling studies of psammaplin A and its analogs as potent histone deacetylases inhibitors and cytotoxic agents.
AID1566821Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1876461Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence plate reader assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1816685Inhibition of recombinant LSD1 (157 to 852 residues) (unknown origin) expressed in Escherichia coli BL21 (DE) using H3K4me2 as substrate by amplex red assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID545856Antimalarial activity against Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1293559Antiproliferative activity against human LoVo/DX cells assessed as reduction in cell number after 72 hrs by cell counter analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID1667075Inhibition of HDAC1 in human MDA-MB-231 cells assessed as accumulation of acetylated H4 at 1.5 uM by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1164904Inhibition of HDAC1/2/3 in human HeLa cells assessed as p21 gene expression at 10 uM after 15 hrs by luciferase reporter gene assay relative to SNDX-2752014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1384227Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 100 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1845320Inhibition of BRD4 (unknown origin) by ELISA2021Bioorganic & medicinal chemistry letters, 01-01, Volume: 31Current status in the discovery of dual BET/HDAC inhibitors.
AID274013Inhibition of CYP450 3A42007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1410341Inhibition of HDAC in human HCT116 cells assessed as decrease in acetylated histone H3 levels after 12 hrs by Western blot analysis2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.
AID780574Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
AID1487093Inhibition of HDAC2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
AID1865257Induction of apoptosis in human MV4-11 cells at 1 uM incubated for 24 hrs in presence of SHP099 by propidium iodide and annexin-V staining based flow cytometry2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID663405Half life in mouse plasma2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1439355Inhibition of HDAC6 in human RPMI8226 cells assessed as increase in tubulin acetylation at 3 uM after 24 hrs by western blot analysis2017European journal of medicinal chemistry, Mar-10, Volume: 128Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID1887690Cytotoxicity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1897394Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 0.03 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.41%)
AID626562Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 0.1 uM by fluorescence spectrophotometry2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
AID366641Inhibition of HDAC2 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID732445Inhibition of human A549 cell proliferation after 48 hrs by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID366646Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID670104Antitumor activity against human A549 cells xenografted in nude mouse assessed as tumor growth inhibition at 200 mg/kg, po administered QD till end point2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
AID1487009Selectivity index, ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1821269Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1129777Cell cycle arrest in human Jurkat cells assessed as accumulation at G1-phase at 10 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 65%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1819502Inhibition of HDAC in human HeLa nuclear extract using fluorogenic substrate incubated for 30 mins by fluorescence based assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1754755Inhibition of N-terminal GST-tagged human recombinant full length HDAC5 expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1765331Selectivity index, ratio of IC50 for human recombinant full length HDAC6 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID327545Increase in acetylated histone H3 level in human HCT116 cells at 10 uM after 24 hrs relative to control2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID1775567Inhibition of human G9a enzyme using histone monomethyl-H3K9 peptide as substrate incubated for 1 hr in presence of SAM by TR-FRET assay2021Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
AID316893Inhibition of HDAC82008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1819513Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID527039Cytotoxicity against human NCI-H2126 by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells.
AID1572340Cytotoxicity against human HepaRG cells assessed as cell viability at 100 uM after 24 hrs by CellTiter blue-reagent based assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1234899Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1816968Cytotoxicity against human HeLa cells assessed as cell death incubated for 20 hrs measured by DNS assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their
AID1266095Inhibition of HDAC6 (unknown origin) by fluorimetric assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1401482Selectivity ratio of IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell to IC50 for HDAC2 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1441653Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in TNFalpha level at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by ELISA relative to LPS alone2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1401547Antiproliferative activity against human NB4 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID511068Inhibition of HDAC in human HeLa cells at 0.1 uM after 15 mins2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1403160Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1861650Antiproliferative activity against human SW480 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
AID1487002Inhibition of HDAC6 (unknown origin) by ELISA-based assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1769642Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1303623Potentiation of 0.1 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1367347Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Synthesis and biological evaluation of Santacruzamate-A based analogues.
AID1548259Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay
AID1863174Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID420637Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC50 after 48 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1578154Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1812444Inhibition of human recombinant HDAC3 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1848303Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.04%)2022Bioorganic & medicinal chemistry, Nov-15, Volume: 74Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
AID717827Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1855256Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1449320Antiproliferative activity against human Med8A cells after 72 hrs by Celltiter-Glo assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1441651Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta level pretreated intraperitoneally for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1896927Antiproliferative activity against human NALM-6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID1273870Inhibition of HDAC2 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1709359Induction of apoptosis in human Jurkat cells assessed as early apoptotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 6.05%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1819535Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as heart damage at 60 mg/kg, IG administered for 12 days H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1742742Genotoxicity in Salmonella typhimurium TA100 by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1845307Inhibition of HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, 01-01, Volume: 31Current status in the discovery of dual BET/HDAC inhibitors.
AID316936Inhibition of HDAC72008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1129798Inhibition of HDAC in human Jurkat cells assessed as increase in H3K9 acetylation by measuring geometric mean fluorescence intensity at 10 uM after 12 hrs by FACS flow cytometric analysis (Rvb = 5.91 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1915566Cytotoxicity against African green monkey Vero cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1275246Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.
AID1170745Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1174703Induction of apoptosis in human U937 cells assessed as apoptotic cells at 1.5 uM after 24 hrs by annexin-V/propidium iodide staining-based flow cytometry2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID1339587Growth inhibition of human U937 cells after 44 hrs by MTT assay2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID324954Inhibition of wild type HDAC4 expressed in Escherichia coli at 10 uM2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1469324Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.53%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1486321Genotoxicity in Salmonella typhimurium TA97 at 50 times antiproliferative IC50 by Ames test2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
AID1511138Inhibition of HDAC9 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID1861265Selectivity index, ratio of IC50 for inhibition of HDAC4 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
AID663473Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1845914Inhibition of HIV-1 latency in human CD4+ve Th cells infected NL4.3-Luc virus assessed as p24 expression level incubated for 48 hrs by v450 dye based flow cytometry2021European journal of medicinal chemistry, Mar-05, Volume: 213HIV latency reversal agents: A potential path for functional cure?
AID1534443Cytotoxicity against human A549 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer.
AID1816221Induction of apoptosis in mouse 4T1 cells assessed as early apoptotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.12%)
AID274021AUC after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID481574Cytotoxicity against mouse S180 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID246120Effective Concentration of compound to inhibit the growth of human MDA-MB-231 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1486678Inhibition of HDAC2 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1434360Inhibition of HDAC in HEK293 cells assessed as myc-tagged RUNX3 expression by measuring ratio of RUNX3 level to beta-actin level at 1 uM measured after 24 hrs by Western blot analysis relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators.
AID1235108Inhibition of HDAC1/2 in human HeLa cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1622975Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1784980Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1061953Inhibition of human HDAC3/NCOR2 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1355705Antifungal activity against FLC resistant Candida albicans 0304103 after 48 hrs by checkerboard microdilution method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1633433Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of GAP43 mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
AID1689776Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID695301Upregulation of Nanog gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes.
AID1578157Inhibition of FITC-geldanamycin binding to recombinant human full-length C-terminal His-tagged HSP90alpha expressed in Escherichia coli after 3 hrs by fluorescence polarization assay2020European journal of medicinal chemistry, Jan-01, Volume: 185N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
AID1812436Cytotoxicity against human HL-60 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1816723Induction of apoptosis in human MGC-803 cells assessed as apoptotic cells at 5 uM incubated for 48 hrs by annexin V-FITC and PI staining based flowcytometry analysis (Rvb =4.3 %)2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1684875Antitumor activity against mouse LL/2 cells inoculated in C57BL/6J mouse assessed as reduction of tumor weight at 25 mg/kg, ip administered for 12 days measured at day 14 (Rvb = 0.98 +/- 0.07 g)
AID1485114Inhibition of SIRT2 in human Hs683 cells assessed as increase of alpha-tubulin acetylation at 2 uM after 8 hrs by Western blotting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1129799Inhibition of HDAC in human Jurkat cells assessed as increase in H3K23 acetylation by measuring geometric mean fluorescence intensity at 10 uM after 12 hrs by FACS flow cytometric analysis (Rvb = 20.20 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID347872Growth inhibition of human renal cancer cells at 10 uM relative to control2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Histone deacetylase inhibitors through click chemistry.
AID366652Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1367348Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Synthesis and biological evaluation of Santacruzamate-A based analogues.
AID1486671Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID395022Inhibition of recombinant HDAC1 by fluorimetric assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
AID1386686Inhibition of HDAC in human GM18453 cells harboring NPC1 mutant assessed as increase in total NPC1 protein expression at 5 uM pretreated for 48 hrs followed by endoglycosidase H addition and measured after overnight incubation by Western blot analysis rel2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1890513Inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1441664Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in TNFalpha level pretreated at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1622972Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1667076Inhibition of HDAC6 in human MDA-MB-231 cells assessed as accumulation of acetylated tubulin at 1.5 uM by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1280274Selectivity index, ratio of HDAC6 inhibition in human HeLa cells assessed as ratio of acetylated tubulin to GAPDH level at 0.1 uM over class1 HDAC inhibition in human HeLa cells assessed as ratio of acetylated histone H3 to GAPDH level at 0.1 uM2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1541445Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1784972Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1433254Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1572348Inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 1 uM after 4 hrs by Western blot assay relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1728924Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 5 days by beckman coulter counting method2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1326527Toxicity in nude mouse xenografted with human HCT116 cells assessed as change in body weight at 50 to 100 mg/kg, po qd2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1650411Inhibition of recombinant human HDAC42020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID672024Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1403155Inhibition of HDAC8 (unknown origin)2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1441644Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in protein concentration in BALF at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1401479Selectivity ratio of IC50 for HDAC3 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1622909Inhibition of recombinant human GST-fused HDAC1 expressed in HEK293 cells Fluor-de-lys as substrate measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1055713Antiproliferative activity against human NCI-H460 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1482167Cytotoxicity against human HL60 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1667070Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1380944Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID605533Antiproliferative activity against human HepG2 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1511968Inhibition of full length recombinant GST-tagged N-terminal human HDAC6 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
AID1547265Inhibition of HDAC9 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID90214Inhibitory activity was tested against histone deacetylase (HDAC).2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
AID1566823Antiproliferative activity against human JeKo1 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID1141773Induction of apoptosis in human HCT116 cells assessed as increase in p53 protein level at 0.1 to 3 uM after 24 hrs by immunoblotting analysis2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1737138Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID241538Inhibitory concentration against maize histone deacetylase 1-B (class I HDAC)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID1141772Cytotoxicity against human HT-29 cells by MTT assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.
AID1846130Inhibition of HDAC1 (unknown origin)2021Bioorganic & medicinal chemistry letters, Apr-15, Volume: 38Current status in the discovery of dual BET/HDAC inhibitors.
AID511065Inhibition of HDAC32010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design and synthesis of novel isoxazole-based HDAC inhibitors.
AID1339568Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.
AID632974Cytotoxicity against human AsPC1 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1845917Inhibition of HIV-1 latency infected in human ACH-2 cells assessed as fold increase in HIV production by measuring p24 level incubated for 48 hrs in presence of BIX01294 by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213HIV latency reversal agents: A potential path for functional cure?
AID1547331Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in IL6 mRNA level at 10 uM after 24 hrs by RT-PCR analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID607634Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
AID1676593Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1821271Inhibition of HDAC2 (unknown origin) incubated for 30 mins by microplate reader assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1441661Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in TNFalpha mRNA level at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by qRT-PCR method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1653095Antiproliferative activity against human A549 cells by CCK8 assay2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1361644Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1321739Inhibition of PDE5A in human SH-SY5Y cells assessed as increase in CREB phosphorylation at Ser133 residue at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1578504Induction of apoptosis in human MV4-11 cells assessed as viable cells at 4 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 53.01 to 53.07 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1709349Cytotoxicity against human NAMALVA cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1282229Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1355735Antitumor activity in human HEL cells xenografted in SCID mouse assessed as mouse survival at 10 mg/kg, ip qd measured after 10 days2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
AID1406991Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID316926Inhibition of human SW620 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1293572Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID492813Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID496802Inhibition of human HDAC22010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID663344Growth inhibition of human CCRF-CEM cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID366649Antiproliferative activity against human Panc04.03 cells after 72 hrs by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1321729Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 after 2 hrs by Western blot analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1832693Inhibition of human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method2021European journal of medicinal chemistry, Dec-05, Volume: 225Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.
AID1235109Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1739569Antiproliferative activity against human HL60 assessed as reduction in cell growth at 20 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1897407Induction of apoptosis in human SNU-16 cells assessed as dead cells at 1 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 2.65%)
AID404447Cytotoxicity against human HPDE6c7 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1129795Induction of apoptosis in human Jurkat cells assessed as caspase 3/7 activation at 10 uM after 24 hrs by luminescence assay (Rvb = 136,627 +/- 31846.96 no unit)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1266840Activation of p53 in human HCT116 cells assessed as p53 phosphorylation at ser15 residue at 0.1 to 5 uM after 12 hrs by western blot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1727743Inhibition of HDAC11 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1769651Inhibition of ALK (unknown origin) preincubated for 10 mins followed by addition of substrate and ATP for 25 mins by caliper EZ reader method2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID1437243Cytotoxicity against mouse B16F10 cells assessed as growth inhibition after 72 hrs by MTS assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.
AID1515982Induction of HDAC6 degradation in human MM1S cells assessed as increase in alpha tubulin acetylation at 100 nM measured after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity.
AID1065630Inhibition of HDAC4 in human Jurkat E6.1 cells using Boc-Lys-Ac as substrate incubated for 2 hrs prior to substrate addition measured after 3 hrs by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1312867Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID488275Inhibition of HDAC32010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID760501Cytotoxicity against human NCI60 cells after 48 hrs by SRB assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1597973Antimigratory activity in human A549 cells at 5 to 10 uM incubated for 12 hrs in presence of mitomycin by inverted microscopic-based wound healing assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1394901Inhibition of HDAC in human HL60 cells assessed as upregulation of acetyl-alpha-tubulin levels at 0.1 to 3 uM after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1394888Inhibition of HDAC in human HeLa nuclear extract using Ac-Lys(Ac)-pNA as substrate measured after 30 mins by fluorometric analysis2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1065634Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
AID1876471Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.73 %)2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
AID1401904Inhibition of human recombinant HDAC6 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID670970Inhibition of human recombinant His6-tagged and GST-fuses HDAC1 expressed in insect High5 cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
CCLab--a multi-objective genetic algorithm based combinatorial library design software and an application for histone deacetylase inhibitor design.
AID619054Competitive inhibition of HDAC9 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1467234Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1869148Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
AID695302Upregulation of Sox2 gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes.
AID1162485Growth inhibition of human HCT116 cells after 72 hrs by CellTiter Glo assay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
AID1337279Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID652762Inhibition of HDAC3-NCoR2 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1403153Inhibition of HDAC3 (unknown origin)2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1426426Antiparasitic activity against drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as growth inhibition after 48 hrs by SYBR green 1 dye-based flow cytometry2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID760503Inhibition of HDAC10 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID1511135Inhibition of HDAC5 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.
AID499811Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
AID711156Inhibition of HDAC4 by fluorometric assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.
AID1547314Increase in LIFR expression in tumor tissue of BALB/cAnNCrl mouse xenografted with human HCT116 cells at 30 mg/kg, po administered on day 1 to day 19 measured on day 19 by immunohistochemical analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID760519Cytotoxicity against human HMEC after 72 hrs by WST1 assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Development of a chimeric c-Src kinase and HDAC inhibitor.
AID760373Cytotoxicity against HDF after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1547259Inhibition of human recombinant His-tagged BRD3 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID628287Antiproliferative activity against human HepG2 cells after 48 hrs by XTT assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID524998Inhibition of HDAC5 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID670013Inhibition of human recombinant HDAC1 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID1164798Intrinsic clearance in human hepatocytes assessed per million cells at 5 uM by LCMS/MS analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1454050Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1598103Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID1614130Inhibition of recombinant full length HDAC6 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID1742703Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 5 uM incubated for 72 hrs by annexinV-FITC and PI staining based flow cytometry analysis (Rvb = 90.3 %)2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1251319Growth inhibition of human IGROV1/Pt1 cells after 72 hrs2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
AID1737154Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 10 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.51%)2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID1863173Inhibition of HDAC3 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
AID1396960Antiproliferative activity against human PC3 cells2018Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
AID1819531Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as effect on body weight at 60 mg/kg, IG administered for 12 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID603542Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.
AID434539Cytotoxicity against human HCT116 cells after 24 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.
AID1598093Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID586608Antimalarial activity against trophozoites stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1784187Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 90 mins by fluorescence based micro plate assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.
AID322422Antitumor activity against human LNCap cells xenografted SCID mouse model at 20 to 10 mg/kg/day, sc relative to control2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID1200985AUC (0 to infinity) in ICR mouse at 50 mg/kg, po2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.
AID1890334Stability in human liver microsomes assessed as half-life and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1126999Induction of apoptosis in human U937 cells assessed as necrotic cells using annexin-V/propidium iodide staining at 0.5 uM after 24 hrs by flow cytometry analysis (Rvb = 0.06%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1227046Drug degradation in human plasma assessed as unidentifiable product formation after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID1349721Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1633992Inhibition of HDAC6 in human HuH7 cells assessed as increase in alpha-tubulin K40 acetylation at varying concentrations incubated for 24 hrs by Western blot analysis2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
AID761580Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID1061955Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1361638Inhibition of HDAC in human A549 cells assessed as increase in histone H3 acetylation after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1487087Selectivity index, ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC3 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1659656Antiproliferative activity against human A549 cells incubated for 24 hrs by CCK8 assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID1808548Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1900936Toxicity in mouse bearing intracranial tumor assessed as last day of survival at 50 mg/kg, ip in presence of clorgyline for 10 days (Rvb=16 days)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID350725Growth inhibition of human HBC5 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID488355Agonist activity at VDR in human SCC4 cells assessed as induction of CYP24 gene expression at 1 uM after 5 to 10 mins by RT-PCR analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID352522Antiproliferative activity against human HUPT3 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1886182Inhibition of HDAC in human HeLa cells using BOC-K(Ac)-AMC as substrate at 1 uM measured after 30 mins by fluorescence based microtiter plate reader assay relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1572377Ratio of inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 10 uM to inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 1 uM2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
AID1742627Inhibition of HDAC in human HeLa cell extracts assessed as inhibition of substrate deacetylation using Boc-Lys (q-Ac)-AMC as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1449682Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity.
AID1667071Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1578476Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1166497Inhibition of human recombinant full length HDAC3 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
AID1401477Selectivity ratio of IC50 for HDAC1 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1865303Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on kidney at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID297484Cytotoxicity against human A2780 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1676590Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1485112Inhibition of SIRT1 in human Hs683 cells assessed as increase of histone H4 acetylation at 2 uM after 8 hrs by Western blotting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1441675Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as MPO activity at 50 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 (Rvb = 0.98 U/g)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1882457Inhibition of HDAC2 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID90344Induction of p21 using Histone deacetylase inhibitors2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1578495Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 0.5 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 9.2 to 9.63 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID593549Inhibition of human HDAC4 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID1164914Inhibition of HDAC9 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1887063Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis.
AID1722284Inhibition of HDAC6 in human MDA-MB-231 cells assessed as accumulation of alpha tubulin acetylation at 1.25 to 5 uM incubated for 24 hrs by Western blot analysis2020Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.
AID1380943Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1848618Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition at 10 uM incubated for 24 hrs by MTT assay2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
AID438217Inhibition of HDAC82009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
AID1246523Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human K562 cells2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1742663Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1177053Antiprotozoan activity against Plasmodium falciparum NF54 IEF forms2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1541460Inhibition of class 1 HDAC in human CAL27 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 0.5 uM preincubated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assa2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1865301Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on spleen at 40 mg/kg, po qd administered for 12 days2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID294382Inhibition of HDAC by fluorescent assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.
AID663470Half life in mouse liver microsomes2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID608776Inhibition of HDAC in human HeLa cells using Ac-Arg-Gly-Lys(Ac)-AMC as fluorescent substrate after 20 mins by fluorescence assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure-based optimization of click-based histone deacetylase inhibitors.
AID1128561Inhibition of human HDAC-8 using RHK(Ac)K(Ac) as substrate2014European journal of medicinal chemistry, Apr-09, Volume: 764,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
AID663352Growth inhibition of human NCI-H226 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID420646Antitumor activity against human HCT116 cells athymic nude Swiss mouse assessed as tumor volume inhibition at 100 mg/kg, po QD administered 5 days a week for 4 weeks2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1740129Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1875509Cytotoxicity against HMEC cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay2022ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
AID274169Antiproliferative activity against H661 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID609495Ratio of IC50 for CYP3A4 to IC50 for human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1514613Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining based assay (Rvb = 1.8 %)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1771460Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1886174Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1898909Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1742652Cytotoxicity against human BT-549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1821963Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
AID1742651Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1403180Inhibition of ERK1/2 phosphorylation in human HepG2 cells at 2 uM after 48 hrs by Western blot analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1650409Inhibition of recombinant human HDAC82020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.
AID717658Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1127319Antiproliferative activity against human H460 cells assessed as growth inhibition after 72 hrs2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1227030Inhibition of human recombinant HDAC2 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.
AID737917Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.
AID1281868Induction of apoptosis in human RPMI8226 cells assessed as viable cells at 3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 87.2%)2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1890333Stability in mouse liver microsomes assessed as clearance and measured by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.
AID1623524Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate-3 by fluorescence assay2019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID618084Toxicity in athymic nu/nu Harlan mouse xenografted with human HCT116 cells assessed as body weight loss at 300 mg/kg, po QD for 21 days measured on day 192011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1281850Inhibition of full length His6-tagged GST-fused recombinant human HDAC6 expressed in High5 insect cells using Boc-Lys (e-acetyl)-AMC as substrate after 3 hrs by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1901057Inhibition of HDAC6 (unknown origin) using trypsin and Ac-peptide as substrates2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID408881Inhibition of HDAC22008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1441655Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in pathological changes at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by hematoxylin and eosin staining based micro2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1398811Antagonist activity at ERalpha in human MCF7 cells assessed as down regulation of ESR1 expression at 0.1 to 9 uM after 8 hrs by Western blot analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1566824Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.
AID316872Inhibition of HDAC from human K562 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID476830Toxicity in FVB mouse assessed as effect on mean cell volume of red cells at 50 mg/kg, po administered 5 times per week for 2 weeks (Rvb = 43.7 +/- 0.4 microm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID6191411-Octanol-sodium phosphate buffer distribution coefficient, log D of the compound at pH 7.42011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID1406983Inhibition of class 1 HDAC in human NB4 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
AID316901Inhibition of human MDA-MB-231 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID366642Inhibition of HDAC3 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1476154Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1485127Cell cycle arrest in human Hs683 cells assessed as accumulation at G1 phase at 2 uM after 24 to 48 hrs by propidium iodide staining-based flow cytometry2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
AID1901152Inhibition of HDAC1 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1281869Induction of apoptosis in human RPMI8226 cells assessed as early apoptotic cells at 3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 6.3%)2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID747261Growth inhibition of human A549 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
AID1497924Induction of CRBN ubiquitin ligase-mediated HDAC1 degradation in human MCF7 cells assessed as decrease in HDAC1 levels at 10 uM after 12 hrs by immunoblotting analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Development of the first small molecule histone deacetylase 6 (HDAC6) degraders.
AID1170743Inhibition of human recombinant HDAC8 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.
AID1312899Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as body weight loss at 50 mg/kg, ip administered every 2 days for 11 days measured on day 17 post last dose2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID1421922Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting 2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID327549Cytotoxicity against human HCT116 cells assessed as cell viability after 96 hrs by MTS reduction assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID1433301Induction of DNA damage in p53 null human U937 cells assessed as decrease in CHK1 expression level by measuring ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1401481Selectivity ratio of IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell to IC50 for HDAC1 in human HeLa-S3 cell lysates2018European journal of medicinal chemistry, Jan-01, Volume: 143The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
AID1303685Inhibition of HDAC1 in human Jurkat cells extract after 30 mins by immunoprecipitation assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1690105Inhibition of HSP90a (unknown origin)2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID480067Inhibition of human recombinant HDAC2 preincubated for 1 hr with substrate by protease coupled end-point assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
AID663378Growth inhibition of human LOXIMVI cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1225977Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1398803Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID274066AUC after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID304372Inhibition of human IMPDH 22007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
AID1819554Antitumor activity against mouse B16-F10 cells xenografted in C57BL/6J mouse assessed as reduction in tumor heterogeneity at 60 mg/kg, IG administered for 12 days by H and E staining based histopathological analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1462022Inhibition of HDAC in human HeLa nuclear extract preincubated for 5 mins followed by Boc-Lys (acetyl)-AMC addition measured after 10 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability.
AID350722Ratio of GI50 for human MKN45 cells to IC50 for HDAC in human HeLa cells2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID725666Selectivity ratio of IC50 for C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 to IC50 for C-terminal His-tagged human recombinant HDAC9 (amino acids 604- 1066) by fluorescence analysis2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
AID672027Inhibition of human recombinant HDAC3 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs at 10 uM measured after 35 mins by spectrofluorometric analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1373246Inhibition of HDAC6 (unknown origin) preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
AID1597939Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1727733Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1856996Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1812469Antiplasmodial activity against Plasmodium falciparum NF54 late stage IV-V gametocytes assessed as reduction in number of exflagellation centers in at 1 uM treated for 72 hrs2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1401542Antiproliferative activity against human U2932 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1441654Inhibition of LTB4 biosynthesis in LPS-induced C57BL/6 mouse model of acute lung injury BLAF administered intraperitoneally by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1164040Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1126961Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID421214Inhibition of HDAC6 from human HeLa cells at 5 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID586610Antimalarial activity against Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID297470Inhibition of HDAC in HeLa cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID524993Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in forskolin-stimulated Fdelta508 CFTR channel activity at 10 uM after 24 hrs relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1439772Inhibition of Pseudomonas aeruginosa PA1409 using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by trypsin-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa.
AID1308511Inhibition of HDAC (unknown origin)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
AID352519Inhibition of human recombinant HDAC22009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1677516Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1469495Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as tumor growth inhibition at 130 mg/kg, po administered daily via gavage for 18 days by bioluminescence assay relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer
AID1898921Induction of DNA damage in human NCI-H460 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1055349Cytotoxicity against human HDF after 72 hrs by MTS-PMS assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
AID663355Growth inhibition of human NCI-H460 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1235113Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.
AID1399559Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID476831Toxicity in FVB mouse assessed as effect on number of WBC at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test (Rvb = 9.1 +/- 0.2 10^3/mm^3)2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity.
AID1688043Induction of HDAC6 degradation in human HL-60 cells assessed as decrease in HDAC6 level at 2 uM incubated for 12 hrs by Western blot analysis2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1060993Inhibition of HDAC in human HeLa cell nuclear extract using fluor de Lys as substrate at 1 uM after 15 mins by fluorimetric analysis2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors.
AID1390011Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1622912Inhibition of HDAC1/HDAC2 in human HeLa nuclear extract2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1769656Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.
AID352525Antiproliferative activity against human SU-8686 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
AID1639362Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
AID1398813Antagonist activity at ESR1 in human MCF7 cells assessed as suppression of ESR1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
AID1162227Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential in P4 quadrant at 1 uM by Rhodamine123 assay (Rvb = 96.6%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID1464874Anti-proliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.
AID1164782Inhibition of HDAC3 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
AID1336929Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1869150Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM incubated for 48 hrs by CCK8 assay
AID1869151Cytotoxicity against human L02 cells assessed as cell viability at 10 uM incubated for 48 hrs by CCK8 assay
AID1667079Inhibition of STAT3 in human MDA-MB-231 cells assessed as upregulation of p-p38 expression after 24 hrs by western blot analysis2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID1061951Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.
AID1281853Antiproliferative activity against human NCI-H929 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
AID1336922Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID544095Cytotoxicity against african green monkey Vero cells by MTT assay2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1709346Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1421906Selectivity index, ratio of IC50 for human NFF cells to IC50 for drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID613292Plasma concentration in dog at 150 mg/kg, po administered as single dose2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1177049Cytotoxicity against human NCI-H460 cells2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID673993Inhibition of recombinant HDAC6 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1462216Inhibition of recombinant human HDAC1 at 1 uM after 30 mins by fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1390021Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
AID1454034Growth inhibition of human HL60 cells after 3 days by counting method2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
AID1821337Toxicity in mouse xenografted with human HepG2 cells assessed as cellular inflammation in spleen at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1548272Induction of cell cycle arrest in human RPMI8226 cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27.6%)
AID482951Antiproliferative activity against human HCT116 cells2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1882462Inhibition of HDAC6 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1476152Antiproliferative activity against human Jurkat cells2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1515884Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 500 nM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 5.23%)2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1394886Antiproliferative activity against human NCI-H1975 cells after 48 hrs by sulforhodamine B assay2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1876342Inhibition of recombinant full length human HDAC6 expressed in insect Sf9 cells by EMSA analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID1321723Cytotoxicity against human THLE2 cells assessed as reduction in cell viability after 72 hrs by ATP Vialight assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1697199Cytotoxicity against human NCI-H23 cells by colorimetric method2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.
AID1742743Genotoxicity in Salmonella typhimurium TA1535 by Ames test2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID1393286Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
AID1549137Antifungal activity against azole-resistant Candida albicans 0304103 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID328806Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID371221Inhibition of histone deacetylase in human HeLa cells assessed as induction of histone H3 hyperacetylation2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Alpha-mercaptoketone based histone deacetylase inhibitors.
AID1063036Inhibition of recombinant HDAC10 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.
AID1865248Metabolic stability in mouse liver microsome measured at 2 hrs in presence of NADPH2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID659636Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1732190Cytotoxicity against human HH cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1702050Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1873382Inhibition of HDAC2 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1476155Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID70687Percent of murine erythroleukemia cells that became benzidine reactive after administration (2.5 uM)1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
AID1390012Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID591328Inhibition of HDAC in human HeLa cells at 10 uM by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.
AID1550100Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1181303Inhibition of human recombinant HDAC1 using histone H3 substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1702197Toxicity in Ncr nude mouse xenografted with human HepG2 cells assessed as change in body weight at 60 mg/kg, po QD with 5 days on and 2 days off dosing schedule for 2 weeks cotreated with 75 mg/kg pictilisib and measured at day 12 (Rvb = -0.8%)2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID274014Percent inhibition of CYP450 1A2 at 1 uM concentration2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1605965Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1065962Cytotoxicity against androgen-independent human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.
AID723467Inhibition of HDAC in cisplatin resistant human KYSE-510 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1337287Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1174694Inhibition of HDAC3 (unknown origin)2015European journal of medicinal chemistry, Jan-07, Volume: 89Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.
AID446346Volume of distribution at steady state in CD1 mouse at 15 mg/kg, po2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
AID708276Growth inhibition of human Bel7404 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1203891Inhibition of recombinant HDAC8 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1890516Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1361630Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1864224Inhibition of full length recombinant C-terminal GST-tagged human HDAC1 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID374812Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1614126Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
AID374820Inhibition of C-terminal FLAG-tagged HDAC6 expressed in mammalian cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID300833Growth inhibition of human PC3 cells after 21 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
AID374826Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1493602Inhibition of HDAC1/2/3 in human A549 cells assessed as increase in acetylated acetylated histone H4 levels at 500 nM after 3 hrs by Western blot analysis2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of a fluorescent probe with HDAC6 selective inhibition.
AID1811371Inhibition of HDAC6 (unknown origin) at 0.1 uM using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID449262Antiproliferative activity against human A549 cells after 2 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors.
AID708271Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID605621Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 300 nM after 15 hrs by propidium iodide staining based flow cytometric analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID1727740Inhibition of HDAC3 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID732875Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Development of
AID1764280Inhibition of HDAC in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin IC50 at 0.7 uM pretreated for 48 hrs followed by cisplatin addition and measured after 72 hrs by MTT assay relative to cisplatin 2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1845460Inhibition of HDAC6 (unknown origin)2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?
AID1855257Antiproliferative activity against mouse MC38 cells after 48 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.
AID1337286Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1431816Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1765325Inhibition of human full-length recombinant HDAC2 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID749704Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1361628Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1785341Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay
AID373080Inhibition of human recombinant HDAC72009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
AID304374Antiproliferative activity against human K562 cells after 72 hrs by MTS assay2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
AID1537568Cell cycle arrest in human G55T2 cells assessed as accumulation in G2/M phase at 3 uM incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 26.8 %)2019MedChemComm, Jul-01, Volume: 10, Issue:7
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
AID1466055Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1605975Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1653141Cytotoxicity against human SW620 cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Mar-01, Volume: 165Quinolone hybrids and their anti-cancer activities: An overview.
AID1821350Toxicity in mouse xenografted with human HepG2 cells assessed as necrosis in kidney at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID274030Permeability (Papp) run from pH 6.5-7.42007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID327546Increase in acetylated histone H4 level in human HCT116 cells at 10 uM after 24 hrs relative to control2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
AID1337306Inhibition of HDAC1/HDAC2/HDAC3 signalling in HEL 92.1.7 cells harboring JAK2 V617F mutant assessed as increase in acetylated histone-3(Lys9/Lys14) level at 0.1 to 1 uM after 1 hr by immunoblot method2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID762188Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.
AID1433252Antiproliferative activity against human CMK cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1578502Induction of apoptosis in human MV4-11 cells assessed as viable cells at 2 uM incubated for 18 hrs by annexin V FITC and PI based flow cytometry (Rvb = 53.01 to 53.07 %)2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID258012Inhibition of human leukemic CEM cell viability2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
AID1525777Inhibition of HADC1 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1849158Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
AID1655892Inhibition of EZH2 in human U937 cells assessed as H3K27me3 level at 0.5 uM incubated for 96 hrs by Western blot analysis (Rvb = 1 No_unit)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
AID304375Differentiation of K562 cells at 0.50 uM after 5 days by MTS assay2007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
AID609726Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors.
AID1915597Inhibition of HDAC11 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1234902Antiproliferative activity against human ES2 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1436788Growth inhibition of human NCI-H292 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity.
AID761584Inhibition of HDAC in human HeLa cell extract using fluor de Lys as substrate after 15 mins by fluorometric analysis2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID1897488Antitumor activity against human SNU-16 cells xenografted in BALB/c nude mouse assessed as reduction in tumor growth at 50 mg/kg/day, ip administered for 18 days and measured every 3 days
AID1542189Inhibition of HDAC11 (unknown origin)2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.
AID440466Metabolic stability in Sprague-Dawley rat plasma at 10 uM by LC-MS/MS analysis2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Hydroxamates: relationships between structure and plasma stability.
AID1404339Inhibition of HDAC in human cell lysates using fluoro-substrate peptide/fluoro-deacetylated peptide as substrate incubated for 20 mins measured at 1 to 2 mins interval for 30 to 60 mins by fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1897370Inhibition of FGFR2 (unknown origin)
AID243592Percent inhibition against human histone deacetylase at 100 uM2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID420642Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 24 hrs by Western blot2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1441641Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in lung lesions at 10 to 50 mg/kg, ip pretreated for 1 hr followed LPS challenge measured after 24 hrs by hematoxylin and eosin staining based microsc2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID462791Antiproliferative activity against human SKOV3 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
AID1240555Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 4 uM after 24 hrs using Annexin V-FITC and propidium iodide staining by flow cytometry (Rvb = 2.60%)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.
AID1518779Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC62019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1587860Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
AID1816190Inhibition of recombinant HDAC7 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis
AID1164194Inhibition of HDAC in human MCF7 cells assessed as hyperacetylation of p21 at 5 uM after 24 hrs by Western blot analysis relative to control2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
AID1659649Inhibition of HDAC3 (unknown origin)2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Environment-sensitive fluorescent inhibitors of histone deacetylase.
AID670515Antiproliferative activity against human A431 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.
AID1541558Inhibition of HDAC6 in human Cal27CisR cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID214058Compound was tested for anti-proliferative activity in U-937 human leukemia cell line2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
AID1441665Anti-inflammatory activity in LPS-induced C57BL/6 mouse model of acute lung injury assessed as reduction in IL-1beta level pretreated at 25 mg/kg, ip pretreated for 1 hr followed LPS challenge after 24 hrs by ELISA2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1688031Induction of apoptosis in human HL-60 cells assessed as early apoptotic cells at 0.5 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 2.46 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID462790Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
AID1515887Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 500 nM after 24 hrs by propidium iodide/RNase staining-based FACS analysis2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID90689Tested for maize Histone deacetylase 2 inhibitory activity2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1273867Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
AID1876343Inhibition of recombinant full length human HDAC8 expressed in insect Sf9 cells by EMSA analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia.
AID1352481Inhibition of HDAC2 in human HeLa cells after 72 hrs by ELISA2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID1321698Selectivity ratio of pLC50 for mouse primary glial cells to pLC50 for human THLE2 cells2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1742666Cytotoxicity against human PANC-1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.
AID465158Growth inhibition of human Panc 04.03 cells after 72 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1260638Inhibition of human recombinant HDAC2 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1689775Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID288449Growth inhibition of HCT15 cells by SRB assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
AID619050Competitive inhibition of HDAC5 using KI-104 as substrate by fluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
AID545857Antimalarial activity against Plasmodium falciparum FCR3 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.
AID1689771Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth at 8 uM measured after 72 hrs by CCK-8 assay relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID717821Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 3.125 x 10'-8 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1739567Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 4 uM by CellTiter-non radioactive cell proliferation assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
AID1478587Induction of apoptosis in human K562 cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2.83%)2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.
AID1321619Inhibition of HDAC1/HDAC2 in human HeLa cell nuclear extract preincubated for 20 mins followed by addition of HDAC green as substrate measured after 60 mins by fluorescence analysis2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.
AID1467032Stabilization of human luc fused SMN protein expressed in HEK293 cells at 10 uM after 24 hrs in presence of 10 uM cycloheximide by luciferase reporter gene assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy.
AID1826633Synergistic antiproliferative effect on HEL cells assessed as combination index at 0.04 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1234903Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.
AID1404298Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay2018ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.
AID1597956Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 uM incubated for 72 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometric analysis (Rvb = 2.76%)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1737133Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
AID672035Ratio of inhibition of human HDAC3 at 10 uM preincubated for 3 hrs to inhibition of human HDAC3 at 10 uM preincubated for 5 mins2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.
AID1890511Inhibition of HDAC2 (unknown origin)2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID1859936Antiproliferation activity against human HCT-116 cells assessed as reduction in cell viability at 5 to 50 uM measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability.
AID659637Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 protein expression at 2.5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID761579Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID1548264Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay
AID274023Oral bioavailability after oral dosing at 5 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1689811Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth at 2 uM measured after 72 hrs by CCK-8 assay relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.
AID659492Inhibition of HDAC1/2 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
AID1784189Inhibition of recombinant human HDAC1 using ZMAL as substrate incubated for 90 mins by fluorescence based micro plate assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.
AID1206753Cell cycle arrest in human HEL cells assessed as accumulation at S phase at 0.5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 46.88%)2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID473192Growth inhibition of human MUF cells after 48 hrs by MTT assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
AID1266831Induction of apoptosis in human HCT116 cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.
AID1436789Growth inhibition of human NCI-H292 cells after 72 hrs in presence of LDL by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity.
AID1545989Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1269321Cytotoxicity against human A2780S/CP5 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
AID725668Inhibition of C-terminal His-tagged full length human recombinant HDAC3 co-expressed with NcoR2 in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured af2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
AID1702056Inhibition of human full-length recombinant p110alpha/p85alpha co-expressed in baculovirus expression system using PIP2:PS lipid as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1777024Inhibition of HDAC in human A549 cells assessed as reduction in fluorescent APS probe fluorescence intensity at 10 uM preincubated with compound for 2 hrs followed by co-incubation with APS probe by intracellular fluorescence competition assay2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase.
AID1550107Inhibition of HDAC6 in human A549 cells assessed as increase in acetyl alpha tubulin level at 80 to 400 nM after 6 hrs by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1896951Cytotoxicity against human HUVEC cells assessed as reduction in cell viability by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID1239053Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by CCK8 assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
AID1282244Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1578888Inhibition of human HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.
AID297480Cytotoxicity against human MDA-MB-468 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1403181Inhibition of HDAC1 in human HepG2 cells assessed as upregulation of acetyl-histone H3 levels at 5 uM after 48 hrs by Western blot analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID1622913Inhibition of HDAC3 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1293567Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate incubated for 90 mins by fluorescence assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.
AID717825Inhibition of HDAC6 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1250645Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID613343Inhibition of human ERG at 30 uM2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID316875Inhibition of HDAC from human HeLa cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1487012Selectivity index, ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC8 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.
AID1282294Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as death at 100 mg/kg, po q2d for 8 days2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
AID1403172Antimetastatic activity in human HepG2 cells assessed as reduction in cell invasion at 1 uM after 48 hrs by crystal violet staining-based transwell invasion assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID761583Inhibition of full length His-tagged human recombinant HDAC1 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis2013European journal of medicinal chemistry, Aug, Volume: 66Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.
AID1421917Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID663472Inhibition of human CYP3A42012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID310187Antitumor activity against MDA-MB-231 cells xenografted BALB/c nude mouse assessed as body weight at 30 mg/kg, ip for 15 days2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
AID1819539Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as increase in proportion of T cells in spleen by flow cytometry analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
AID1431812Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1476159Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1547269Inhibition of HDAC3 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1753841Selectivity index, ratio of IC50 for inhibition of HDAC2 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Jun-05, Volume: 218Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.
AID1765330Selectivity index, ratio of IC50 for human recombinant full length HDAC3 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1702156Inhibition of human ERG by fluorescence polarization assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1897508Antiangiogenic activity against BALB/c mouse xenografted with human SNU-16 cells assessed as downregulation of CD31 expression in tumor at 50 mg/kg/day, ip administered for 18 days by immunohistochemical staining based analysis
AID1529550Cytotoxicity against human PBL cells assessed as cell growth inhibition after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1164041Antiproliferative activity against human U937 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID675296Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 0.01 uM by fluorescence assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
AID1349722Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID1709360Induction of apoptosis in human Jurkat cells assessed as late apoptotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 6.77%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1863433Inhibition of HDAC1 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1699969Antiproliferative activity against human K562 cells by MTT assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1623535Selectivity index, ratio of IC50 for human recombinant HDAC3 to IC50 for human recombinant HDAC62019European journal of medicinal chemistry, Feb-15, Volume: 164A novel class of anthraquinone-based HDAC6 inhibitors.
AID723479Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID609489Inhibition of purified recombinant HDAC12011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1864677Inhibition of full length recombinant human HDAC6 in MV4-11 cells assessed as upregulation of acetylated histone H4 at 1 uM measured upto 24 hrs by western blot analysis
AID1449339Inhibition of HDAC1/HDAC6 in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 1 uM preincubated for 48 hrs followed by cisplatin treatment measured after 72 hrs by MTT assay 2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1677498Induction of mitochondrial membrane potential loss in human HeLa cells at 1 to 3 uM after 24 hrs by TMRE staining based fluorescence assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
AID1709367Induction of apoptosis in human NAMALVA cells assessed as late apoptotic cells at IC50 measured after 48 hrs by Annexin V-FITC/7AAD staining based flow cytometry (Rvb = 3.52%)2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1821958Inhibition of recombinant human HDAC1 expressed in baculovirus expression system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay
AID1826624Synergistic antiproliferative effect on HEL cells assessed as fractional inhibitory concentration index at 0.12 uM in presence of 3-Fluoro-10-hydroxy-14-methyl-8,13,13b,14-tetrahydro-7H-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5-one2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID274026Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-12007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID274097Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 50% of isolates after 24h.2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
AID274078Inhibition of MDA-MB-231 cell proliferation (mean of two experiments)2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1890509Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
AID744875Inhibition of mouse liver HDAC by fluorescence assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Discovery of adamantane based highly potent HDAC inhibitors.
AID1502983Inhibition of MAOA (unknown origin) using beetle luciferin as substrate by MAO-Glo assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
AID1547343Inhibition of HDAC in human HCT116 cells assessed as activation of IL6-JAK-STAT signaling pathway by measuring increase in OSMR expression at 10 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1753637Selectivity index, ratio of IC50 for inhibition of human HDAC1 to IC50 for inhibition of human HDAC62021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
AID1549165Inhibition of HDAC6 (unknown origin) after 30 mins by fluorescence based assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1164910Inhibition of HDAC5 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID1511970Inhibition of full length recombinant FLAG-tagged C-terminal human HDAC2 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
AID1810051Inhibition of HDAC1 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader
AID663377Growth inhibition of human U251 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1880243Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 3 days by trypan blue assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
The
AID1535339Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.
AID1758465Phototoxicity in human HCT-116 cells assessed as reduction in cell viability irradiated 10 j/cm2 for 24 hrs followed by incubated for 24 hrs by CCK8 assay2021European journal of medicinal chemistry, May-05, Volume: 217Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.
AID1280309Inhibition of human KDAC82016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1785345Inhibition of full length human CDK4 (1 to 303 residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay
AID1206763Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.
AID1622976Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 24 hrs and measured after 60 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1816208Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 2.5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.38%)
AID1476118Cytotoxicity against TAMH cells assessed as cell viability after 24 hrs by CellTiter-Glo assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
AID1614257Toxicity against NOD/SCID mouse xenografted with human MM1S cells assessed as mouse survival at 50 mg/kg, po qd administered for 10 days co-treated with 25 mg/kg RAPA
AID1245683Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors.
AID1225990Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 5.25%)2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
AID1652191Inhibition of human recombinant HDAC4 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1164037Antiproliferative activity against human BGC823 cells assessed as growth inhibition after 72 hrs by CCK-8 assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
AID1676598Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1503840Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluoresce2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
AID1821262Toxicity in mouse xenografted with human HepG2 cells assessed as cellular inflammation in liver at 12 mg/kg, ip administered every 2 days for 4 weeks by H and E staining based microscopic method2022European journal of medicinal chemistry, Feb-05, Volume: 229Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
AID1784977Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID1126979Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1873386Inhibition of HDAC6 (unknown origin)2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1808545Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
AID1667072Cytotoxicity against African Green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTS assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.
AID274017Percent inhibition of CYP450 2C19 at 1 uM concentration2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID297490Cytotoxicity against human AsPC1 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1752941Cytotoxicity against human HepG2-A16-CD81EGFP cells assessed as inhibition of cell growth incubated for 24 hrs followed by medium transfer and incubation in multimode plate for 48 hrs by CellTiterGlo reagent based luminescence assay
AID1816699Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1784975Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
AID593555Inhibition of human HDAC10 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.
AID759304Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID1647336Upregulation of acetylated H3K14 protein expression in hippocampus of bilateral common carotid artery occlusion-induced vascular dementia C57BL/6J mouse model at 25 mg/kg, ip measured after 3 months by Western blot analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1515904Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
AID1549136Antifungal activity against azole-sensitive Candida albicans SC5314 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1266094Inhibition of HDAC3 (unknown origin) by fluorimetric assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1598094Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
AID1250648Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1730867cytotoxicity against human HL-7702 cells assessed as reduction of cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR
AID1421907Selectivity index, ratio of IC50 for human NFF cells to IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1514604Inhibition of HDAC1 in human HepG2 cells assessed as acetylated histone H4 levels at 5 uM by Western blot analysis relative to beta-actin (Rvb = 1 No_unit)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1173503Inhibition of C-terminal 6x-His tagged human HDAC5 (657 to 1123 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
AID1386705Inhibition of HDAC in human GM18453 cells assessed as increase in 250 kDa NPC1 protein expression at 5 uM pretreated for 48 hrs followed by endoglycosidase H addition and measured after overnight incubation by Western blot analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
GEX1A, a Polyketide from Streptomyces chromofuscus, Corrects the Cellular Defects Associated with Niemann-Pick Type C1 in Human Fibroblasts.
AID1394885Antiproliferative activity against human HL60 cells after 48 hrs by sulforhodamine B assay2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1811363Inhibition of HDAC1 (unknown origin)2021European journal of medicinal chemistry, Dec-15, Volume: 226Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
AID663346Growth inhibition of human K562 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID780588Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.
AID1312891Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as mortality at 50 mg/kg, ip administered every 2 days for 8 days2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
AID246067Effective Concentration of compound to inhibit the growth of human DU-145 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
AID1754808Upregulation of SIRT2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1762488Inhibition of HDAC in human HeLa nuclear extracts using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based assay2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
AID604138Inhibition of histone acetyltransferase in human U937 cells assessed as increase of acetylation of histone H3 at K18 at 5 uM after 24 hrs by Western blotting2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
AID609724Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors.
AID1421920Antiplasmodial activity against exo-erythrocytic stage of GFP-Luc-fused Plasmodium berghei ANKA infected in human HepG2 cells after 48 hrs by bioluminescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID1326510Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID605532Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
AID344918Inhibition of 2-oxoglutarate-dependent human JMJD2E preincubated for 30 mins by FDH coupled assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID1403182Inhibition of HDAC6 in human HepG2 cells assessed as upregulation of acetyl-alpha-tubulin levels at 5 uM after 48 hrs by Western blot analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
AID241537Inhibitory concentration against maize histone deacetylase 1-A (class IIa HDAC)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID481546Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1126995Induction of apoptosis in human U937 cells assessed as necrotic cells using annexin-V/propidium iodide staining at 1 uM after 24 hrs by flow cytometry analysis (Rvb = 0.06%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.
AID1280276Inhibition of HDAC6 in human HL60 cells assessed as ratio of acetylated tubulin to GAPDH level at 1 uM after 4 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.
AID1486669Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID297483Cytotoxicity against human SK-OV-3 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
AID1563942Inhibition of recombinant HDAC3 (unknown origin) measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
AID348793Antiproliferative activity against human HeLa cells after 72 hrs by celltiter-blue viability assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
AID328795Inhibition of HDAC32008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID465154Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1408193Inhibition of MOF in human HCT116 cells assessed as decrease in H4K16 acetylation level after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, Sep-05, Volume: 157Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening.
AID1897400Induction of apoptosis in human SNU-16 cells assessed as live cells at 0.3 uM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 90.92%)
AID586607Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1162220Cell cycle arrest in human HL60 cells assessed as accumulation at G2/M phase at 1 uM by propidium iodide staining-based flow cytometry (Rvb = 21.3%)2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
AID1897371Inhibition of FGFR3 (unknown origin)
AID1754751Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release using fluorogenic HDAC substrate 3 measured every 5 mins by fluoresc2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1882089Inhibition of HDAC1 (unknown origin) using fluorimetric substrate incubated for 30 mins by fluorogenic assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Medicinal chemistry updates of novel HDACs inhibitors (2020 to present).
AID1337255Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
AID1514598Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
AID1816187Inhibition of HDAC3 (unknown origin) incubated for 60 mins using microplate reader analysis
AID1326522Inhibition of His-tagged full length recombinant human HDAC8 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay2016European journal of medicinal chemistry, Oct-21, Volume: 1222-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
AID1129791Induction of apoptosis in human Jurkat cells assessed as cell death at 10 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based FACS flow cytometric analysis (Rvb = 0.348%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID1275593Inhibition of HDAC in mouse forebrain primary neurons assessed as acetylation of histone H3K9 after 24 hrs by immunofluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
AID1547247Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Discovery of Thieno[2,3-
AID1599789Inhibition of HDAC6 in human A549 cells assessed as upregulation of semaphorin 3F mRNA expression at 2.5 uM after 24 hrs by RT-Sybr green PCR analysis2019ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.
AID1702082Antiproliferative activity against human SNU-387 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID438219Inhibition of HDAC62009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
AID1865271Inhibition of HDAC in human MV4-11 cells assessed as upregulation of acetylated H3 level incubated for 24 hrs by Western blot analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID316891Inhibition of HDAC2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1129788Induction of apoptosis in human Jurkat cells assessed as viable cells at 10 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based FACS flow cytometric analysis (Rvb = 99.3%)2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
AID639364Clearance in mouse2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
AID1550157Toxicity in BALB/c nu mouse xenografted with HEL cells assessed as change in body weight at 60 mg/kg/day, ip administered for 16 days and measured every day during compound dosing in presence of ruxolitinib2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
AID1688037Induction of apoptosis in human HL-60 cells assessed as necrotic cells at 1 uM measured after 24 hrs by Annexin-V/FITC and propidium iodide staining based flow cytometry (Rvb = 1.01 %)2020European journal of medicinal chemistry, Feb-15, Volume: 188A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
AID1816199Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
AID546560Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1449227Inhibition of HDAC1/2/3/6 in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 1 uM preincubated for 48 hrs followed by cisplatin addition measured after 72 hrs by MTT assay r2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
AID1482168Cytotoxicity against human MOLT4 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.
AID1215097Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis relative to dexamethasone2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1303630Potentiation of 0.5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 2.5 uM after 48 hrs by cell titer-glo luminescence assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821.
AID1260649Inhibition of HDAC in human MV411 cells assessed as increase in H3K9 aceylation at 0.1 to 5 uM after 4 hrs by western blot analysis
AID710840Cytotoxicity against human PC3 cells assessed as growth inhibition by SRB assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles.
AID663351Growth inhibition of human HOP92 cells after 72 hrs by MTS assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
AID1900918Induction of apoptosis in mouse GL26 cells assessed as proteolytic cleavage of PARP1 incubated for 48 hrs by Western blot analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
AID541649Inhibition of human HDAC5 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1349718Inhibition of NAMPT (unknown origin) using NAM as substrate incubated for 5 mins followed by substrate addition measured after 15 mins by fluorometric method2018ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
AID481551Cytotoxicity against human HO8910 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
AID1864251Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1164911Inhibition of HDAC6 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.
AID313733Inhibition of HDAC52008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1754760Downregulation of HDAC1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
AID1798524HDAC Activity Assay from Article 10.1021/jm800079s: \\A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.\\2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1797826HDAC Enzyme Activity Assay from Article 10.1021/jm0703800: \\The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.\\2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID1802589HDAC2 Enzyme Assay from Article 10.1016/j.bioorg.2017.02.002: \\Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.\\2017Bioorganic chemistry, 04, Volume: 71Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.
AID1798419HDAC Inhibition Assay from Article 10.1021/jm701606b: \\A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.\\2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1800141In vitro HDACs Inhibition Fluorescence Assay from Article 10.1111/cbdd.12144: \\Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.\\2013Chemical biology & drug design, Aug, Volume: 82, Issue:2
Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.
AID1802011HDAC6 fluorescence anisotropy assay from Article 10.1038/nchembio.2134: \\Histone deacetylase 6 structure and molecular basis of catalysis and inhibition\\2016Nature chemical biology, 09, Volume: 12, Issue:9
Histone deacetylase 6 structure and molecular basis of catalysis and inhibition.
AID1802356Inhibitor Competition Assay from Article 10.1021/acschembio.6b00776: \\LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.\\2017ACS chemical biology, 01-20, Volume: 12, Issue:1
LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.
AID1801572In-vitro HDAC Enzymatic Endpoint Assay from Article 10.1021/acschembio.5b00640: \\An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in u00DF-Cell Protection.\\2016ACS chemical biology, Feb-19, Volume: 11, Issue:2
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.
AID1802920HDAC Activity Assay from Article 10.3109/14756360903049034: \\Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.\\2010Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 25, Issue:1
Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.
AID1799021pfHDAC-1 Enzyme Assay from Article 10.1021/jm801654y: \\Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.\\2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID1798635FDH Coupled Inhibition Assay from Article 10.1021/jm800936s: \\Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases.\\2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID1802398Enzymatic HDAC Activity Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1800408HDAC8 Inhibition Assay (spectrofluorometric titration) from Article 10.1021/bi400740x: \\Kinetic and thermodynamic rationale for suberoylanilide hydroxamic acid being a preferential human histone deacetylase 8 inhibitor as compared to the structurally simi2013Biochemistry, Nov-12, Volume: 52, Issue:45
Kinetic and thermodynamic rationale for suberoylanilide hydroxamic acid being a preferential human histone deacetylase 8 inhibitor as compared to the structurally similar ligand, trichostatin a.
AID1802059In vitro HDAC8 Assay from Article 10.1111/cbdd.12778: \\Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.\\2016Chemical biology & drug design, 10, Volume: 88, Issue:4
Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.
AID1794865Enzyme inhibition assay from Article 10.3109/14756366.2013.827678: \\Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.\\2014Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 29, Issue:4
Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.
AID1798526HDAC Activity Assay from Article 10.1016/j.bmcl.2008.02.025: \\Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.\\2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1802239In vitro HDACs Inhibition Fluorescence Assay from Article 10.1111/cbdd.12819: \\Design, synthesis, and preliminary bioactivity evaluation of N(1) -hydroxyterephthalamide derivatives with indole cap as novel histone deacetylase inhibitors.\\2017Chemical biology & drug design, Jan, Volume: 89, Issue:1
Design, synthesis, and preliminary bioactivity evaluation of N
AID1802399Proteros Reporter Displacement Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1794854HDAC Activity screening from Article 10.3109/14756366.2013.827675: \\Quinolone-based HDAC inhibitors.\\2014Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 29, Issue:4
Quinolone-based HDAC inhibitors.
AID1798196Enzyme Inhibition Assay from Article 10.1021/jm7015254: \\Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.\\2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
AID1800409HDAC8 Inhibition Assay (kinetic method) from Article 10.1021/bi400740x: \\Kinetic and thermodynamic rationale for suberoylanilide hydroxamic acid being a preferential human histone deacetylase 8 inhibitor as compared to the structurally similar ligand, tri2013Biochemistry, Nov-12, Volume: 52, Issue:45
Kinetic and thermodynamic rationale for suberoylanilide hydroxamic acid being a preferential human histone deacetylase 8 inhibitor as compared to the structurally similar ligand, trichostatin a.
AID1798784HDAC Activity Assay from Article 10.1021/jm801128g: \\Non-peptide macrocyclic histone deacetylase inhibitors.\\2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Non-peptide macrocyclic histone deacetylase inhibitors.
AID1801045HDAC Enzyme Activity Assay from Article 10.1016/j.bioorg.2015.02.009: \\An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.\\2015Bioorganic chemistry, Apr, Volume: 59An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.
AID1802060APN Inhibition Assay from Article 10.1111/cbdd.12778: \\Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.\\2016Chemical biology & drug design, 10, Volume: 88, Issue:4
Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1346082Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346066Human histone deacetylase 5 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346068Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs))2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1346080Human histone deacetylase 11 (3.5.1.- Histone deacetylases (HDACs))2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1346032Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346090Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs))2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1346068Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346077Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346048Human histone deacetylase 10 (3.5.1.- Histone deacetylases (HDACs))2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
AID1346134Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347415qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,495)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (0.24)18.2507
2000's480 (19.24)29.6817
2010's1591 (63.77)24.3611
2020's418 (16.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.95

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.95 (24.57)
Research Supply Index7.91 (2.92)
Research Growth Index6.82 (4.65)
Search Engine Demand Index88.45 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials181 (7.16%)5.53%
Reviews139 (5.50%)6.00%
Case Studies38 (1.50%)4.05%
Observational1 (0.04%)0.25%
Other2,170 (85.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (272)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I Trial Of Vorinostat In The Treatment Of Advanced Laryngeal, Hypopharyngeal, Nasopharyngeal And Oropharyngeal Squamous Cell Carcinoma Of The Head And Neck. [NCT01064921]Phase 127 participants (Actual)Interventional2010-01-19Completed
Phase I Study of the Combination of Vorinostat and Radiation Therapy for the Treatment of Patients With Brain Metastases [NCT00838929]Phase 117 participants (Actual)Interventional2009-03-31Completed
A Feasibility Study of Vorinostat (SAHA) Combined With Isotretinoin and Chemotherapy in Infants With Embryonal Tumors of the Central Nervous System [NCT00867178]Phase 133 participants (Actual)Interventional2009-02-25Completed
Phase I Study of Vorinostat in Combination With 13-Cis-retinoic Acid in Patients With Refractory/Recurrent Neuroblastoma [NCT01208454]Phase 129 participants (Actual)Interventional2010-12-31Completed
Phase I Study on Suberoylanilide Hydroxyamic Acid (Vorinostat) a Histone Deacetylase Inhibitor, in Palliative Radiotherapy for Advanced Tumors. [NCT00455351]Phase 115 participants (Actual)Interventional2007-02-28Completed
A Phase I Study of Vorinostat and Bortezomib in Children With Refractory of Recurrent Solid Tumors, Including CNS Tumors and Lymphomas [NCT01132911]Phase 15 participants (Anticipated)Interventional2010-05-10Completed
A Phase I Trial of Sirolimus (mTOR Inhibitor) or Vorinostat (HDAC Inhibitor) in Combination With Hydroxychloroquine (Autophagy Inhibitor) in Patients With Advanced Malignancies [NCT01266057]Phase 1143 participants (Actual)Interventional2011-04-28Completed
A Phase I/II Trial of Vorinostat and Pegylated Liposomal Doxorubicin in Relapsed or Refractory Lymphomas [NCT00785798]Phase 1/Phase 217 participants (Actual)Interventional2009-01-31Terminated(stopped due to sponsor requested)
The Effect of Vorinostat on ACTH Producing Pituitary Adenomas in Cushing's Disease [NCT04339751]Phase 222 participants (Anticipated)Interventional2024-01-03Recruiting
Phase I Trial of Ixabepilone and Vorinostat in Metastatic Breast Cancer [NCT01084057]Phase 156 participants (Actual)Interventional2010-05-17Completed
Vorinostat With Gemcitabine/Clofarabine/Busulfan for Allogeneic Transplantation for Aggressive Lymphomas [NCT04220008]Phase 230 participants (Anticipated)Interventional2023-06-01Not yet recruiting
A Pilot Study of Peroral Vorinostat (SAHA) in Patients With Refractory Histone Deacetylase-positive Uterine Sarcoma [NCT03509207]Phase 23 participants (Actual)Interventional2017-12-14Terminated(stopped due to The early termination was NOT due to safety reasons, terminated because of the very slow recruitment and problematic access to the study medication in Europe)
A Phase IIb Trial of Vorinostat in Combination With Lenalidomide and Dexamethasone in Multiple Myeloma Patients Refractory to Previous Lenalidomide Containing Regimens [NCT01502085]Phase 1/Phase 225 participants (Actual)Interventional2011-12-31Completed
Pilot Study of the Effect of Vorinostat on Nervous System Hemangioblastomas In Von Hippel-Lindau Disease [NCT02108002]Phase 17 participants (Actual)Interventional2014-04-05Completed
A Randomized Phase II/III Study of Azacitidine in Combination With Lenalidomide (NSC-703813) vs. Azacitidine Alone vs. Azacitidine in Combination With Vorinostat (NSC-701852) for Higher-Risk Myelodysplastic Syndromes (MDS) and Chronic Myelomonocytic Leuke [NCT01522976]Phase 2282 participants (Actual)Interventional2012-03-01Active, not recruiting
A Phase I Clinical Study of L-001079038 in Patients With Solid Tumors [NCT00127127]Phase 118 participants (Actual)Interventional2005-06-10Completed
A Phase I Study of Pazopanib and Vorinostat in Patients With Advanced Malignancies [NCT01339871]Phase 1152 participants (Actual)Interventional2011-04-20Completed
A Pilot Study to Assess the Safety and Effect on HIV Transcription of Vorinostat in Patients Receiving Suppressive Combination Anti-retroviral Therapy [NCT01365065]Phase 220 participants (Actual)Interventional2011-05-31Active, not recruiting
High-Dose Vorinostat With Radiation Therapy in the Treatment of Recurrent Glioma [NCT01378481]Phase 130 participants (Actual)Interventional2012-06-30Terminated
A Phase 2 Clinical Trial Testing the Safety and Efficacy of Voronistat in Pediatric Patients With Drug Resistant Epilepsy [NCT03894826]Phase 212 participants (Anticipated)Interventional2018-12-10Recruiting
SOLAR: A Phase 2, Randomized, Open-label, Parallel-group, Active Comparator, Multi-center Study to Investigate the Efficacy and Safety of Cobomarsen (MRG-106) in Subjects With Cutaneous T-Cell Lymphoma (CTCL), Mycosis Fungoides (MF) Subtype [NCT03713320]Phase 237 participants (Actual)Interventional2019-04-02Terminated(stopped due to The study was terminated early for business reasons, and not due to concerns regarding safety or lack of efficacy.)
A Phase III, Randomized, Double-Blind, Placebo-Controlled Trial of Oral Suberoylanilide Hydroxamic Acid (Vorinostat, MK-0683) in Patients With Advanced Malignant Pleural Mesothelioma Previously Treated With Systemic Chemotherapy [NCT00128102]Phase 3661 participants (Actual)Interventional2005-06-30Completed
Phase I Clinical Trial of Vorinostat (MK-0683) in Combination With Bortezomib in Patients With Advanced Multiple Myeloma [NCT00111813]Phase 134 participants (Actual)Interventional2005-09-30Completed
TINI 2: Total Therapy for Infants With Acute Lymphoblastic Leukemia II [NCT05848687]Phase 1/Phase 290 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Phase I/II Study of Carboplatin and Etoposide in Combination With Vorinostat for Patients With Extensive Stage Small Cell Lung Cancer [NCT00702962]Phase 1/Phase 28 participants (Actual)Interventional2008-09-30Terminated(stopped due to Poor accrual)
Multicenter Phase I/Ib Trial of Olaparib in Combination With Vorinostat in Patients With Relapsed/Refractory and/or Metastatic Breast Cancer [NCT03742245]Phase 128 participants (Anticipated)Interventional2019-06-11Recruiting
Carfilzomib/SAHA Combined With High-Dose Gemcitabine/Busulfan/Melphalan With Autologous Stem Cell Transplant for Patients With Refractory/Relapsed Myeloma [NCT02114502]Phase 20 participants (Actual)Interventional2014-09-30Withdrawn
A Study Using Molecular Guided Therapy With Induction Chemotherapy Followed by a Randomized Controlled Trial of Standard Immunotherapy With or Without DFMO Followed by DFMO Maintenance for Subjects With Newly Diagnosed High-Risk Neuroblastoma [NCT02559778]Phase 2500 participants (Anticipated)Interventional2015-09-30Recruiting
Phase I Study of the HDAC Inhibitor Vorinostat With Chemotherapy and Radiation Therapy for Treatment of Locally Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT01059552]Phase 118 participants (Actual)Interventional2009-12-16Completed
Phase I Clinical Trial of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Pemetrexed and Cisplatin in Patients With Advanced Cancer [NCT00106626]Phase 152 participants (Actual)Interventional2005-08-31Completed
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524]Phase 12 participants (Actual)Interventional2020-04-01Active, not recruiting
A Phase I Study of the Combination of Lenalidomide With the Histone Deacetylase Inhibitor, Vorinostat in Hodgkin and Non Hodgkin's Lymphoma [NCT01116154]Phase 130 participants (Anticipated)Interventional2010-05-31Terminated(stopped due to Sponsor withdrew support for the study)
Phase I Study of Decitabine, Vorinostat, and Cytarabine in Acute Myeloid Leukemia [NCT01130506]Phase 117 participants (Actual)Interventional2010-05-17Completed
A Phase I Study of Carboplatin + Paclitaxel and MK0683 in Patients With Chemotherapy-naive Non-Small Cell Lung Cancer (NSCLC) [NCT00424775]Phase 13 participants (Actual)Interventional2007-01-31Terminated
A Phase I Clinical Trial of Vorinostat in Combination With Gemcitabine Plus Platinum in Patients With Advanced Non-Small Cell Lung Cancer [NCT00423449]Phase 161 participants (Actual)Interventional2007-03-31Completed
MT2022-06: Phase I Study of FT538 Monotherapy and in Combination With Vorinostat for the Treatment of Persistent Low-Level HIV Viremia [NCT05700630]Phase 134 participants (Anticipated)Interventional2024-07-15Not yet recruiting
Research In Viral Eradication of HIV Reservoirs [NCT02336074]Phase 260 participants (Actual)Interventional2015-11-27Completed
A Phase I/II Trial of Vorinostat (SAHA) (NSC-701852) in Combination With Rituximab-CHOP in Patients With Newly Diagnosed Advanced Stage Diffuse Large B-Cell Lymphoma (DLBCL) [NCT00972478]Phase 1/Phase 283 participants (Actual)Interventional2010-11-15Active, not recruiting
Fludarabine/Clofarabine/Busulfan Combined With SAHA in Patients Receiving Allogeneic Hematopoietic Stem Cell Transplantation for Acute Leukemia [NCT02083250]Phase 170 participants (Actual)Interventional2014-03-06Completed
A Phase I/II Study of First Line Vorinostat With Pemetrexed-cisplatin, in Patients With Malignant Pleural Mesothelioma [NCT01353482]Phase 1/Phase 20 participants (Actual)InterventionalWithdrawn(stopped due to UCL CTC were informed by Merck Sharp & Dohme on 22.08.11 that support for the trial had been withdrawn in light of results from another trial with trial drug.)
A Randomized Phase II/III Study of Vorinostat and Local Irradiation OR Temozolomide and Local Irradiation OR Bevacizumab and Local Irradiation Followed by Maintenance Bevacizumab and Temozolomide in Children With Newly Diagnosed High-Grade Gliomas [NCT01236560]Phase 2/Phase 3101 participants (Actual)Interventional2010-11-15Active, not recruiting
A Sequential Phase I/Randomized Phase II Trial of Vorinostat and Risk-Adapted Chemotherapy With Rituximab in HIV-Related B-Cell Non-Hodgkin's Lymphoma [NCT01193842]Phase 1/Phase 2107 participants (Actual)Interventional2010-10-06Completed
Modulation of Autophagy: A Clinical Study of Vorinostat Plus Hydroxychloroquine Versus Regorafenib in Refractory Metastatic Colorectal Cancer (mCRC) Patients (CTMS# 14-2015) [NCT02316340]Phase 244 participants (Actual)Interventional2015-02-11Completed
Cisplatin and Sodium Thiosulfate Otoprotection With or Without SAHA/Vorinostat Histone Deacetylase Inhibition for Relapsed/Refractory Hepatoblastoma and Other Embryonal Tumors [NCT05756660]Early Phase 133 participants (Anticipated)Interventional2023-03-01Recruiting
Phase I/II Adaptive Randomized Trial of Bevacizumab Versus Bevacizumab Plus Vorinostat in Adults With Recurrent Glioblastoma [NCT01266031]Phase 1/Phase 296 participants (Actual)Interventional2011-07-12Completed
A Phase 1 Study of Lenalidomide in Combination With Vorinostat in Pediatric Patients With High Grade or Progressive Central Nervous System Tumors [NCT03050450]Phase 18 participants (Actual)Interventional2016-08-10Terminated(stopped due to Lack of feasibility to accrue patients in allotted time.)
Phase I Study of the Aurora Kinase a Inhibitor MLN8237 in Combination With the Histone Deacetylase Inhibitor Vorinostat in Lymphoid Malignancies [NCT01567709]Phase 134 participants (Actual)Interventional2012-04-16Completed
A Phase I Study of 131I-MIBG With Dinutuximab +/- Vorinostat for Relapsed/Refractory Neuroblastoma [NCT03332667]Phase 145 participants (Actual)Interventional2018-09-12Active, not recruiting
A Phase I/II Clinical Study of Vorinostat in Combination With Etoposide in Pediatric Patients < 21 Years at Diagnosis With Refractory Solid Tumors [NCT01294670]Phase 1/Phase 227 participants (Actual)Interventional2011-02-09Completed
A Dose-escalating and Phase II Clinical Trial of the Histone Deacetylase (HDAC) Inhibitor Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA, ZolinzaTM) in Combination With Capecitabine (XelodaTM) Using a New Weekly Dose Regimen for Advanced Breast Cancer [NCT00719875]Phase 124 participants (Actual)Interventional2008-12-31Completed
A Randomized Phase II Study of Two Dose-Levels of Vorinostat in Combination With 5-FU and Leucovorin in Patients With Refractory Metastatic Colorectal Cancer [NCT00942266]Phase 258 participants (Actual)Interventional2009-07-31Completed
IGHID 11627 - A Phase I Study to Evaluate the Effects of Vorinostat and HIV-1 Antigen Expanded Specific T Cell Therapy (HXTC) on Persistent HIV-1 Infection in HIV-Infected Individuals Started on Antiretroviral Therapy (The XTRA Study) [NCT03212989]Phase 117 participants (Actual)Interventional2017-06-27Completed
A Phase I/II Study of Vorinostat in Combination With Low Dose Ara-C for Patients With Intermediate-2 or High Risk Myelodysplastic Syndromes [NCT00776503]Phase 1/Phase 252 participants (Actual)Interventional2008-05-31Completed
A Phase 1b Study to Evaluate the Safety and Tolerability of AMG 655 in Combination With Bortezomib or Vorinostat in Subjects With Relapsed or Refractory Lymphoma [NCT00791011]Phase 133 participants (Actual)Interventional2008-02-29Completed
Phase I/II Clinical Trial Evaluating the Use of Vorinostat Combined With Paclitaxel and Radiotherapy in Patients With Inoperable Stage III Non-Small Cell Lung Cancer Unable to Tolerate Cisplatin [NCT00662311]Phase 1/Phase 25 participants (Actual)Interventional2008-03-31Terminated
A Phase I Clinical Trial of Vorinostat in Combination With Vinorelbine in Patients With Advanced Cancer. [NCT00801151]Phase 130 participants (Anticipated)Interventional2009-01-31Terminated
A Phase I/II Study of Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA) in Combination With Isotretinoin (13-cis Retinoic Acid, 13-CRA) in the Treatment of Patients With Advanced Renal Cell Carcinoma [NCT00324740]Phase 1/Phase 214 participants (Actual)Interventional2006-03-31Terminated
Phase II Study of Idarubicin, Cytarabine, and Vorinostat in Patients With High-Risk MDS and AML [NCT00656617]Phase 2106 participants (Actual)Interventional2008-04-30Completed
BMS CA180157: A Phase I Combination Study of Dasatinib Plus Vorinostat in Accelerated Phase, Chronic Phase Refractory to Second Line Therapy or Blast Crisis Chronic Myelogenous Leukemia (CML), and in Philadelphia Chromosome Positive Acute Lymphoblastic Le [NCT00816283]Phase 15 participants (Actual)Interventional2008-09-30Completed
HDAC Inhibitor Vorinostat in Resistant BRAF V600 Mutated Advanced Melanoma [NCT02836548]Phase 1/Phase 222 participants (Anticipated)Interventional2016-06-30Recruiting
Phase II Trial of Velcade Plus Vorinostat in the Treatment of High Risk MDS and Relapsed/Refractory AML [NCT00818649]Phase 216 participants (Actual)Interventional2009-01-31Terminated(stopped due to Met protocol stop rule [i.e., extreme toxicity])
An Open-Label, Proof of Concept Study of Vorinostat for the Treatment of Moderate-to-Severe Crohn's Disease and Maintenance Therapy With Ustekinumab [NCT03167437]Phase 1/Phase 235 participants (Anticipated)Interventional2017-10-30Recruiting
IGHID 11802 - Combination Therapy With the Novel Clearance Modality (VRC07-523LS) and the Latency Reversal Agent (Vorinostat) to Reduce the Frequency of Latent, Resting CD4+ T Cell Infection (The VOR-07 Study) [NCT03803605]Phase 115 participants (Actual)Interventional2019-02-12Completed
A Randomized Study to Compare the Efficacy of Vorinostat/Hydroxychloroquine/Maraviroc (VHM) in Controlling HIV After Treatment Interruption in Subjects Who Initiated ART During Acute HIV Infection [NCT02475915]Phase 1/Phase 215 participants (Actual)Interventional2015-01-31Completed
Epigenetic Reprogramming in Relapse AML: A Phase 1 Study of Decitabine and Vorinostat Followed by Fludarabine, Cytarabine and G-CSF (FLAG) in Children and Young Adults With Relapsed/Refractory AML [NCT03263936]Phase 137 participants (Actual)Interventional2017-07-11Completed
Phase I of Vorinostat-Iressa Combined Therapy on Resistance by BIM Polymorphysim in EGFR Mutant Lung Cancer [NCT02151721]Phase 112 participants (Actual)Interventional2014-06-01Active, not recruiting
A Single Arm Phase I/II Study of MK-3475 Combined With Vorinostat for Recurrent Unresectable and/or Metastatic Squamous Cell Head and Neck Cancer and Recurrent Unresectable and/or Metastatic Salivary Gland Malignancies [NCT02538510]Phase 1/Phase 250 participants (Actual)Interventional2015-10-08Completed
Phase I Trial of Chemoradiation With Capecitabine and Vorinostat in Pancreatic Cancer. [NCT00983268]Phase 121 participants (Actual)Interventional2009-10-31Completed
A Phase I Trial Evaluating the Safety and Efficacy of Vorinostat (Zolinza ®) + RVD (Lenalidomide {Revlimid ®} + Bortezomib {Velcade ®} + Dexamethasone) for Patients With Newly Diagnosed Multiple Myeloma [NCT01038388]Phase 130 participants (Actual)Interventional2010-01-15Completed
Phase I/II Trial of Lenalidomide in Combination With Vorinostat and Dexamethasone as Therapy in Relapsed or Refractory Patients With Peripheral T-Cell Non-Hodgkin's Lymphoma (PTCL) [NCT00972842]Phase 1/Phase 220 participants (Anticipated)Interventional2009-09-30Terminated(stopped due to slow recruitment)
A Phase I Study of Vorinostat and Bortezomib in Children With Refractory or Recurrent Solid Tumors, Including CNS Tumors and Lymphomas [NCT00994500]Phase 120 participants (Actual)Interventional2009-08-31Completed
A Phase I Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (Vorinostat; Zolinza) in Combination With Bexarotene in Patients With Advanced Cutaneous T-Cell Lymphoma [NCT00127101]Phase 123 participants (Actual)Interventional2005-09-30Terminated(stopped due to The study was stopped due to low enrollment.)
A Phase I/II Study of Pembrolizumab and Vorinostat in Patients With Immune Therapy Naïve and Immune Therapy Pretreated Stage IV NSCLC [NCT02638090]Phase 1/Phase 2124 participants (Actual)Interventional2016-03-22Active, not recruiting
A Randomized Phase IIa Study of Vorinostat in Patients With Low or Intermediate-1 Risk Myelodysplastic Syndrome [NCT00486720]Phase 222 participants (Actual)Interventional2007-06-30Terminated
A Phase I Trial of Vorinostat Concurrent With Stereotactic Radiotherapy in Treatment of Brain Metastases From Non-Small Cell Lung Cancer [NCT00946673]Phase 117 participants (Actual)Interventional2009-06-30Completed
A Pilot Study Evaluating Surrogates of Response to Short Term Oral Suberoylanilide Hydroxamic Acid (SAHA) in Women With Newly Diagnosed Breast Cancer [NCT00262834]Phase 254 participants (Actual)Interventional2005-10-31Completed
A Multi-Institutional Double-Blind Phase II Study Evaluating Response and Surrogate Biomarkers to Carboplatin and Nab-Paclitaxel (CP) With or Without Vorinostat as Preoperative Chemotherapy in HER2-negative Primary Operable Breast Cancer [NCT00616967]Phase 268 participants (Actual)Interventional2008-05-31Active, not recruiting
Phase I Clinical and Pharmacological Study of Suberoylanilide Hydroxamic Acid- SAHA (MSK390) in Patients With Advanced Solid Tumors [NCT00005634]Phase 10 participants Interventional2000-01-31Completed
An International, Multicenter, Open-Label Study of Vorinostat (MK0683) in Combination With Bortezomib in Patients With Relapsed or Refractory Multiple Myeloma [NCT00773838]Phase 2143 participants (Actual)Interventional2008-12-01Completed
A Multicenter, Open-Label, Phase I Study of MK-0683 in Combination With Bortezomib in Patients With Relapsed and/or Refractory Multiple Myeloma [NCT00858234]Phase 19 participants (Actual)Interventional2009-02-13Completed
Phase II Study of Vorinostat (SAHA), Cladribine, and Rituximab (SCR) in Mantle Cell Lymphoma, Chronic Lymphocytic Leukemia, and Relapsed B Cell Non-Hodgkin Lymphoma [NCT00764517]Phase 257 participants (Actual)Interventional2008-08-31Completed
Phase I Study of Vorinostat in Combination With Niacinamide, and Etoposide for the Treatment of Patients With Relapsed and Refractory Lymphoid Malignancies [NCT00691210]Phase 140 participants (Actual)Interventional2008-06-30Completed
A Phase I Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of MK0683 in Patients With Advanced Cancer [NCT00750178]Phase 130 participants (Actual)Interventional2004-11-01Completed
Neoadjuvant Androgen Depletion in Combination With Vorinostat Followed by Radical Prostatectomy for Localized Prostate Cancer: Total Androgen-Receptor Gene Expression Targeted Therapy (TARGET) [NCT00589472]Phase 219 participants (Actual)Interventional2007-11-30Completed
A Phase I/II Non-Comparative Study of Paclitaxel Plus Carboplatin in Combination With Vorinostat in Patient With Advanced, Recurrent, Epithelial Ovarian Cancer [NCT00772798]Phase 270 participants (Anticipated)Interventional2007-06-30Recruiting
A Phase II Study to Investigate the Efficacy and Tolerability of Vorinostat in Patients Suffering From Advanced, Metastatic Soft Tissue Sarcoma [NCT00918489]Phase 240 participants (Actual)Interventional2010-05-31Completed
A Phase II Study of Vorinostat (Suberoylanilide Hydroxamic Acid) Plus Rituximab in Indolent Non-Hodgkin's Lymphoma [NCT00720876]Phase 230 participants (Actual)Interventional2008-07-23Completed
Phase I Study of Carboplatin, Paclitaxel, Bevacizumab and Vorinostat for Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00702572]Phase 125 participants (Actual)Interventional2008-04-30Terminated(stopped due to Low Enrollment)
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Flavopiridol in Advanced Solid Tumors [NCT00324480]Phase 160 participants (Actual)Interventional2006-03-31Completed
A Phase I/II of Vorinostat Plus CHOP in Untreated T-cell Non-Hodgkin's Lymphoma [NCT00787527]Phase 1/Phase 214 participants (Actual)Interventional2008-11-30Completed
Phase II Trial of Vorinostat Plus Tacrolimus & Mycophenolate to Prevent Graft Versus Host Disease Following Reduced Intensity Conditioning Related Donor Allogeneic Transplant [NCT00810602]Phase 1/Phase 261 participants (Actual)Interventional2009-01-31Completed
A Phase 1/2 Study of Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat) and Local Irradiation, Followed by Maintenance SAHA in Children With Newly Diagnosed Diffuse Intrinsic Pontine Gliomas (DIPG) [NCT01189266]Phase 1/Phase 279 participants (Actual)Interventional2010-08-09Completed
An International, Multicenter, Randomized, Double-Blind Study of Vorinostat (MK-0683) or Placebo in Combination With Bortezomib in Patients With Multiple Myeloma [NCT00773747]Phase 3637 participants (Actual)Interventional2008-12-01Completed
A Phase I Trial of Vorinostat in Combination With Bevacizumab and Irinotecan in Recurrent Glioblastoma [NCT00762255]Phase 119 participants (Actual)Interventional2008-09-30Completed
A Phase II Pharmacodynamic Investigation of the Efficacy of Vorinostat to Induce Fetal Hemoglobin in Adults With Severe Sickle Cell Disease Who Have Not Benefitted From Prior Therapy [NCT01000155]Phase 25 participants (Actual)Interventional2009-10-31Terminated(stopped due to The study terminated early due to slow accrual.)
A Phase I Study of Ridaforolimus and Vorinostat in Patients With Advanced Solid Tumors or Lymphoma (IND 109130) [NCT01169532]Phase 116 participants (Actual)Interventional2010-10-31Completed
Phase I Study of Induction Therapy With VELCADE and Vorinostat in Patients With Surgically Resectable Non-Small Cell Lung Cancer [NCT00731952]Phase 121 participants (Actual)Interventional2006-06-30Completed
Phase II Clinical Evaluation of Vorinostat Combined With Salvage Reinduction Chemotherapy Including Gemtuzumab Ozogamicin, Idarubicin and Cytarabine and Vorinostat Maintenance in Relapse or Refractory Acute Myeloid Leukemia Patients With 50 Years or Older [NCT01039363]Phase 227 participants (Anticipated)InterventionalNot yet recruiting
IGHID 11424 - A Pilot Trial of the Effect of Vorinostat and AGS-004 on Persistent HIV-1 Infection (The VOR VAX Study) [NCT02707900]Phase 16 participants (Actual)Interventional2016-03-31Terminated(stopped due to Manufacturing of the AGS-004 HIV vaccine by Argos could no longer be provided.)
GCC 0845: Pilot and Phase II- Vorinostat and Lapatinib in Patients With Advanced Solid Tumor Malignancies and Women With Recurrent Local-Regional or Metastatic Breast Cancer to Evaluate Response and Biomarkers of EMT and Breast Cancer Stem Cells [NCT01118975]Phase 1/Phase 212 participants (Actual)Interventional2010-03-31Terminated(stopped due to Lost sponsorship for study drug)
A Phase 1 Dose Escalation Study of Bortezomib (Velcade®), Pegylated Liposomal Doxorubicin (Doxil®), and Vorinostat (Suberoylanilide Hydromaxic Acid, Saha, Zolinzatm) in Patients With Relapse/Refractory Multiple Myeloma [NCT00744354]Phase 132 participants (Actual)Interventional2008-10-31Terminated(stopped due to Drugs unavailable- study terminated 1/2/18)
Phase I/II Trial of Vorinostat and Radiation Therapy in Patients With Locally Advanced Pancreatic Cancer [NCT00831493]Phase 1/Phase 23 participants (Actual)Interventional2009-05-31Terminated(stopped due to Slow Accrual.)
Progression Free Survival (PFS) Comparison Between Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat TM) in Combination With Bortezomib (Velcade TM) and SAHA Alone in Refractory or Recurrent Advanced CTCL. A Randomized Study. [NCT01386398]Phase 30 participants (Actual)InterventionalWithdrawn(stopped due to Company withdrew interest)
Safety of Vorinostat in Combination With Bortezomib, Doxorubicin and Dexamethasone (VBDD) in Patients With Refractory or Relapsed Multiple Myeloma, A Phase I/II Study, Short Title: VBDD [NCT01394354]Phase 1/Phase 234 participants (Actual)Interventional2011-08-31Completed
Phase I, Open-label, Dose-escalation Study of the Combination of Sorafenib and Vorinostat in Poor-risk Acute Myelogenous Leukemia (AML) and High Risk Myelodysplastic Syndrome (MDS) [NCT00875745]Phase 115 participants (Actual)Interventional2009-04-30Completed
Phase I/II Study of a Combination of Suberoylanilide Hydroxamic Acid (Vorinostat) Plus Paclitaxel and Bevacizumab in Patients With Advanced Metastatic and/or Local Chest Wall Recurrent Breast Cancer [NCT00368875]Phase 1/Phase 254 participants (Actual)Interventional2006-07-31Completed
A Phase II Study of MK-0683 in Patients With Polycythaemia Vera and Essential Thrombocythaemia. [NCT00866762]Phase 260 participants (Anticipated)Interventional2009-02-28Active, not recruiting
Randomized Phase II Study of Vorinostat or Placebo in Combination With Carboplatin and Paclitaxel for Patients With Advanced or Metastatic Non-Small Cell Lung Cancer [NCT00481078]Phase 294 participants (Actual)Interventional2007-05-31Completed
A Window Trial of Vorinostat in Patients With Ductal Carcinoma in Situ (DCIS) of the Breast [NCT00788112]Phase 117 participants (Actual)Interventional2009-07-31Completed
Bortezomib and Vorinostat as Maintenance Therapy After Autologous Stem Cell Transplant for Multiple Myeloma [NCT00839956]Phase 231 participants (Actual)Interventional2009-02-28Completed
A Phase 2 Study of Suberoylanilide Hydroxamic Acid (SAHA) in Acute Myeloid Leukemia (AML) [NCT00305773]Phase 237 participants (Actual)Interventional2006-01-31Completed
Phase II Study of Vorinostat (SAHA) in Combination With Bortezomib (PS-341) in Patients With Recurrent Glioblastoma Multiforme [NCT00641706]Phase 244 participants (Actual)Interventional2008-07-31Completed
A Phase I Study of Vorinostat in Combination With Lenalidomide and Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma [NCT00642954]Phase 131 participants (Actual)Interventional2008-02-13Completed
A Pilot Clinical Trial to Evaluate the Biological Activity of HDAC (Histone Deacetylase Transferases) Inhibition on ER and PR Expression in Triple Negative Invasive Breast Cancer [NCT01695057]0 participants (Actual)Interventional2012-10-31Withdrawn(stopped due to Lack of funding)
Phase II Study of Combination Vorinostat and Bortezomib in Patients With Relapsed and/or Refractory Non-Hodgkin Lymphoma [NCT00837174]Phase 20 participants (Actual)Interventional2010-06-30Withdrawn(stopped due to Study never activated/opened as funding source and other support not available.)
Phase II Trial of Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Recurrent Glioblastoma [NCT00238303]Phase 2103 participants (Actual)Interventional2005-09-30Completed
A Phase II, Pharmacokinetic and Biologic Correlative Study of Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Advanced Renal Cell Carcinoma (RCC) [NCT00278395]Phase 214 participants (Actual)Interventional2005-10-31Completed
Phase I Study of Vorinostat [Suberoylanilide Hydroxamic Acid (VORINOSTAT)] With Irinotecan, 5-Fluorouracil (5-FU) and Leucovorin (FOLFIRI) for Advanced Upper Gastrointestinal Cancers [NCT00537121]Phase 123 participants (Actual)Interventional2006-11-30Completed
A Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Indolent Non-Hodgkin's Lymphoma [NCT00253630]Phase 237 participants (Actual)Interventional2005-09-30Completed
MK0683 Phase1 Clinical Study - Solid Tumor - [NCT00373490]Phase 116 participants (Actual)Interventional2006-07-31Completed
A Phase I/II Clinical Trial of Oral Vorinostat (MK0683) in Combination With Erlotinib in Patients With Relapsed/Refractory Non-Small-Cell Lung Cancer [NCT00251589]Phase 1/Phase 223 participants (Actual)Interventional2006-01-31Terminated(stopped due to This trial is being closed based on lack of substantive efficacy, slow accrual and overall tolerance in patients treated to date.)
A Phase I Study of SAHA and Temozolomide in Children With Relapsed or Refractory Primary Brain or Spinal Cord Tumors [NCT01076530]Phase 127 participants (Actual)Interventional2010-02-28Completed
A Phase II Trial of Suberoylanilide Hydroxamic Acid (NSC-701852) for Recurrent or Primary Refractory Hodgkin's Lymphoma [NCT00132028]Phase 227 participants (Actual)Interventional2005-09-30Completed
A Phase I/II Study of Vorinostat (Zolinza®) in Combination With Capecitabine (X) and Cisplatin (P) for 1st Line Treatment of Metastatic or Recurrent Gastric Cancer [NCT01045538]Phase 1/Phase 245 participants (Actual)Interventional2010-02-28Completed
A Phase I Study of Sorafenib and Vorinostat in Advanced Hepatocellular Carcinoma [NCT01075113]Phase 116 participants (Actual)Interventional2010-08-10Completed
A Phase 1 Study of SAHA (NSC# 701852) in Pediatric Patients With Recurrent or Refractory Solid Tumors (Including Lymphomas) and Leukemia Followed by a Phase I Study of SAHA in Combination With 13-Cis-Retinoic Acid for Patients With Selected Recurrent/Refr [NCT00217412]Phase 160 participants (Actual)Interventional2005-08-31Completed
A Phase I Trial of Sirolimus or Everolimus or Temsirolimus (mTOR Inhibitor) and Vorinostat (Histone Deacetylase Inhibitor) in Patients With Advanced Cancer [NCT01087554]Phase 1249 participants (Anticipated)Interventional2010-03-31Active, not recruiting
A Phase II Study of Suberoylanilide Hydroxamic Acid and Bortezomib in Advanced Soft Tissue Sarcomas [NCT00937495]Phase 216 participants (Actual)Interventional2009-06-30Completed
A Phase I Study of Suberoylanilide Hydroxamic Acid (Vorinostat) (NSC 701852) in Combination With Docetaxel in Patients With Advanced and Relapsed Solid Malignancies [NCT00565227]Phase 112 participants (Actual)Interventional2007-04-30Terminated(stopped due to closed due to toxicity)
A Phase II/III Randomized, Double-Blind Study of Paclitaxel Plus Carboplatin in Combination With Vorinostat or Placebo in Patients With Stage IIIB (With Pleural Effusion) or Stage IV Non-Small-Cell Lung Cancer (NSCLC) [NCT00473889]Phase 2/Phase 3253 participants (Actual)Interventional2007-05-31Terminated(stopped due to The study was terminated based on the recommendation by the DSMB following a pre-planned protocol interim analysis because the endpoint was not achieved.)
A Phase I Clinical Trial of Vorinostat in Combination With Decitabine in Patients With Acute Myelogenous Leukemia or Myelodysplastic Syndrome [NCT00479232]Phase 171 participants (Actual)Interventional2007-06-30Completed
A Phase 1 Study of Pembrolizumab Plus Vorinostat for Relapsed or Refractory Diffuse Large B-Cell Lymphoma, Follicular Lymphoma, and Hodgkin Lymphoma [NCT03150329]Phase 152 participants (Actual)Interventional2017-07-18Active, not recruiting
Vorinostat and Concomitant Whole Brain Radiation Therapy in Patients With Brain Metastases: A Randomized, Double-blind, Placebo-controlled, Phase II Study [NCT01600742]Phase 24 participants (Actual)Interventional2012-08-31Terminated(stopped due to Sponsor stops to provide the study drug.)
Vorinostat to Augment Response to Lutetium-PSMA-617 in the Treatment of Patients With PSMA-Low Metastatic Castration-Resistant Prostate Cancer [NCT06145633]Phase 215 participants (Anticipated)Interventional2024-04-01Not yet recruiting
Vorinostat (SAHA) and Lenalidomide After Autologous Transplant for Patients With Multiple Myeloma [NCT00729118]Phase 119 participants (Actual)Interventional2008-09-26Completed
Phase I-II Study of Oral Suberoylanilide Hydroxamic Acid (Vorinostat) in Combination With Topotecan in Patients With Chemosensitive Recurrent Small Cell Lung Cancer (SCLC) [NCT00697476]Phase 1/Phase 22 participants (Actual)Interventional2009-01-31Terminated(stopped due to insufficient enrollment)
NPI-0052 and Vorinostat in Patients With Non-small Cell Lung Cancer, Pancreatic Cancer, Melanoma or Lymphoma [NCT00667082]Phase 122 participants (Actual)Interventional2008-03-31Completed
A Phase I Safety and Tolerability Study of Vorinostat in Combination With Sorafenib in Patients With Advanced Solid Tumors, With Exploration of Two Tumor-type Specific Expanded Cohorts at the Recommended Phase 2 Dose [NCT00635791]Phase 136 participants (Actual)Interventional2008-03-31Completed
Phase Ib/II Study of Combination of Vorinostat, Carboplatin and Gemcitabine + Vorinostat Maintenance in Women With Recurrent, Platinum-Sensitive Epithelial Ovarian, Fallopian Tube, or Peritoneal Cancer [NCT00910000]Phase 1/Phase 215 participants (Actual)Interventional2009-06-30Terminated(stopped due to Terminated due to unacceptable toxicity)
A Continuation Clinical Trial of Oral Vorinostat (MK-0683) in Advanced Cancers [NCT00907738]Phase 227 participants (Actual)Interventional2005-08-31Completed
Bortezomib* and Vorinostat as Maintenance Therapy After Autologous Transplant for Non-Hodgkin Lymphoma Using R-BEAM or BEAM Conditioning Transplant Regimen [NCT00992446]Phase 227 participants (Actual)Interventional2010-09-02Completed
A Phase II Prospective Non-Randomized Clinical Trial of Dose-Adjusted Schedule of Vorinostat in Patients With Primary Cutaneous T-Cell Lymphoma Who Did Not Receive Prior Systemic Therapy or Have Been Treated With Single Agent Targretin [NCT00958074]Phase 211 participants (Actual)Interventional2009-07-31Terminated(stopped due to Terminated due to slow accrual)
Phase 1/2 Study of Vorinostat in Combination With Radiation Therapy and Infusional 5-FU in Patients With Locally Advanced Adenocarcinoma of the Pancreas [NCT00948688]Phase 1/Phase 210 participants (Actual)Interventional2009-08-31Terminated(stopped due to Funding was withdrawn after only 10 participants were enrolled)
A Phase 2 Trial of Vorinostat in Combination With Azacitidine in Patients With Newly-Diagnosed Acute Myelogenous Leukemia (AML) or Myelodysplastic Syndrome (MDS) Who Are Ineligible for Other Leukemia Protocols [NCT00948064]Phase 2110 participants (Actual)Interventional2009-09-08Completed
Phase I Trial of Vorinostat (NSC-701852, Suberoylanilide Hydroxamic Acid) and Doxorubicin (NSC-123127, Adriamycin) [NCT00331955]Phase 140 participants (Actual)Interventional2006-03-31Completed
Vorinostat (SAHA) Combined With High-Dose Gemcitabine, Busulfan, and Melphalan With Autologous Hematopoietic Cell Support for Patients With Relapsed or Refractory Lymphoid Malignancies [NCT01421173]Phase 178 participants (Actual)Interventional2011-08-31Completed
Phase I/II Intra-patient Dose Escalation Study of Vorinostat in Children With Relapsed Solid Tumor, Lymphoma or Leukemia [NCT01422499]Phase 1/Phase 250 participants (Actual)Interventional2012-03-31Completed
A Pilot Study of Oral Vorinostat Plus Oral Eltrombopag Support in Patients With Lymphoma (VEIL) [NCT01500538]Phase 21 participants (Actual)Interventional2012-10-31Terminated(stopped due to Poor recruitment rate)
A Phase I/II, Multi-Center, Open Label Study of Vorinostat Plus Melphalan and Prednisone (ZMP) in Advanced, Refractory Multiple Myeloma Patients [NCT00857324]Phase 1/Phase 218 participants (Actual)Interventional2009-03-31Terminated(stopped due to The Phase I of the study was completed, but Phase 2 has not been activated)
A Phase II Study of MK-0683 in Patients With Relapsed / Refractory Follicular Lymphoma (FL), Other Indolent B-cell Non-Hodgkin's Lymphoma (B-NHL) or Mantle Cell Lymphoma (MCL) [NCT00875056]Phase 256 participants (Actual)Interventional2009-04-15Completed
Phase I/II Study of Vorinostat (Suberoylanilide Hydroxamic Acid [SAHA]), Temozolomide, and Radiation Therapy in Patients With Newly Diagnosed Glioblastoma [NCT00731731]Phase 1/Phase 2125 participants (Actual)Interventional2009-07-10Completed
Phase I Clinical Study of MK-0683 in Patients With Relapsed or Refractory Cutaneous T-Cell Lymphoma (CTCL) [NCT00771472]Phase 110 participants (Actual)Interventional2008-08-31Completed
Phase IIb Multicenter Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Advanced Cutaneous T-cell Lymphoma [NCT00091559]Phase 274 participants (Actual)Interventional2005-02-03Completed
A Phase I/II Study of Fludarabine, Cyclophosphamide, Rituximab, and Vorinostat Followed by Rituximab and Vorinostat Maintenance Therapy in Patients With Previously Untreated B-Cell Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Lymphoma (SLL) [NCT00918723]Phase 1/Phase 240 participants (Actual)Interventional2009-06-30Completed
A Phase II Trial of Combination Treatment With Vorinostat, Bortezomib and Dexamethasone in Patients With Relapsed and Relapsed Refractory Multiple Myeloma [NCT01720875]Phase 216 participants (Actual)Interventional2013-08-09Completed
Selective Estrogen Receptor Modulators to Enhance the Efficacy of Viral Reactivation With Histone Deacetylase Inhibitors [NCT03382834]Phase 231 participants (Actual)Interventional2018-04-26Active, not recruiting
A Multi-Center, Single-Arm, Phase II Study of Vorinostat (V) in Combination With Pegylated Liposomal Doxorubicin (PLD) and Bortezomib (B) Followed by VB Maintenance in Patients With Relapsed and Relapsed/Refractory Multiple Myeloma [NCT01492881]Phase 20 participants (Actual)Interventional2012-04-30Withdrawn(stopped due to Doxil is currently unavailable)
A Phase I/II Investigation of the Effect of Vorinostat (VOR) on HIV RNA Expression in the Resting CD4+ T Cells of HIV-Infected Patients Receiving Stable Antiretroviral Therapy [NCT01319383]Phase 1/Phase 225 participants (Actual)Interventional2011-02-28Completed
A Pilot Study of Vorinostat to Restore Sensitivity to Aromatase Inhibitor Therapy [NCT01153672]8 participants (Actual)Interventional2010-11-30Completed
A Phase 1 Study of Paclitaxel and Carboplatin in Solid Tumors (With Focus on Upper Aerodigestive Cancers) in Persons With HIV Infection [NCT01249443]Phase 117 participants (Actual)Interventional2013-11-30Terminated(stopped due to Inadequate accrual rate)
A Phase 2 Study of Suberoylanilide Hydroxamic Acid (SAHA) in Subjects With Locally Advanced, Recurrent or Metastatic Adenoid Cystic Carcinoma (ACC) [NCT01175980]Phase 230 participants (Actual)Interventional2010-08-06Completed
A Multicenter, Open-label, Randomized, Phase I/II Study Evaluating the Safety and Efficacy of Low-dose (12 Gy) Total Skin Electron Beam Therapy (TSEBT) Combined With Vorinostat Versus Low-dose TSEBT Monotherapy in Mycosis Fungoides (MF) [NCT01187446]Phase 1/Phase 228 participants (Actual)Interventional2010-12-31Terminated(stopped due to Business decision by funding source)
Phase I / II Adaptive Randomized Trial of Vorinostat, Isotretinoin and Temozolomide in Adults With Recurrent Glioblastoma Multiforme [NCT00555399]Phase 1/Phase 2135 participants (Anticipated)Interventional2007-11-28Active, not recruiting
Temozolomide Plus Vorinostat in Patients With Relapse/Refractory Acute Myeloid Leukemia (AML) [NCT01550224]Phase 223 participants (Actual)Interventional2013-05-01Completed
Proof of Concept Study of Vorinostat, A Histone Deacetylase Inhibitor, in Patients With Class 2 High Risk Uveal Melanoma [NCT03022565]Early Phase 10 participants (Actual)Interventional2020-01-31Withdrawn(stopped due to Investigator Decision)
A Phase I Trial of SAHA (NSC 701852) and Decitabine (IND 50733, NSC 127716) in Patients With Relapsed, Refractory or Poor Prognosis Leukemia [NCT00357708]Phase 150 participants (Actual)Interventional2006-06-30Completed
A Phase II Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Relapsed Diffuse Large B-Cell Lymphoma (DLBCL) [NCT00097929]Phase 218 participants (Actual)Interventional2005-05-01Completed
A Phase 1 Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Gemcitabine in Patients With Epithelial Tumors [NCT00243100]Phase 121 participants (Actual)Interventional2005-11-30Completed
A Phase 1 Study of Vorinostat (Suberoylanilide Hydroxamic Acid; SAHA) in Combination With Decitabine in Patients With Advanced Solid Tumors, Relapsed or Refractory Non-Hodgkin's Lymphoma, Acute Myeloid Leukemia, Acute Lymphocytic Leukemia, or Chronic Myel [NCT00275080]Phase 180 participants (Actual)Interventional2006-02-28Completed
A Phase I Study of SAHA in Combination With Bortezomib in Relapsed and Refractory Multiple Myeloma [NCT00310024]Phase 140 participants (Actual)Interventional2005-11-30Completed
An Open Label, Expanded Access Protocol Using 131I-METAIODOBENZYLGUANIDINE (131I-MIBG) Therapy +/- Vorinostat in Patients With Refractory Neuroblastoma, Pheochromocytoma, or Paraganglioma [NCT01838187]0 participants Expanded AccessNo longer available
A Phase 1 Study of Suberoylanilide Hydroxamic Acid (Vorinostat, SAHA) in Combination With Idarubicin in Relapsed or Refractory Leukemia [NCT00331513]Phase 140 participants (Actual)Interventional2006-03-31Completed
Phase II Evaluation of Suberoylanilide Hydroxamic Acid (NSC 701852) in Patients With Advanced Prostate Cancer That Has Progressed on One Prior Chemotherapy [NCT00330161]Phase 229 participants (Actual)Interventional2006-03-31Completed
A Phase I Trial of Pembrolizumab and Vorinostat Combined With Temozolomide and Radiation Therapy for Newly Diagnosed Glioblastoma [NCT03426891]Phase 121 participants (Actual)Interventional2018-03-16Completed
A Phase I Clinical Study of MK0683 in Patients With Malignant Lymphoma [NCT00127140]Phase 110 participants (Actual)Interventional2005-06-30Completed
A Phase I Study of Suberoylanilide Hydroxamic Acid (Vorinostat) in Combination With 5-Fluorouracil, Leucovorin, and Oxaliplatin (mFOLFOX) in Patients With Colorectal Cancer and Other Solid Tumors [NCT00138177]Phase 154 participants (Actual)Interventional2005-07-31Completed
Phase II Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Advanced Multiple Myeloma [NCT00109109]Phase 160 participants Interventional2003-12-01Terminated
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Capecitabine in Patients With Solid Tumors [NCT00121277]Phase 128 participants (Actual)Interventional2005-09-30Completed
Sequential Phase I/II Trial of Oral Vorinostat in Combination With Erlotinib in Non-small-cell Lung Cancer Patients With Mutations at Epidermal Growth Factor Receptor With Disease Progression After Erlotinib Treatment [NCT00503971]Phase 1/Phase 250 participants (Actual)Interventional2007-12-31Terminated
Phase II Study of Vorinostat (SAHA, Zolinza) and Bortezomib (PS341, Velcade) as Third-Line Treatment in Patients With Advanced Non-Small Cell Lung Cancer [NCT00798720]Phase 218 participants (Actual)Interventional2008-12-31Completed
A Phase II Study To Determine The Safety and Efficacy Of The Combination of Vorinostat and Bortezomib In Patients With Relapsed Or Refractory T-Cell Non-Hodgkin's Lymphoma [NCT00810576]Phase 21 participants (Actual)Interventional2009-01-31Terminated(stopped due to Terminated due to slow accrual.)
Phase I / II Adaptive Randomized Trial of Vorinostat, Erlotinib and Temozolomide in Adults With Recurrent Glioblastoma Multiforme [NCT01110876]Phase 1/Phase 221 participants (Actual)Interventional2011-06-30Terminated(stopped due to Unanticipated Toxicities)
A Therapeutic Trial of Bortezomib (Velcade), Vorinostat (SAHA) and Dexamethasone for Relapsed/Refractory Acute Lymphoblastic Leukemia (ALL) [NCT01312818]Phase 22 participants (Actual)Interventional2011-06-30Terminated(stopped due to Slow accrual)
Phase II Randomized Study of Vorinostat or Placebo in Combination With Carboplatin and Paclitaxel for Patients With Advanced Non-small Cell Lung Cancer [NCT01413750]Phase 1/Phase 223 participants (Actual)Interventional2010-11-30Terminated(stopped due to Slow Accrual)
Phase I and Pharmacokinetic Study of Vorinostat for Solid Tumors and Lymphomas in Patients With Varying Degrees of Hepatic Dysfunction [NCT00499811]Phase 115 participants (Actual)Interventional2007-06-30Completed
Safety and Effectiveness of A-dmDT390-bisFv(UCHT1) Fusion Protein (Resimmune®) in Subjects With Mycosis Fungoides: A Phase II Multi-center Randomized Clinical Trial [NCT02943642]Phase 2162 participants (Anticipated)Interventional2017-01-31Not yet recruiting
A Phase II Study of Bortezomib and Vorinostat in Patients With Refractory or Relapsed MLL Rearranged Hematologic Malignancies [NCT02419755]Phase 212 participants (Actual)Interventional2015-04-14Terminated(stopped due to Accrual goals were no longer feasible based on restrictions imposed by the DSMB.)
A Multi-Institutional Phase II Study Evaluating Surrogate Biomarkers of Response to Short Term Oral Vorinostat and Tamoxifen in Women With Newly Diagnosed Breast Cancer [NCT01194427]Phase 22 participants (Actual)Interventional2011-03-31Terminated(stopped due to Difficulty meeting patient accrual goals)
Randomised Comparisons, in Myeloma Patients of All Ages, of Thalidomide, Lenalidomide, Carfilzomib and Bortezomib Induction Combinations, and of Lenalidomide and Combination Lenalidomide Vorinostat as Maintenance (Myeloma XI) [NCT01554852]Phase 34,420 participants (Actual)Interventional2010-05-31Active, not recruiting
A Phase II, Open Label, Two-Arm Study of Therapeutic Iobenguane (131I) as Single Agent or in Combination With Vorinostat for Recurrent or Progressive High- Risk Neuroblastoma Subjects (OPTIMUM TRIAL) [NCT03561259]Phase 260 participants (Anticipated)Interventional2019-10-21Recruiting
A Phase II Clinical Study of Oral Suberoylanilide Hydroxamic Acid in Patients With Relapsed or Refractory Breast, Colorectal, and Non-small Cell Lung Cancer. [NCT00126451]Phase 216 participants (Actual)Interventional2004-12-01Terminated
A Phase II Evaluation of Vorinostat, (SAHA, NCI-Supplied Agent [NSC #701852]) in the Treatment of Persistent or Recurrent Epithelial Ovarian or Primary Peritoneal Carcinoma [NCT00132067]Phase 260 participants (Actual)Interventional2005-10-31Completed
Phase I Clinical Trial of Oral Suberoylanilide Hydroxamic Acid - SAHA (MSK390) in Patients With Advanced Solid Tumors and Hematologic Malignancies [NCT00045006]Phase 10 participants Interventional2001-07-31Completed
Phase II Study of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Recurrent or Metastatic Transitional Cell Carcinoma of the Urothelium [NCT00363883]Phase 214 participants (Actual)Interventional2006-06-30Terminated(stopped due to Trial stopped early for futility)
Phase II Trial of Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat) in Combination With Tamoxifen for Patients With Advanced Breast Cancer Who Have Failed Prior Anti-hormonal Therapy. [NCT00365599]Phase 243 participants (Actual)Interventional2006-02-28Completed
Phase II Trial of Vorinostat (Suberoylanilide Hydroxamic Acid or SAHA; Zolinza™) in Combination With Gemtuzumab Ozogamicin (Mylotarg™) as Induction and Post-Remission Therapy in Older Patients With Previously Untreated Non-M3 Acute Myeloid Leukemia [NCT00673153]Phase 231 participants (Actual)Interventional2008-03-31Terminated
A Multi-Center Phase I/II Trial of Vorinostat in Combination With Cyclophosphamide, Etoposide, Prednisone and Rituximab for Elderly Patients With Relapsed Diffuse Large B-Cell Lymphoma (DLBCL) [NCT00667615]Phase 1/Phase 230 participants (Actual)Interventional2008-04-30Completed
Phase 1/2 Study of Vorinostat Therapy in Niemann-Pick Disease, Type C1 [NCT02124083]Phase 1/Phase 212 participants (Actual)Interventional2014-04-25Completed
Phase I Trial of Carfilzomib (PR-171) in Combination With Vorinostat (SAHA) in Patients With Relapsed/Refractory B-Cell Lymphomas [NCT01276717]Phase 120 participants (Actual)Interventional2011-01-31Completed
A Dose Escalation Study of Vorinostat in Combination With Palliative Radiotherapy for Patients With Non-Small Cell Lung Cancer [NCT00821951]Phase 117 participants (Actual)Interventional2009-05-31Completed
Epigenetic Priming for Immune Therapy in ER-Positive Breast Cancer in Biomarker Select Population [NCT04190056]Phase 21 participants (Actual)Interventional2021-03-11Terminated(stopped due to Change in practice patterns)
Olaparib Combined With High-Dose Chemotherapy for Refractory Lymphomas [NCT03259503]Phase 150 participants (Actual)Interventional2019-09-13Active, not recruiting
Total Therapy for Infants With Acute Lymphoblastic Leukemia (ALL) I [NCT02553460]Phase 1/Phase 250 participants (Actual)Interventional2016-01-29Active, not recruiting
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Bortezomib in Patients With Advanced Malignancies [NCT00227513]Phase 166 participants (Actual)Interventional2005-07-31Completed
Phase I/II Clinical Trial of Vorinostat in Patients With Recurrent and/or Metastatic Breast Cancer [NCT00416130]Phase 1/Phase 249 participants (Anticipated)Interventional2007-01-31Active, not recruiting
Phase I Study Of Suberoylanilide Hydroxamic Acid (SAHA) (NSC 701852) in Combination With Paclitaxel /Carboplatin for Advanced and Refractory Solid Malignancies [NCT00287937]Phase 130 participants (Actual)Interventional2005-07-31Completed
Pilot Study of Curcumin, Vorinostat, and Sorafenib in Patients With Advanced Solid Tumors [NCT01608139]Phase 10 participants (Actual)Interventional2012-11-30Withdrawn
Histone Deacetylase (HDAC) Inhibition Using Vorinostat (SAHA) After Autologous Hematopoietic Stem Cell Transplantation for High Risk Lymphoma [NCT00561418]Phase 123 participants (Actual)Interventional2007-11-30Completed
A Clinical Trial to Validate Molecular Targets of Vorinostat in Patients With Aerodigestive Tract Cancer [NCT00735826]10 participants (Actual)Interventional2009-03-31Completed
Phase I Trial of Vorinostat (SAHA) in Combination With Alvocidib (Flavopiridol) in Patients With Relapsed, Refractory, or (Selected) Poor Prognosis Acute Leukemia or Refractory Anemia With Excess Blasts-2 [NCT00278330]Phase 124 participants (Actual)Interventional2006-01-31Completed
Phase I/II Clinical Trial With Vorinostat and Infusional 5-FU/LV in Patients With Metastatic Colorectal Cancer Who Failed 5-FU-Based Chemotherapy [NCT00336141]Phase 110 participants (Actual)Interventional2006-06-30Completed
A Phase II, Multi-center, Open-label, Randomized Study of Vorinostat Plus Lenalidomide and Dexamethasone or Lenalidomide Plus Dexamethasone in Multiple Myeloma Patients Who Experience Biochemical Relapse During Lenalidomide Maintenance Therapy [NCT01501370]Phase 20 participants (Actual)Interventional2012-01-31Withdrawn
A Phase 1/2 Study of Vorinostat (Zolinza®) in Combination With Gemtuzumab Ozogamicin (Mylotarg®) and Azacitidine (Vidaza®) in Patients 50 Years of Age and Older With Relapsed/Refractory Non-APL Acute Myeloid Leukemia (AML) [NCT00895934]Phase 1/Phase 252 participants (Actual)Interventional2009-05-31Completed
A Phase I Study of Venetoclax to Augment Epigenetic Modification and Chemotherapy in Pediatric and Young Adult Patients With Relapsed and Refractory Acute Myeloid Leukemia [NCT05317403]Phase 140 participants (Anticipated)Interventional2023-03-31Recruiting
Addition of Suberoylanilide Hydroxamic Acid (Vorinostat) to Azacitidine in Patients With Higher Risk Myelodysplastic Syndromes (MDS): a Phase II add-on Study in Patients With Azacitidine Failure. [NCT01748240]Phase 221 participants (Actual)Interventional2013-03-31Terminated(stopped due to inefficiency)
Phase I Study of Vorinostat (Suberoylanilide Hydroxamic Acid, or SAHA) in Combination With Cytosine Arabinoside (Ara-C) and Etoposide for Patients With Relapsed and/or Refractory Acute Leukemias, Myelodysplasias and Myeloproliferative Disorders [NCT00357305]Phase 125 participants (Actual)Interventional2006-05-31Completed
A Pilot Study of Vorinostat to Restore Sensitivity to Aromatase Inhibitor Therapy Part B [NCT01720602]15 participants (Actual)Interventional2012-11-30Completed
Phase I/II Study of Combination of Sorafenib, Vorinostat, and Bortezomib for the Treatment of Acute Myeloid Leukemia With Complex- or Poor-risk (Monosomy 5/7) Cytogenetics or FLT3-ITD Positive Genotype [NCT01534260]Phase 1/Phase 237 participants (Actual)Interventional2012-02-10Completed
Vorinostat With 131-I MIBG Therapy for Resistant/Relapsed Neuroblastoma: A Phase I Study IND# 105,744 [NCT01019850]Phase 127 participants (Actual)Interventional2010-03-31Completed
A Phase I/II, Open-Label, Non-Randomized, Pilot Study of Weekly Paclitaxel, Every Four-week Carboplatin and Oral Vorinostat for Patients Newly Diagnosed With Stage III/IV Epithelial Ovarian, Fallopian Tube or Peritoneal Cancer [NCT00976183]Phase 1/Phase 218 participants (Actual)Interventional2009-10-31Terminated(stopped due to toxicities)
Open-Label, Multi-Center, Randomized Study of Anti-CCR4 Monoclonal Antibody KW-0761 (Mogamulizumab) Versus Vorinostat in Subjects With Previously Treated Cutaneous T-Cell Lymphoma [NCT01728805]Phase 3372 participants (Actual)Interventional2012-11-30Completed
Phase 1b/2 Study of Vorinostat in Combination With Gemcitabine and Docetaxel in Advanced Sarcoma [NCT01879085]Phase 1/Phase 237 participants (Actual)Interventional2013-09-24Completed
A Phase II Study of Vorinostat in Patients With Advanced Melanoma [NCT00121225]Phase 232 participants (Actual)Interventional2005-09-30Completed
A Phase I/II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Trastuzumab (Herceptin) in Patients With Advanced Metastatic and/or Local Chest Wall Recurrent Her-2 Amplified Breast Cancer [NCT00258349]Phase 1/Phase 216 participants (Actual)Interventional2006-08-31Completed
A Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Relapsed Non-small Cell Lung Cancer [NCT00138203]Phase 216 participants (Actual)Interventional2005-06-30Completed
Epigenetic Modification for Relapse Prevention: a Dose-finding Study of Vorinostat Used in Combination With Low-dose Azacitidine in Children Undergoing Allogeneic Hematopoietic Cell Transplantation for Myeloid Malignancies [NCT03843528]Phase 115 participants (Anticipated)Interventional2019-05-01Recruiting
A Phase I Study of the mTOR Inhibitor Temsirolimus in Combination With the HDAC Inhibitor Vorinostat in Patients With Metastatic Prostate Cancer [NCT01174199]Phase 113 participants (Actual)Interventional2012-02-29Terminated(stopped due to no value in finding efficacy)
Phase I/II Study of Bevacizumab Plus Daily Temozolomide and Vorinostat for Recurrent Malignant Glioma Patients [NCT00939991]Phase 1/Phase 248 participants (Actual)Interventional2009-10-31Completed
A Therapeutic Trial of Decitabine and Vorinostat in Combination With Chemotherapy (Vincristine, Prednisone, Doxorubicin and PEG-Asparaginase) for Relapsed/Refractory Acute Lymphoblastic Leukemia (ALL) or Lymphoblastic Lymphoma (LL) [NCT00882206]Phase 215 participants (Actual)Interventional2009-04-30Terminated(stopped due to Slow accrual)
A Phase II Investigation of Vorinostat in Combination With Intravenous Fludarabine, Mitoxantrone, and Dexamethasone in Patients With Relapsed or Refractory Mantle Cell Lymphoma [NCT01578343]Phase 220 participants (Actual)Interventional2012-06-30Terminated(stopped due to we collected data of a total of 19 patients for an interim analysis. but there are less than 7 responses out of the initial 19 patients.)
Phase II Randomised Trial of 5-azacitidine Versus 5-azacitidine in Combination With Vorinostat in Patients With Acute Myeloid Leukaemia or High Risk Myelodysplastic Syndromes Ineligible for Intensive Chemotherapy [NCT01617226]Phase 2260 participants (Actual)Interventional2012-09-30Completed
Phase I/II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With the VEGF Inhibitor Bevacizumab in Patients With Metastatic Renal Cell Carcinoma [NCT00324870]Phase 1/Phase 237 participants (Actual)Interventional2006-02-28Completed
A Randomized, Partially-Blind, Placebo-Controlled, 2-Period Crossover Study to Assess the Effects of a Single Dose of Vorinostat on the QTc Interval in Patients With Advanced Cancer [NCT00632931]Phase 125 participants (Actual)Interventional2007-07-31Completed
A Phase II Study of Vorinostat and Capecitabine in Recurrent and/or Metastatic Squamous Cell Carcinoma of Head and Neck (SCCHN) and Nasopharyngeal Carcinoma (NPC) [NCT01267240]Phase 225 participants (Actual)Interventional2010-12-31Terminated(stopped due to Study treatment did not show clinical activity.)
Lenalidomide Combined With Vorinostat/Gemcitabine/Busulfan/Melphalan With Autologous Stem-Cell Transplantation in Diffuse Large B-Cell Lymphoma of the ABC Subtype [NCT02589145]Phase 1/Phase 28 participants (Actual)Interventional2016-06-22Terminated(stopped due to Closed due to very slow accrual)
Reversing Therapy Resistance With Epigenetic-immune Modification: Phase II Trial of Vorinostat, Tamoxifen and Pembrolizumab in Hormone Receptor Expressing Advanced Breast Cancer [NCT02395627]Phase 238 participants (Actual)Interventional2015-05-04Terminated(stopped due to Insufficient efficacy in an unselected patient population)
Azacitidine/Vorinostat/GemBuMel With Autologous Stem-Cell Transplant (SCT) in Patients With Refractory Lymphomas [NCT01983969]Phase 1/Phase 261 participants (Actual)Interventional2013-11-07Completed
A Pilot Trial of Vorinostat Plus Tacrolimus and Methotrexate to Prevent Graft Versus Host Disease Following Unrelated Donor Hematopoietic Stem Cell Transplantation [NCT01789255]Phase 212 participants (Actual)Interventional2013-06-30Completed
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat) With Temsirolimus in Children With Newly Diagnosed or Progressive Diffuse Intrinsic Pontine Glioma (DIPG) [NCT02420613]Phase 118 participants (Anticipated)Interventional2015-10-05Active, not recruiting
A Phase I Study of MLN9708 and Vorinostat to Target Autophagy in Patients With Advanced p53 Mutant Malignancies [NCT02042989]Phase 168 participants (Actual)Interventional2014-06-27Completed
Phase II Study of Histone Deacetylase Inhibitor SAHA (Vorinostat) in Patients With Metastatic Thyroid Carcinoma [NCT00134043]Phase 219 participants (Actual)Interventional2005-12-31Completed
A Phase I Study of Vorinostat in Combination With Vincristine, Irinotecan, and Temozolomide in Children, Adolescents, and Young Adults With Relapsed or Refractory Solid Tumors and CNS Malignancies [NCT04308330]Phase 130 participants (Anticipated)Interventional2017-03-17Recruiting
Epigenetic Reprogramming in Relapse AML: A Phase 1 Study of Decitabine and Vorinostat Followed by Fludarabine, Cytarabine and G-CSF (FLAG) in Children and Young Adults With Relapsed/Refractory AML [NCT02412475]Phase 13 participants (Actual)Interventional2015-02-21Terminated(stopped due to We opened a competing study with the TACL consortium)
A Phase 2 Study of Vorinostat in Combination With Chemoradiation in Patients With Locally Advanced HPV Negative HNSCC [NCT05608369]Phase 264 participants (Anticipated)Interventional2023-12-01Not yet recruiting
Phase I-II Trial of Vorinostat Plus Weekly Paclitaxel (+/- Trastuzumab) Followed by Doxorubicin-cyclophosphamide in Patients With Locally Advanced Breast Cancer [NCT00574587]Phase 1/Phase 255 participants (Actual)Interventional2007-12-31Completed
Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) (NSC 701852) as Salvage Therapy in Metastatic Breast Cancer [NCT00132002]Phase 214 participants (Actual)Interventional2005-06-30Terminated(stopped due to Early termination for discouraging results)
Total Therapy XVII for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia and Lymphoma [NCT03117751]Phase 2/Phase 3790 participants (Actual)Interventional2017-03-29Active, not recruiting
Vorinostat and Carboplatin or Vorinostat and Paclitaxel in Patients With Advanced Solid Tumors: A Pharmacokinetic and Pharmacodynamic Study [NCT01281176]Phase 120 participants (Actual)Interventional2011-02-09Active, not recruiting
Phase II Study of Bevacizumab and Vorinostat for Recurrent WHO Grade IV Malignant Glioma Patients [NCT01738646]Phase 248 participants (Actual)Interventional2013-01-31Completed
Phase I/II Study of 5-azacitidine in Combination With Vorinostat in Patients With Relapsed or Refractory DLBCL [NCT01120834]Phase 1/Phase 217 participants (Actual)Interventional2010-09-30Completed
A Phase 1/2 Multi-Center Trial of Vorinostat for Graft vs Host Disease Prevention in Children, Adolescents and Young Adults Undergoing Allogeneic Blood and Marrow Transplantation [NCT03842696]Phase 1/Phase 249 participants (Anticipated)Interventional2020-02-04Recruiting
Combination Latency Reversal With High Dose Disulfiram Plus Vorinostat in HIV-infected Individuals on ART (DIVA): A Single Arm Clinical Trial [NCT03198559]Phase 1/Phase 22 participants (Actual)Interventional2017-08-08Terminated(stopped due to A re-evaluation of research risks to participants were greater than originally anticipated)
Multicenter, Open-label Phase Ib Dose-escalation and Dose-confirmational Study for the Tolerability and Safety of N-hydroxy-N'-Phenyl-octanediamide (Vorinostat) in Patients With Mild Alzheimer's Disease [NCT03056495]Phase 144 participants (Anticipated)Interventional2017-09-28Recruiting
A Phase I/II Study of Carfilzomib, Lenalidomide, Vorinostat, and Dexamethasone in Relapsed and/or Refractory Multiple Myeloma [NCT01297764]Phase 1/Phase 217 participants (Actual)Interventional2011-04-30Active, not recruiting
Phase II Basket Trial Evaluating the Efficacy of a Combination of Pembrolizumab and Vorinostat in Patients With Recurrent and/or Metastatic Squamous Cell Carcinoma [NCT04357873]Phase 2112 participants (Actual)Interventional2020-10-28Active, not recruiting
A Phase I/II Study of Vorinostat Plus Rituximab, Ifosphamide, Carboplatin, and Etoposide for Patients With Relapsed or Refractory Lymphoid Malignancies or Untreated T- or Mantle Cell Lymphoma [NCT00601718]Phase 1/Phase 229 participants (Actual)Interventional2007-12-31Completed
Phase II Trial of Bortezomib and Vorinostat in Mantle Cell and Diffuse Large B-Cell Lymphomas [NCT00703664]Phase 265 participants (Actual)Interventional2008-07-09Completed
Using Proton Magnetic Resonance Spectroscopy (MRS) to Predict Response of Vorinostat Treatment in Glioblastoma [NCT01342757]12 participants (Actual)Interventional2010-12-31Completed
A Randomized Phase III Study of Standard Cytarabine Plus Daunorubicin (7+3) Therapy or Idarubicin With High Dose Cytarabine (IA) Versus IA With Vorinostat (NSC-701852) (IA + V) in Younger Patients With Previously Untreated Acute Myeloid Leukemia (AML) [NCT01802333]Phase 3754 participants (Actual)Interventional2013-02-12Completed
Decitabine and Vorinostat With CD3/CD19 Depleted Haploidentical Donor Natural Killer (NK) Cells for the Treatment of High Risk Myelodysplastic Syndromes (MDS) [NCT01593670]Phase 29 participants (Actual)Interventional2013-03-31Completed
A Phase 1 Study of Neoadjuvant Chemotherapy, Followed by Concurrent Chemoradiation With Gemcitabine, Sorafenib, and Vorinostat in Pancreatic Cancer [NCT02349867]Phase 123 participants (Actual)Interventional2015-01-29Completed
Compassionate Use of Vorinostat (MK0683) for the Treatment of Patients With Advanced Cutaneous T-Cell Lymphoma [NCT00419367]0 participants Expanded AccessNo longer available
Pilot Trial of Vorinostat Plus Tacrolimus & Methotrexate to Prevent Graft Versus Host Disease Following Unrelated Donor Allogeneic Transplant [NCT01790568]Phase 226 participants (Actual)Interventional2014-12-31Completed
A Phase 2 Study of Vorinostat (NSC 701852) in Metastatic Uveal Melanoma [NCT01587352]Phase 240 participants (Anticipated)Interventional2012-04-20Active, not recruiting
A Phase I/Ib, Open Label, Dose Finding Study to Evaluate Safety, Pharmacodynamics and Efficacy of Pembrolizumab (MK-3475) in Combination With Vorinostat in Patients With Advanced Renal or Urothelial Cell Carcinoma [NCT02619253]Phase 153 participants (Actual)Interventional2016-02-23Completed
NANT 2011- 01: Randomized Phase II Pick the Winner Study of 131I-MIBG, 131I-MIBG With Vincristine and Irinotecan, or 131I-MIBG With Vorinostat for Resistant/Relapsed Neuroblastoma [NCT02035137]Phase 2114 participants (Actual)Interventional2014-07-31Completed
Inhibition of Autophagy in Solid Tumors: A Phase I Pharmacokinetic and Pharmacodynamic Study of Hydroxychloroquine in Combination With the HDAC Inhibitor Vorinostat for the Treatment of Patients With Advanced Solid Tumors With an Expansion Study in Advanc [NCT01023737]Phase 172 participants (Actual)Interventional2009-11-30Completed
A Phase 1/2 Study of Vorinostat [Suberoylanilide Hydroxamic Acid (SAHA)] in Combination With Azacitidine in Patients With the Myelodysplastic Syndrome (MDS) [NCT00392353]Phase 1/Phase 2135 participants (Anticipated)Interventional2006-11-22Active, not recruiting
A Phase I Trial of 5Azacitidine and Suberoylanilide Hydroxamic Acid in Patients With Metastatic or Locally Recurrent Nasopharyngeal Carcinoma and Nasal NK-T Cell Lymphoma [NCT00336063]Phase 118 participants (Actual)Interventional2006-03-03Active, not recruiting
A Phase I Study of Vorinostat (Suberoylanilide Hydroxamic Acid [SAHA]) in Combination With Temozolomide in Patients With Malignant Gliomas [NCT00268385]Phase 183 participants (Actual)Interventional2005-12-16Active, not recruiting
A Pilot Study of Decitabine and Vorinostat With Chemotherapy for Relapsed ALL [NCT01483690]Phase 1/Phase 223 participants (Actual)Interventional2011-12-31Terminated(stopped due to Toxicity)
HDAC Inhibitor Augmentation to Clozapine [NCT03263533]Early Phase 10 participants (Actual)Interventional2017-04-30Withdrawn(stopped due to PIs were unable to recruit any participants)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00106626 (2) [back to overview]Safety and Tolerability as Measured by the Number of Participants With Disease Progression
NCT00106626 (2) [back to overview]Maximum Tolerated Dose (MTD) Status as Determined by Number of Participants With Dose Limiting Toxicity (DLT) at Each Dose Level
NCT00111813 (5) [back to overview]Number of Participants With Dose Modifications of Either Vorinostat or Bortezomib Due to Adverse Experiences (AEs) After Treatment With Study Drug
NCT00111813 (5) [back to overview]Mean Duration of Treatment With Vorinostat
NCT00111813 (5) [back to overview]Laboratory AE Summary
NCT00111813 (5) [back to overview]Clinical AE Summary
NCT00111813 (5) [back to overview]Mean Time to First AE Resulting in a Dose Modification in Either Vorinostat or Bortezomib
NCT00121225 (5) [back to overview]Objective Response Rate Assessed by Response Evaluation Criteria for Solid Tumors (RECIST)
NCT00121225 (5) [back to overview]Comparison of VEGF Serum Levels to Response to Vorinostat
NCT00121225 (5) [back to overview]Time to Progression Assessed by RECIST
NCT00121225 (5) [back to overview]Difference in HP1 and MacroH2A Nuclear Foci Expression Between Progressive Minus Stable Disease Outcomes
NCT00121225 (5) [back to overview]Number of Patients With p53 Allelic Variations (72R or 72P)
NCT00127101 (2) [back to overview]Number of Participants Who Responded to Treatment
NCT00127101 (2) [back to overview]Maximum Tolerated Dose (MTD) as Determined by the Number of Participants With Dose Limiting Toxicities
NCT00127127 (15) [back to overview]Cmax of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration
NCT00127127 (15) [back to overview]Cmax of Vorinostat After a Single Oral Dose in a Fed State
NCT00127127 (15) [back to overview]Maximum Concentration (Cmax) of Vorinostat After a Single Oral Dose in a Fasted State
NCT00127127 (15) [back to overview]Number of Participants Who Discontinued Study Treatment Due to an Adverse Event
NCT00127127 (15) [back to overview]Number of Participants Who Experienced One or More Adverse Events
NCT00127127 (15) [back to overview]Number of Participants With a Dose-Limiting Toxicity (DLT) During Cycle 1
NCT00127127 (15) [back to overview]t½ of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration
NCT00127127 (15) [back to overview]t½ of Vorinostat After a Single Oral Dose in a Fed State
NCT00127127 (15) [back to overview]Time to Maximum Concentration (Tmax) of Vorinostat After a Single Oral Dose in a Fasted State
NCT00127127 (15) [back to overview]Tmax of Vorinostat After a Single Oral Dose in a Fed State
NCT00127127 (15) [back to overview]AUC0-inf of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration
NCT00127127 (15) [back to overview]Apparent Terminal Half-Life (t½) of Vorinostat After a Single Oral Dose in a Fasted State
NCT00127127 (15) [back to overview]Area Under the Plasma Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of Vorinostat After a Single Oral Dose in a Fasted State
NCT00127127 (15) [back to overview]Tmax of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration
NCT00127127 (15) [back to overview]AUC0-Inf of Vorinostat After a Single Oral Dose in a Fed State
NCT00128102 (10) [back to overview]Number of Participants Who Experienced Adverse Events (AEs) Characterized as Grade 3 or Grade 4 According to the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE)
NCT00128102 (10) [back to overview]Percentage of Participants With ≥10% Change From Baseline in FVC at Week 12
NCT00128102 (10) [back to overview]Progression Free Survival (PFS)
NCT00128102 (10) [back to overview]Number of Participants Who Discontinued Study Treatment Due to an AE
NCT00128102 (10) [back to overview]Percentage of Participants With ≥50% Change Together With a >10 mm Change From Baseline in the LCSS-Meso Dyspnea Score at Week 12
NCT00128102 (10) [back to overview]Number of Participants Who Experienced an AE
NCT00128102 (10) [back to overview]Objective Response Rate (ORR)
NCT00128102 (10) [back to overview]Overall Survival (OS)
NCT00128102 (10) [back to overview]Percent Change From Baseline in Forced Vital Capacity (FVC) at Week 12
NCT00128102 (10) [back to overview]Percent Change From Baseline in Lung Cancer Symptom Scale, Modified for Mesothelioma (LCSS-Meso) Dyspnea Score at Week 12
NCT00132002 (3) [back to overview]Objective Tumor Response Rate
NCT00132002 (3) [back to overview]Overall Survival
NCT00132002 (3) [back to overview]Progression-free Survival
NCT00132028 (3) [back to overview]Assess Number of Patients Who Achieve Confirmed and Unconfirmed Complete Response (CR) or Partial Response (PR)
NCT00132028 (3) [back to overview]Progression-Free Survival
NCT00132028 (3) [back to overview]Overall Survival
NCT00134043 (1) [back to overview]Objective Response Rate (PR + CR) Using RECIST/WHO Response Criteria
NCT00138203 (4) [back to overview]Toxicity
NCT00138203 (4) [back to overview]Response Per RECIST Criteria
NCT00138203 (4) [back to overview]Overall Survial
NCT00138203 (4) [back to overview]Time to Progression
NCT00238303 (4) [back to overview]Survival
NCT00238303 (4) [back to overview]Time to Progression
NCT00238303 (4) [back to overview]Confirmed Tumor Response
NCT00238303 (4) [back to overview]Proportion of Successes (Patients Alive and Progression-free)
NCT00251589 (8) [back to overview]Stable Disease (SD) as Best Response Based on Response Criteria in Solid Tumors (RECIST)
NCT00251589 (8) [back to overview]Disease Progression After Week 8 Based on Response Criteria in Solid Tumors (RECIST)
NCT00251589 (8) [back to overview]Dose Limiting Toxicity (DLT) Occurring in Cycle 1 of the Phase I Portion of the Study
NCT00251589 (8) [back to overview]Dose Limiting Toxicity Occurring in Cycle 1 of the Phase II Portion of the Study
NCT00251589 (8) [back to overview]Dose Limiting Toxicity Occurring in Cycles 2 and Beyond of the Phase II Portion of the Study
NCT00251589 (8) [back to overview]Progression-free Survival
NCT00251589 (8) [back to overview]Progressive Disease (PD) as Best Response Based on Response Criteria in Solid Tumors (RECIST)
NCT00251589 (8) [back to overview]Unconfirmed Partial Response (UPR) Based on Response Criteria in Solid Tumors (RECIST)
NCT00253630 (4) [back to overview]2-Year Overall Survival
NCT00253630 (4) [back to overview]2-Year Progression Free-Survival
NCT00253630 (4) [back to overview]Response Rate
NCT00253630 (4) [back to overview]Number of Participants With Adverse Events
NCT00258349 (3) [back to overview]Response Rate
NCT00258349 (3) [back to overview]Time to Progression
NCT00258349 (3) [back to overview]Overall Survival
NCT00262834 (4) [back to overview]Change in Tissue Apoptosis After 3 Days of Treatment
NCT00262834 (4) [back to overview]Change in Tissue Histone Acetylation After 3 Days of Treatment
NCT00262834 (4) [back to overview]Change in Tissue Proliferation After 3 Days of Treatment
NCT00262834 (4) [back to overview]Number of Participants With Adverse Events
NCT00278395 (1) [back to overview]Objective Response
NCT00305773 (4) [back to overview]Time to Treatment Failure (TTF)
NCT00305773 (4) [back to overview]Overall Survival (OS)
NCT00305773 (4) [back to overview]Number of Participants With Severe (Grade 3, 4 or 5) Adverse Events
NCT00305773 (4) [back to overview]Confirmed Complete Response (CR) Rate
NCT00324740 (2) [back to overview]Number of Participants With at Least One Dose Limiting Toxicity Associated With Vorinostat Concurrently Administered With Isotretinoin
NCT00324740 (2) [back to overview]Maximum Tolerated Dose of Vorinostat in Combination With Isotretinoin
NCT00324870 (1) [back to overview]Progression-free Survival Assessed by Response Evaluation Criteria for Solid Tumors (RECIST) (Phase II)
NCT00330161 (4) [back to overview]Objective Response Rate
NCT00330161 (4) [back to overview]Median Survival
NCT00330161 (4) [back to overview]Progression-free Survival
NCT00330161 (4) [back to overview]Incidence of Toxicity
NCT00363883 (3) [back to overview]Objective Tumor Response Rate
NCT00363883 (3) [back to overview]Progression-free Survial
NCT00363883 (3) [back to overview]Overall Survival
NCT00365599 (3) [back to overview]Number of Participants With Objective Response (OR)
NCT00365599 (3) [back to overview]Number of Participants With Serious Adverse Events (SAEs)
NCT00365599 (3) [back to overview]Time to Progression (TTP)
NCT00368875 (4) [back to overview]Overall Survival(OS)
NCT00368875 (4) [back to overview]Progression-free Survival (PFS),
NCT00368875 (4) [back to overview]Recommended Phase II Dose as Assessed by NCI Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0 (Phase I)
NCT00368875 (4) [back to overview]Objective Response Rate (CR + PR)
NCT00373490 (7) [back to overview]Area Under the Curve (AUC(0-infinity) at Day 21 (400 mg)
NCT00373490 (7) [back to overview]Maximum Concentration (Cmax) at Day 21 (400 mg)
NCT00373490 (7) [back to overview]Maximum Concentration (Cmax) at Day 1 (600 mg and 400 mg)
NCT00373490 (7) [back to overview]Area Under the Curve (AUC(0-infinity)) at Day 3 (600 mg)
NCT00373490 (7) [back to overview]Area Under the Curve (AUC(0-infinity)) at Day 1 (600 mg and 400 mg)
NCT00373490 (7) [back to overview]Number of Participants With a Dose Limiting Toxicity (DLT)
NCT00373490 (7) [back to overview]Maximum Concentration (Cmax) at Day 3 (600 mg)
NCT00423449 (4) [back to overview]Maximum Tolerated Dose of Vorinostat Administered in Combination With Standard Doses of Gemcitabine Plus Either Cisplatin or Carboplatin in Patients With Advanced Stage Non-Small Cell Lung Cancer Who Have Not Received Chemotherapy for Advanced Disease
NCT00423449 (4) [back to overview]Number of Participants With Dose-limiting Toxicities (DLT) Due to Vorinostat Administered in Combination With Standard Dose of Gemcitabine Plus Either Cisplatin or Carboplatin
NCT00423449 (4) [back to overview]Number of Participants With Laboratory Adverse Experiences (Safety and Tolerability)
NCT00423449 (4) [back to overview]Number of Participants With Clinical Adverse Experiences (Safety and Tolerability)
NCT00424775 (5) [back to overview]Number of Participants With a Dose Limited Toxicity at First Cycle
NCT00424775 (5) [back to overview]Area Under the Curve (AUC(0-24 hr)) at Day 4
NCT00424775 (5) [back to overview]Area Under the Curve (AUC(0-24 hr)) at Day 5
NCT00424775 (5) [back to overview]Maximum Concentration (Cmax) at Day 4
NCT00424775 (5) [back to overview]Maximum Concentration (Cmax) at Day 5
NCT00473889 (3) [back to overview]Overall Survival
NCT00473889 (3) [back to overview]Progression Free Survival
NCT00473889 (3) [back to overview]Number of Participants Who Had a Disease Response to Treatment
NCT00479232 (3) [back to overview]Number of Participants Experiencing Dose Limiting Toxicity (DLT) Events
NCT00479232 (3) [back to overview]Objective Response Rate in Participants Treated With Vorinostat + Decitabine With Intermediate-high Risk Myelodysplastic Syndrome (MDS) or Untreated Acute Myelogenous Leukemia (AML)
NCT00479232 (3) [back to overview]Objective Response Rate in Participants Treated With Vorinostat + Decitabine With Refractory or Relapse Acute Myelogenous Leukemia (AML)
NCT00481078 (3) [back to overview]Response Rate
NCT00481078 (3) [back to overview]Progression-free Survival
NCT00481078 (3) [back to overview]Overall Survival
NCT00486720 (2) [back to overview]Number of Responders and Number of Non-responders Defined by International Working Group Response Criteria
NCT00486720 (2) [back to overview]Safety and Tolerability as Assessed by the Number of Participants With Adverse Events.
NCT00561418 (3) [back to overview]Duration of Response
NCT00561418 (3) [back to overview]Clinical Benefit
NCT00561418 (3) [back to overview]Safety and Tolerability of Vorinostat (SAHA) After Autologous Stem Cell Transplantation
NCT00574587 (2) [back to overview]Pathological Complete Response (CR) Rate in Patients With Her2/Neu Positive Locally Advanced Breast Cancer.
NCT00574587 (2) [back to overview]Recommended Phase II Dose of Vorinostat in Combination With Weekly Paclitaxel/Trastuzumab
NCT00589472 (6) [back to overview]Levels of Testosterone in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]Levels of PSA in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]Levels of DHT in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]Gleason Score
NCT00589472 (6) [back to overview]Levels of DHEA in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]Levels of DHEA-S in Blood From Radical Prostatectomy Specimens
NCT00601718 (4) [back to overview]Efficacy (Response Rate) of Vorinostat Combined With RICE Chemotherapy
NCT00601718 (4) [back to overview]Ability to Proceed to Peripheral Blood Stem Cell Collection Following Treatment
NCT00601718 (4) [back to overview]Maximum Tolerated Dose of Vorinostat
NCT00601718 (4) [back to overview]Safety and Toxicity According to CTCAE v3.0
NCT00616967 (8) [back to overview]Change in Standard Uptake Value (SULmax) From Baseline to Day 15 on FDG-PET
NCT00616967 (8) [back to overview]Cumulative Methylation Index (CMI) at Day 15
NCT00616967 (8) [back to overview]Number of Participants Who Experience Death During Treatment
NCT00616967 (8) [back to overview]Number of Participants With Clinical Complete Response (cCR)
NCT00616967 (8) [back to overview]Safety as Measured by Number of Participants Who Experience Adverse Events
NCT00616967 (8) [back to overview]Change in Cumulative Methylation Index (CMI)
NCT00616967 (8) [back to overview]Pathological Complete Response (pCR) Rate
NCT00616967 (8) [back to overview]Absolute Change From Baseline in Ki-67
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 1 Hour
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 0.5 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 12 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 2 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 3 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 4 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 8 Hours
NCT00632931 (8) [back to overview]Change From Baseline in QTcF at 24 Hours
NCT00641706 (4) [back to overview]Overall Survival
NCT00641706 (4) [back to overview]Proportion of Confirmed Tumor Response Defined as an Objective Status of Confirmed Response (CR), Partial Response (PR), or Regression (REGR) on Two Consecutive Evaluations
NCT00641706 (4) [back to overview]Time to Progression
NCT00641706 (4) [back to overview]Progression-free Survival at 6 Months
NCT00642954 (3) [back to overview]Number of Participants Experiencing Dose-Limiting Toxicities (DLTs)
NCT00642954 (3) [back to overview]Number of Participants Experiencing Drug-Related Adverse Events (AEs)
NCT00642954 (3) [back to overview]Number of Participants Experiencing Best Overall Response Determined by Complete Response (CR), Near Complete Response (NCR), Very Good Partial Response (VGPR), Partial Response (PR), Minimal Response (MR), Stable Disease (SD) or Progressive Disease (PD)
NCT00656617 (2) [back to overview]Progression Free Survival (PFS) at 7 Months
NCT00656617 (2) [back to overview]Participant Response
NCT00662311 (6) [back to overview]Radiological Response Rate as Assessed by CT
NCT00662311 (6) [back to overview]Safety and Toxicity of Vorinostat at the MTD as Assessed by NCI CTCAE Version 3.0
NCT00662311 (6) [back to overview]Progression-free Survival
NCT00662311 (6) [back to overview]MTD of Vorinostat When Administered in Combination With Paclitaxel and Radiotherapy Therapy as Assessed by NCI Common Toxicity Criteria for Adverse Events (CTCAE) Version 3.0 (Phase I)
NCT00662311 (6) [back to overview]Overall Survival
NCT00662311 (6) [back to overview]Duration of Response
NCT00667615 (2) [back to overview]Complete Response Rate to Rituximab and a Combination of Vorinostat With Cyclophosphamide, Etoposide, and Prednisone in Elderly Pts With Relapsed Diffuse Large B-cell Lymphoma Who Aren't Candidates for Autologous Stem Cell Transplantation.
NCT00667615 (2) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat Given Orally for 10 Days in Combination With Cyclophosphamide, Etoposide, Prednisone and Rituximab for Elderly Patients With Relapsed Diffuse Large B-cell Lymphoma
NCT00673153 (5) [back to overview]Number of Participants Alive at Day 30 (Poor-risk Group)
NCT00673153 (5) [back to overview]Relapse-free Survival (Good- and Poor-risk Group)
NCT00673153 (5) [back to overview]Number of Participants Achieving CR or CRi With Induction Therapy (Good-risk Group)
NCT00673153 (5) [back to overview]Number of Participants Achieving CR or CRi With Induction Therapy (Poor-risk Group)
NCT00673153 (5) [back to overview]Number of Participants Alive at Day 30 (Good-risk Group)
NCT00691210 (2) [back to overview]The Maximum Tolerated Dose (MTD) of Niacinamide in the Combination of Vorinostat and Niacinamide
NCT00691210 (2) [back to overview]The Greatest Number of Cycles Received in Each Treatment Group
NCT00703664 (5) [back to overview]Best Response
NCT00703664 (5) [back to overview]Progression-free Survival (PFS)
NCT00703664 (5) [back to overview]Duration of Partial Response
NCT00703664 (5) [back to overview]Duration of Stable Disease
NCT00703664 (5) [back to overview]Overall Response Rate (ORR)
NCT00720876 (3) [back to overview]Overall Response Rate (Complete and Partial Response)
NCT00720876 (3) [back to overview]Progression-free Survival
NCT00720876 (3) [back to overview]Number of Participants With Grade 3 and 4 Toxicities
NCT00731731 (5) [back to overview]Maximum Tolerated Dose of Vorinostat, Defined as the Dose at Which Fewer Than One-third of Patients Experience DLTs, Graded According to NCI CTCAE (Common Toxicity Criteria for Adverse Effects) Version 3.0 (Phase I)
NCT00731731 (5) [back to overview]Time to Tumor Progression (Phase II)
NCT00731731 (5) [back to overview]Incidence of Adverse Events, as Per NCI CTCAE Version 3.0 (Phase II)
NCT00731731 (5) [back to overview]Incidence of Adverse Events, Based on CTC (Common Toxicity Criteria) Severity Grade
NCT00731731 (5) [back to overview]Overall Survival at 15 Months (Phase II)
NCT00735826 (3) [back to overview]Concentration of Vorinostat in Tumor Tissue
NCT00735826 (3) [back to overview]Changes in Tumor Markers on Tumors of the Lung, Esophagus, or Head and Neck, After 7 Days of Treatment With Vorinostat
NCT00735826 (3) [back to overview]Effects of Vorinostat Treatment on Induction of Apoptosis or Necrosis in Treated vs. Untreated Tumors
NCT00764517 (5) [back to overview]Event-free Survival
NCT00764517 (5) [back to overview]Objective Response Rate
NCT00764517 (5) [back to overview]Progression-free Survival
NCT00764517 (5) [back to overview]Tolerability of Treatment
NCT00764517 (5) [back to overview]Toxicities as Assessed Using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) Version 4.0
NCT00771472 (6) [back to overview]Part I: Number of Participants Experiencing Dose Limiting Toxicity (DLT)
NCT00771472 (6) [back to overview]Part I: Maximum Drug Concentration (Cmax)
NCT00771472 (6) [back to overview]Part I: The Amount of Time it Takes for the Drug Concentration to Decrease by Half (T1/2)
NCT00771472 (6) [back to overview]Part I: Total Drug Exposure (Area Under the Concentration Curve, AUC[0-24 Hours])
NCT00771472 (6) [back to overview]Part I: Time at Which Cmax Occurs (Tmax)
NCT00771472 (6) [back to overview]Parts I & II: Number of Participants Experiencing Clinical or Laboratory Adverse Experiences (AE)
NCT00773747 (5) [back to overview]Objective Response Rate
NCT00773747 (5) [back to overview]Overall Survival
NCT00773747 (5) [back to overview]Progression-Free Survival (PFS)
NCT00773747 (5) [back to overview]Time to Progression
NCT00773747 (5) [back to overview]Number of Participants With Grade 3-5 Clinical or Laboratory Adverse Events (AEs)
NCT00773838 (8) [back to overview]Overall Survival (OS)
NCT00773838 (8) [back to overview]Time To Disease Progression (TTP) as Determined by IAC Per EBMT Criteria
NCT00773838 (8) [back to overview]Objective Response Rate (RR)
NCT00773838 (8) [back to overview]Number of Participants Who Discontinued Study Treatment Due to an AE
NCT00773838 (8) [back to overview]Number of Participants Who Experienced an Adverse Event (AE)
NCT00773838 (8) [back to overview]TTP as Assessed by Investigator Per EBMT Criteria
NCT00773838 (8) [back to overview]Progression-Free Survival (PFS) as Determined by IAC Per EBMT Criteria
NCT00773838 (8) [back to overview]PFS as Assessed by Investigator Per EBMT Criteria
NCT00785798 (2) [back to overview]Number of Subjects With Progressive Disease (PR)
NCT00785798 (2) [back to overview]Overall Response Rate
NCT00787527 (3) [back to overview]Number of Participants With Dose Limiting Toxicity for Determination Phase I (Schedule A) MTD of Vorinostat
NCT00787527 (3) [back to overview]Phase I Maximum Tolerated Dose (MTD) of Vorinostat
NCT00787527 (3) [back to overview]Phase II MTD of Vorinostat
NCT00798720 (4) [back to overview]Toxicity
NCT00798720 (4) [back to overview]Median Overall Survival
NCT00798720 (4) [back to overview]Three-month Progression-free Survival
NCT00798720 (4) [back to overview]Response Rate
NCT00810576 (1) [back to overview]Number of Patients With Response
NCT00810602 (4) [back to overview]Percent Survival at 2-years
NCT00810602 (4) [back to overview]100-day Cumulative Incidence of Grade 2-4 Acute Graft Versus Host Disease (GVHD)
NCT00810602 (4) [back to overview]Number of Serious Adverse Events
NCT00810602 (4) [back to overview]Percent Cumulative Incidence of Relapse at 2 Years.
NCT00818649 (1) [back to overview]Number of Patients by Best Clinical Response
NCT00821951 (1) [back to overview]The Primary Endpoint of the Study is to Establish the Maximum Tolerated Dose of Vorinostat When Given Concurrently With Palliative Radiation.
NCT00831493 (1) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat + Chemoradiation
NCT00838929 (1) [back to overview]Maximum Tolerated Dose (MTD) and Recommended Phase II Dose (RP2D) of Vorinostat and Radiotherapy in Patients With Brain Metastases.
NCT00839956 (4) [back to overview]Toxicity as Assessed by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) v3.0
NCT00839956 (4) [back to overview]Median Follow-up Survival for All Patients
NCT00839956 (4) [back to overview]Survival for All Patients
NCT00839956 (4) [back to overview]Time to Disease Progression in Patients Who Progressed
NCT00858234 (3) [back to overview]Number of Participants With an Adverse Event (AE)
NCT00858234 (3) [back to overview]Number of Participants With Dose-Limiting Toxicity (DLT) During Cycle 1
NCT00858234 (3) [back to overview]Area Under the Plasma Concentration-Time Curve From 0 to 24 Hours Postdose (AUC0-24hr) of Vorinostat Administered With Bortezomib on Days 1 and 11
NCT00875056 (5) [back to overview]Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event (AE)
NCT00875056 (5) [back to overview]Number of Participants Who Experienced an Adverse Event (AE)
NCT00875056 (5) [back to overview]Objective Response Rate (ORR)
NCT00875056 (5) [back to overview]Time to Response for Relapsed/Refractory FL
NCT00875056 (5) [back to overview]Time to Treatment Failure for Relapsed/Refractory FL
NCT00882206 (4) [back to overview]Level of Methylation
NCT00882206 (4) [back to overview]Response to Treatment
NCT00882206 (4) [back to overview]Level of Methylation
NCT00882206 (4) [back to overview]Level of Methylation
NCT00895934 (4) [back to overview]Number of Participants With Dose-limiting Toxicity (Phase I)
NCT00895934 (4) [back to overview]Number of Participants With Dose-limiting Toxicity After the Vorinostat Dose
NCT00895934 (4) [back to overview]Disease Relapse
NCT00895934 (4) [back to overview]Number of Participants With Complete Remission
NCT00907738 (1) [back to overview]Percent of Participants With a Serious Drug-related Adverse Event (AE)
NCT00910000 (3) [back to overview]Vorinostat Maximum Tolerated Dose (MTD) [Phase Ib]
NCT00910000 (3) [back to overview]Response
NCT00910000 (3) [back to overview]Dose Limiting Toxicity (DLT) [Phase Ib]
NCT00918723 (4) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat That Can be Combined With Fludarabine Phosphate, Cyclophosphamide and Rituximab (FCR) (Phase I)
NCT00918723 (4) [back to overview]Overall Survival
NCT00918723 (4) [back to overview]Percentage of Patients With Progression-free Survival at 2 Years
NCT00918723 (4) [back to overview]To Estimate the Rate of Conversion of Partial Response (PR) to Complete Response (CR) After Fludarabine, Cyclophosphamide and Rituximab (FCR) Plus Vorinostat
NCT00937495 (3) [back to overview]Overall Survival
NCT00937495 (3) [back to overview]Progression Free Survival
NCT00937495 (3) [back to overview]Confirmed Tumor Responses
NCT00939991 (6) [back to overview]Phase II: Radiographic Response.
NCT00939991 (6) [back to overview]Phase I: Determination of the Maximum Tolerated Dose (MTD)
NCT00939991 (6) [back to overview]Phase II: 6-month Progression-free Survival (PFS)
NCT00939991 (6) [back to overview]Phase II: Median Overall Survival (OS)
NCT00939991 (6) [back to overview]Phase II: Median Progression-free Survival (PFS)
NCT00939991 (6) [back to overview]Phase II: Number of Patients With Grade 2 or Greater, Treatment-related Toxicities
NCT00942266 (7) [back to overview]Overall Survival
NCT00942266 (7) [back to overview]Response Rate
NCT00942266 (7) [back to overview]Disease Control Rate (Stable Disease or Objective Response)
NCT00942266 (7) [back to overview]Fluorouracil Steady-state Pharmacokinetics
NCT00942266 (7) [back to overview]Vorinostat Pharmacokinetics
NCT00942266 (7) [back to overview]Median Progression-free Survival
NCT00942266 (7) [back to overview]Toxicity
NCT00948064 (3) [back to overview]Survival at Day 60
NCT00948064 (3) [back to overview]Survival at Day 60
NCT00948064 (3) [back to overview]Response Rate
NCT00948688 (7) [back to overview]Progression Free Survival (PFS) at 7 Months From Registration
NCT00948688 (7) [back to overview]Progression Free Survival
NCT00948688 (7) [back to overview]Overall Survival
NCT00948688 (7) [back to overview]Number of Participants Experiencing Unacceptable Toxicity
NCT00948688 (7) [back to overview]Maximally Tolerated Dose (MTD) of Vorinostat in Combination With Infusional 5-FU and Radiation Therapy.
NCT00948688 (7) [back to overview]Resectability Rate
NCT00948688 (7) [back to overview]Response Rate
NCT00958074 (5) [back to overview]Changes in the Physicians Serial Assessment of Erythroderma Score
NCT00958074 (5) [back to overview]Objective Response
NCT00958074 (5) [back to overview]Objective Response Rate of Extracutaneous Manifestations of CTCL (Lymph Node Enlargement, Sezary Cells in Peripheral Blood);
NCT00958074 (5) [back to overview]Number of Participants With Overall Response as Measured by Sezary Cell Count
NCT00958074 (5) [back to overview]Occurrences of Dose Adjustment as Measured by Safety/Toxicity
NCT00972478 (5) [back to overview]Overall Survival (Phase II)
NCT00972478 (5) [back to overview]Toxicity of Vorinostat-R-CHOP in Patients With Newly Diagnosed DLBCL
NCT00972478 (5) [back to overview]Safe Dose of Vorinostat to be Used in Combination With R-CHOP Assessed by CTCAE Version 4.0 (Phase I)
NCT00972478 (5) [back to overview]Response Rate (Complete Response [CR]+Partial Response [PR]) (Phase II)
NCT00972478 (5) [back to overview]Progression-free Survival (Phase II)
NCT00976183 (2) [back to overview]Objective Response Rate
NCT00976183 (2) [back to overview]Number of Participants With Progression Free Survival (PFS) up to 24 Months
NCT00992446 (4) [back to overview]Toxicity of Vorinostat Bortezomib Maintenance Therapy After Autologous Transplant
NCT00992446 (4) [back to overview]Median Time to Disease Progression
NCT00992446 (4) [back to overview]Event-free Survival
NCT00992446 (4) [back to overview]Overall Survival
NCT01000155 (3) [back to overview]γ-globin to β-globin Ratio
NCT01000155 (3) [back to overview]Percent Fetal Hemoglobin (HbF%) Induction Success Rate
NCT01000155 (3) [back to overview]F-Cell Percentage Level
NCT01110876 (1) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat in Combination With Escalating Doses of Erlotinib and Temozolomide
NCT01118975 (2) [back to overview]Clinical Benefit Rate
NCT01118975 (2) [back to overview]Dose Limiting Toxicities
NCT01120834 (1) [back to overview]Overall Response Rate (ORR)
NCT01153672 (5) [back to overview]Overall Survival
NCT01153672 (5) [back to overview]Rate of Clinical Benefit According to RECIST
NCT01153672 (5) [back to overview]Progression-free Survival
NCT01153672 (5) [back to overview]Percentage of Patients That Experience Adverse Events as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0
NCT01153672 (5) [back to overview]Duration of Response
NCT01169532 (3) [back to overview]Maximum Tolerated Dose (MTD)
NCT01169532 (3) [back to overview]Progression Free Survival
NCT01169532 (3) [back to overview]Overall Survival
NCT01175980 (11) [back to overview]Response Duration (RD)
NCT01175980 (11) [back to overview]Stable Disease Duration (SDD)
NCT01175980 (11) [back to overview]The Number of Genes Sequenced in the WES Assay as a Measure of the Whole Exome Profile of the Sorted Tumor Population and Matching Germ Line Sample
NCT01175980 (11) [back to overview]Time to Recurrence (TTR)
NCT01175980 (11) [back to overview]Unique Probes on the Oligonucleotide CGH Array as a Measure of the Genomic Profile of Each Cell Population.
NCT01175980 (11) [back to overview]Number of Participants With Grade 3 or Grade 4 Toxicity as Assessed by the Common Terminology Criteria for Adverse Events Version 4.0
NCT01175980 (11) [back to overview]Progression-free Survival (PFS)
NCT01175980 (11) [back to overview]Number of Patients With Flow Sort Aneuploid Populations of Tumor Cells From FFPE Tissue
NCT01175980 (11) [back to overview]Number of Patients With Flow Sort Diploid Populations of Tumor Cells From FFPE Tissue Blocks
NCT01175980 (11) [back to overview]Number of Patients With Flow Sort Tetraploid Populations of Tumor Cells From FFPE Tissue
NCT01175980 (11) [back to overview]Overall Survival (OS)
NCT01187446 (4) [back to overview]Complete Clinical Response (CCR)
NCT01187446 (4) [back to overview]Duration of Clinical Benefit (Per Protocol Follow-up)
NCT01187446 (4) [back to overview]Duration of Clinical Benefit (Supplemental Follow-up)
NCT01187446 (4) [back to overview]Safety and Tolerability as Measured by Severity and Frequency of Adverse Events
NCT01189266 (5) [back to overview]Overall Survival
NCT01189266 (5) [back to overview]Incidence of Toxicity During Maintenance Therapy
NCT01189266 (5) [back to overview]Incidence of Toxicity During Chemoradiation Therapy
NCT01189266 (5) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat
NCT01189266 (5) [back to overview]Event-Free Survival
NCT01193842 (14) [back to overview]Changes in Epstein-Barr Virus (EBV) Viral Load
NCT01193842 (14) [back to overview]Changes in Human Herpes Virus (HHV)-8 Viral Load
NCT01193842 (14) [back to overview]Changes in Human Herpes Virus (HHV)-8 Viral Load
NCT01193842 (14) [back to overview]Changes in Human Immunodeficiency Virus (HIV) Viral Load
NCT01193842 (14) [back to overview]Percentage of Participant Experiencing Adverse Events (AEs) for Each Treatment Arm as Assessed by Common Terminology Criteria for Adverse Events Version 4.0 (CTCAE v4.0) (Phase II)
NCT01193842 (14) [back to overview]Tumor Response (Phase I)
NCT01193842 (14) [back to overview]Event-free Survival (EFS) (Phase II)
NCT01193842 (14) [back to overview]Overall Survival (OS) (Phase II)
NCT01193842 (14) [back to overview]Percentage of Participants With Complete Response (CR) as Assessed by Response Evaluation Criteria in Solid Tumors (Phase II)
NCT01193842 (14) [back to overview]Recommended Phase II Dose of Vorinostat Determined According to Dose-limiting Toxicities Graded Using Common Terminology Criteria for Adverse Events Version 4.0 (CTCAE v4.0) (Phase I)
NCT01193842 (14) [back to overview]Change in CD8 Cell Counts (Phase I)
NCT01193842 (14) [back to overview]Change in Plasma Associated Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) (Phase I)
NCT01193842 (14) [back to overview]Pharmacokinetic Clearance (Phase I)
NCT01193842 (14) [back to overview]Changes in Absolute CD4 Cell Counts (Phase I)
NCT01236560 (4) [back to overview]Cumulative Incidence of Disease Progression in Each Treatment Arm
NCT01236560 (4) [back to overview]Overall Survival
NCT01236560 (4) [back to overview]Maximum Tolerated Dose (MTD) of Vorinostat
NCT01236560 (4) [back to overview]Event-free Survival
NCT01266031 (8) [back to overview]Time to Progression (TTP)
NCT01266031 (8) [back to overview]Maximum Tolerated Dose (MTD) of Oral Vorinostat Used With Bevacizumab
NCT01266031 (8) [back to overview]Number of Participants With Serious and Non-Serious Adverse Events
NCT01266031 (8) [back to overview]Overall Survival (OS)
NCT01266031 (8) [back to overview]Mean Symptom Severity Using the MD Anderson Symptom Inventory-Brain Tumor Module (MDASI-BT) Self Reporting Tool
NCT01266031 (8) [back to overview]Percentage of Patients Rating Their Symptoms to be 7 or Greater on a 0-10 Scale Using the Mean Severity of the MD Anderson Symptom Inventory-Brain Tumor Module (MDSAI-BT) Self Reporting Tool
NCT01266031 (8) [back to overview]Mean Symptom Interference at the Time of Clinical Evaluation
NCT01266031 (8) [back to overview]Progression Free Survival (PFS) at 6 Months
NCT01267240 (3) [back to overview]Response Rate According to Response Evaluation Criteria in Solid Tumors
NCT01267240 (3) [back to overview]Progression-free Survival
NCT01267240 (3) [back to overview]Survival
NCT01312818 (2) [back to overview]Number of Subjects Who Achieved Complete Remission of Their Disease
NCT01312818 (2) [back to overview]Number of Subjects Experiencing Drug Related Adverse Events
NCT01319383 (8) [back to overview]Number of Participants Exhibiting an in Vivo Resting CD4+ T Cell- Associated HIV RNA (RCVL) Increase After Receiving a Single Dose of VOR 400 mg PO
NCT01319383 (8) [back to overview]Number of Participants Developing Cancer Within 5 Years Following >/= 8 Vorinostat Dose Exposures
NCT01319383 (8) [back to overview]Number of Participants With Measurable Changes in Plasma HIV-1 RNA
NCT01319383 (8) [back to overview]Number of Participants With Confirmed Non-hematologic Toxicity >/= Grade 3 and Related to VOR Per Division of AIDS (DAIDS) Grading Table
NCT01319383 (8) [back to overview]Number of Participants With Confirmed Hematologic Toxicity >/= Grade 2 and Related to VOR Per Division of AIDS (DAIDS) Grading Table
NCT01319383 (8) [back to overview]Number of Participants With a Significant in Vivo Response in Resting Cell Infection (RCI) and HIV RNA After Paired Doses
NCT01319383 (8) [back to overview]Number of Participants Exhibiting an in Vivo Resting CD4+ T-cell-associated HIV RNA (Rc-RNA) Increase Following Multiple (n = 10) Interval Doses
NCT01319383 (8) [back to overview]Number of Participants Exhibiting an in Vivo Resting CD4+ T-cell-associated HIV RNA (Rc-RNA) Increase Following Each of Two Multiple Dose Cycles (11 Doses/Cycle)
NCT01342757 (3) [back to overview]Mean Change in Metabolite Levels
NCT01342757 (3) [back to overview]Measurable Change on Magnetic Resonance Spectroscopy Imaging After Vorinostat Administration
NCT01342757 (3) [back to overview]Proportion of Patients With Magnetic Resonance Spectroscopy (MRS) Response to Initial Vorinostat by MRI and MRS Scans as Determined by Spectroscopic Index
NCT01413750 (3) [back to overview]Maximum Tolerated Dose (MTD) (Phase I)
NCT01413750 (3) [back to overview]Progression-free Survival (PFS)
NCT01413750 (3) [back to overview]Dose Limiting Toxicity (DLT) (Phase I)
NCT01483690 (2) [back to overview]Number of Participants Who Experienced a Dose Limiting Toxicity (DLT).
NCT01483690 (2) [back to overview]Disease Response Rate After Treatment.
NCT01502085 (1) [back to overview]Overall Response Rate (PR or Better) of Vorinostat in Combination With Lenalidomide and Dexamethasone in Patients With Relapsed/Refractory MM Refractory to a Previous Lenalidomide Containing Regimen
NCT01522976 (5) [back to overview]Response Rate (Phase II)
NCT01522976 (5) [back to overview]Relapse-free Survival
NCT01522976 (5) [back to overview]Overall Survival
NCT01522976 (5) [back to overview]Toxicity Rate
NCT01522976 (5) [back to overview]Pre-study Cytogenetic Abnormalities
NCT01534260 (4) [back to overview]Phase II - Treatment-Related Adverse Events Grade 3 or Higher
NCT01534260 (4) [back to overview]Number of Patients With Dose Limiting Toxicity
NCT01534260 (4) [back to overview]Phase II - Percentage of Patients With a Partial Response or Greater
NCT01534260 (4) [back to overview]Phase II - Time to Relapse
NCT01550224 (9) [back to overview]Complete Remission (CR)
NCT01550224 (9) [back to overview]Complete Remission With Incomplete Blood Count Recovery (CRp)
NCT01550224 (9) [back to overview]Cytogenetic Response (CyR)
NCT01550224 (9) [back to overview]Disease-free Survival (DFS) at 2 Years
NCT01550224 (9) [back to overview]Morphologic Leukemia-free State (MLFS)
NCT01550224 (9) [back to overview]Overall Survival (OS) at 2 Years
NCT01550224 (9) [back to overview]Partial Remission (PR)
NCT01550224 (9) [back to overview]Relapse-Free Survival (RFS) at 2 Years
NCT01550224 (9) [back to overview]Treatment Failure (TF)
NCT01593670 (5) [back to overview]Overall Survival
NCT01593670 (5) [back to overview]Number of Patients Who Had Natural Killer (NK) Cell Expansion
NCT01593670 (5) [back to overview]Number of Patients Who Experienced Grade 3 or Higher Non-hematologic Adverse Events
NCT01593670 (5) [back to overview]Number of Patients Who Became Transfusion Independent
NCT01593670 (5) [back to overview]The Number of Patients Who Achieved a Clinical Response
NCT01720602 (5) [back to overview]Duration of Response
NCT01720602 (5) [back to overview]Response Rate According to RECIST
NCT01720602 (5) [back to overview]Rate of Clinical Benefit of Patients Receiving Vorinostat/AI Combination Therapy According to RECIST
NCT01720602 (5) [back to overview]Progression-free Survival (PFS)
NCT01720602 (5) [back to overview]Overall Survival
NCT01728805 (4) [back to overview]Quality of Life (QoL) Assessment - Skindex-29 Symptoms Scale Score
NCT01728805 (4) [back to overview]Progression Free Survival
NCT01728805 (4) [back to overview]Overall Response Rate
NCT01728805 (4) [back to overview]Pruritis Evaluation
NCT01738646 (5) [back to overview]Six-month Progression-free Survival (PFS6)
NCT01738646 (5) [back to overview]Radiographic Response
NCT01738646 (5) [back to overview]Percentage of Participants Who Experience Grade 3 or Greater, Treatment Related, Non-hematologic Toxicities.
NCT01738646 (5) [back to overview]Median Progression-free Survival (PFS)
NCT01738646 (5) [back to overview]Median Overall Survival (OS)
NCT01748240 (1) [back to overview]Response Rate
NCT01789255 (7) [back to overview]The Percentage of Patients Alive at 1 Year
NCT01789255 (7) [back to overview]The Number of Participants That Experience Grade 2-4 Acute GVHD (Graft Versus Host Disease) by Day 100
NCT01789255 (7) [back to overview]Mean Percent of Planned Dose Administered
NCT01789255 (7) [back to overview]Median Plasma Concentration of IL-6 in Patients Treated With Vorinostat and Patients Not Treated With Vorinostat
NCT01789255 (7) [back to overview]Median Ac-H3 Levels in Patients Treated With Vorinostat and Patients Not Treated With Vorinostat
NCT01789255 (7) [back to overview]The Percentage of Patients With Relapse at 1 Year
NCT01789255 (7) [back to overview]The Percentage of Patients Alive Without GVHD or Use of Steroids
NCT01790568 (3) [back to overview]Non-Relapse Mortality Incidence
NCT01790568 (3) [back to overview]Percentage of Patients Alive at 1 Year
NCT01790568 (3) [back to overview]Percentage of Patients That Experience Grade 2-4 GVHD Within 100 Days of Transplant
NCT01802333 (10) [back to overview]Frequency and Severity of Toxicities
NCT01802333 (10) [back to overview]Cytogenetic Risk Distribution of Patients on This Study
NCT01802333 (10) [back to overview]Prevalence of the Mutation NPM1 in Patients on This Study.
NCT01802333 (10) [back to overview]Rate of Allogeneic HCT
NCT01802333 (10) [back to overview]Overall Survival (OS)
NCT01802333 (10) [back to overview]Complete Response (CR) Rate
NCT01802333 (10) [back to overview]Disease-free Survival (DFS)
NCT01802333 (10) [back to overview]Disease-free Survival (DFS) Among High Risk Patients
NCT01802333 (10) [back to overview]EFS of Arm I Compared to Arm II
NCT01802333 (10) [back to overview]Event-free Survival (EFS)
NCT01879085 (8) [back to overview]One-year Overall Survival (OS)
NCT01879085 (8) [back to overview]Objective Response Rate (ORR)
NCT01879085 (8) [back to overview]Six-month Overall Survival (OS)
NCT01879085 (8) [back to overview]Progression-free Survival (PFS)
NCT01879085 (8) [back to overview]Phase I: Recommended Phase II Dose of Vorinostat
NCT01879085 (8) [back to overview]Overall Survival (OS)
NCT01879085 (8) [back to overview]One-year Progression-free Survival (PFS)
NCT01879085 (8) [back to overview]Six-month Progression-free Survival (PFS)
NCT01983969 (2) [back to overview]Frequency of DLT
NCT01983969 (2) [back to overview]Participants With Event-free Survival (EFS)
NCT02035137 (2) [back to overview]Number of Participants With Grade 3 or Greater Non-hematologic Toxicities
NCT02035137 (2) [back to overview]Objective Tumor Response After One Course of Therapy
NCT02124083 (6) [back to overview]Biochemical Efficacy as Measured by Serum LGALS3
NCT02124083 (6) [back to overview]Biochemical Efficacy as Measured by Serum Cathepsin D
NCT02124083 (6) [back to overview]Biochemical Efficacy as Measured by Serum Cathepsin D
NCT02124083 (6) [back to overview]Biochemical Efficacy as Measured by Serum LGALS3
NCT02124083 (6) [back to overview]Number of Participants With Tolerabilty of 200 mg Vorinostat in Niemann-Pick Disease, Type C1
NCT02124083 (6) [back to overview]Number of Participants With Tolerabilty of 400 mg Vorinostat in Niemann-Pick Disease, Type C1
NCT02336074 (6) [back to overview]Viral Inhibition
NCT02336074 (6) [back to overview]CD8+ T-cell Responses
NCT02336074 (6) [back to overview]Percentage of CD4+ CD154+ IFNγ+ T Cells
NCT02336074 (6) [back to overview]Total HIV DNA From CD4 T-cells
NCT02336074 (6) [back to overview]Quantitative Viral Outgrowth
NCT02336074 (6) [back to overview]Histone H4 Acetylation
NCT02395627 (6) [back to overview]Number of Participants With Treatment-related Adverse Events (AE)
NCT02395627 (6) [back to overview]Duration of Response
NCT02395627 (6) [back to overview]Number of Participants With Tumor Responses Calculated by Immune Related Response-Criteria (irRC)
NCT02395627 (6) [back to overview]Objective Response Rate (ORR)
NCT02395627 (6) [back to overview]Overall Survival (OS)
NCT02395627 (6) [back to overview]Progression Free Survival
NCT02419755 (1) [back to overview]Number of Relevant Toxicities Related to Therapy
NCT02538510 (3) [back to overview]Progression Free Survival
NCT02538510 (3) [back to overview]Incidence of Toxicity Graded According to the National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.0
NCT02538510 (3) [back to overview]Objective Response Rate
NCT02553460 (1) [back to overview]Percentage of Treatment-related Mortality (TRM)
NCT03050450 (3) [back to overview]Total Number of Adverse Events
NCT03050450 (3) [back to overview]Number Participants With Hematologic and Non-hematologic Toxicities
NCT03050450 (3) [back to overview]Best Response of Children With Recurrent or Refractory Central Nervous System Tumors
NCT03212989 (2) [back to overview]Number of Participants w/ at Least One ≥ Grade 3 Adverse Event That is Possibly or Definitely Related to Vorinostat (VOR) or HIV-specific T Cell (HXTC)
NCT03212989 (2) [back to overview]Number of Participants Demonstrating an HIV-specific Immune Response to the Combination of Vorinostat (VOR) and HIV-specific T Cells (HXTC) Therapy as Well as a Change in the Frequency of Latent HIV Infection
NCT03382834 (4) [back to overview]Number of Participants With HIV-1 RNA Levels (Measured by Single Copy Assay) Greater or Equal to the Lower Limit of Quantification
NCT03382834 (4) [back to overview]Proportion of Participants With New Grade 3 or Greater Adverse Events
NCT03382834 (4) [back to overview]Change From Baseline in Total HIV-1 DNA Levels in CD4+ T Cells
NCT03382834 (4) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA in CD4+ T Cells
NCT03713320 (14) [back to overview]Complete Response Rate
NCT03713320 (14) [back to overview]Duration of Response in Skin
NCT03713320 (14) [back to overview]Objective Response Rate in the Skin of at Least 28-days Duration (ORR1)
NCT03713320 (14) [back to overview]Percentage of Subjects Achieving ≥ 50% Improvement in mSWAT at 28 Days
NCT03713320 (14) [back to overview]Percentage of Subjects Achieving ≥ 50% Improvement in mSWAT at 4 Months
NCT03713320 (14) [back to overview]Progression-free Survival (PFS)
NCT03713320 (14) [back to overview]Pruritus Medication Utilization
NCT03713320 (14) [back to overview]Time to ≥ 50% Improvement in mSWAT
NCT03713320 (14) [back to overview]Time to Maximal Effect in mSWAT
NCT03713320 (14) [back to overview]Peak Plasma Concentration (Cmax) of Cobomarsen - First Dose
NCT03713320 (14) [back to overview]Peak Plasma Concentration (Cmax) of Cobomarsen - Week 5
NCT03713320 (14) [back to overview]Percentage of Subjects Achieving an Objective Skin Response of at Least 4 Months Duration (ORR4)
NCT03713320 (14) [back to overview]Area Under the Plasma Concentration vs. Time Curve (AUC) of Cobomarsen - Week 5
NCT03713320 (14) [back to overview]Time to Progression
NCT03803605 (1) [back to overview]Percent of Participants With a Grade 3 or Higher Treatment-Related Adverse Event (AE)
NCT04190056 (5) [back to overview]Percentage of Participants With Tumor Responses
NCT04190056 (5) [back to overview]Duration of Response (DOR)
NCT04190056 (5) [back to overview]Median Overall Survival (OS)
NCT04190056 (5) [back to overview]Median Progression Free Survival (PFS)
NCT04190056 (5) [back to overview]Overall Response Rate (ORR)

Safety and Tolerability as Measured by the Number of Participants With Disease Progression

Number of participants with disease progression (protocol-mandated reason for discontinuation). Disease progression was determined by the principle investigator. (NCT00106626)
Timeframe: Any time during 8 cycle treatment period through 30 days after.

InterventionParticipants (Number)
Cohort A - Vorinostat BID + Pemetrexed + Cisplatin4
Cohort B - Vorinostat QD + Pemetrexed + Cisplatin1
Cohort C - Vorinostat BID + Pemetrexed9
Cohort D - Vorinostat QD + Pemetrexed10

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Maximum Tolerated Dose (MTD) Status as Determined by Number of Participants With Dose Limiting Toxicity (DLT) at Each Dose Level

MTD was determined by the occurrence of DLTs during the first treatment cycle. DLT describes side effects of a drug or other treatment that are serious enough to prevent an increase in dose or level of that treatment. The dose level is equal to the MTD if < 2 patients experience a DLT and is also the highest tolerated dose level in the cohort. (NCT00106626)
Timeframe: Cycle 1 (21 days)

,,,,,,,,
InterventionParticipants (Number)
Number (#) of DLT# Participants treated at a dose level # Participants treated at a dose level =MTD# Participants treated at a dose level >MTD
Dose Level A.11060
Dose Level A.23007
Dose Level B.10030
Dose Level B.22006
Dose Level C.11700
Dose Level C.20400
Dose Level C.30030
Dose Level D.11090
Dose Level D.22007

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Number of Participants With Dose Modifications of Either Vorinostat or Bortezomib Due to Adverse Experiences (AEs) After Treatment With Study Drug

An adverse experience (AE) was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the sponsor's product, was also an adverse experience. (NCT00111813)
Timeframe: Day 1 to disease progression, toxicity, or death, assessed up to 29 months

,,,,,
InterventionParticipants (Number)
No dose modificationOne dose modificationTwo or more dose modifications
Vorinostat 200 mg + Bortezomib 0.7 mg/m^2300
Vorinostat 200 mg + Bortezomib 0.9 mg/m^2300
Vorinostat 300 mg + Bortezomib 1.3 mg/m^2820
Vorinostat 400 mg + Bortezomib 0.9 mg/m^2420
Vorinostat 400 mg + Bortezomib 1.1 mg/m^2312
Vorinostat 400 mg + Bortezomib 1.3 mg/m^2303

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Mean Duration of Treatment With Vorinostat

"Event causing discontinuation from the study was defined as (1) progressive disease OR (2) intolerable toxicity.~Progressive disease was defined as:~>25% increase in the level of serum monoclonal paraprotein.~25% increase in 24-hour urinary light chain excretion.~>25% increase in plasma cells in a bone marrow aspirate or on trephine~biopsy.~Development of new bone lesions or soft tissue plasmacytomas.~Development of hypercalcemia.~Intolerable toxicity was based on the clinical judgment of the investigator." (NCT00111813)
Timeframe: Day 1 to an event causing discontinuation from the study, assessed up to 29 months

InterventionDays (Mean)
200 mg300 mg400 mg
All Participants4.672.6107.1

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Laboratory AE Summary

"An AE was defined as any unfavorable/unintended change in the structure/function/chemistry of the body temporally associated with the use of study drug, or any worsening of a preexisting condition.~A SAE was any AE that resulted in death, was life threatening, resulted in a persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was a new cancer, or was an overdose.~A lab (S)AE was any lab value considered clinically significant in the investigator's judgment." (NCT00111813)
Timeframe: Day 1 up to disease progression, toxicity, or death, assessed up to 29 months

,,,,,
InterventionParticipants (Number)
With one or more laboratory AEsWith no laboratory AEsWith drug-related laboratory AEsWith laboratory Serious AEs (SAEs)With drug-related laboratory SAEsWho diedWho discontinued due to laboratory AEsWho discontinued due to drug-related lab AEsWho discontinued due to laboratory SAEsWho discontinued due to drug-related lab SAEs
Vorinostat 200 mg + Bortezomib 0.7 mg/m^21210000000
Vorinostat 200 mg + Bortezomib 0.9 mg/m^21200000000
Vorinostat 300 mg + Bortezomib 1.3 mg/m^23720000000
Vorinostat 400 mg + Bortezomib 0.9 mg/m^20600000000
Vorinostat 400 mg + Bortezomib 1.1 mg/m^22410000000
Vorinostat 400 mg + Bortezomib 1.3 mg/m^23330000000

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Clinical AE Summary

"An AE was defined as any unfavorable/unintended change in the structure/function/chemistry of the body temporally associated with the use of study drug, or any worsening of a preexisting condition.~A serious AE (SAE) was any AE that resulted in death, was life threatening, resulted in a persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was a new cancer, or was an overdose." (NCT00111813)
Timeframe: Day 1 up to disease progression, toxicity, or death, assessed up to 30 days after end of treatment (up to 30 months)

,,,,,
InterventionParticipants (Number)
With one or more AEsWith no AEsWith drug-related AEsWith Serious AEs (SAEs)With drug-related SAEsWho diedWho discontinued due to AEsWho discontinued due to drug-related AEsWho discontinued due to SAEsWho discontinued due to drug-related SAEs
Vorinostat 200 mg + Bortezomib 0.7 mg/m^23020001000
Vorinostat 200 mg + Bortezomib 0.9 mg/m^23031002200
Vorinostat 300 mg + Bortezomib 1.3 mg/m^2100102104311
Vorinostat 400 mg + Bortezomib 0.9 mg/m^26064402222
Vorinostat 400 mg + Bortezomib 1.1 mg/m^26064201100
Vorinostat 400 mg + Bortezomib 1.3 mg/m^26062102110

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Mean Time to First AE Resulting in a Dose Modification in Either Vorinostat or Bortezomib

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the sponsor's product, was also an adverse experience. (NCT00111813)
Timeframe: Day 1 to disease progression, toxicity, or death, assessed up to 29 months

InterventionDays (Mean)
Vorinostat 200 mg + Bortezomib 0.7 mg/m^2NA
Vorinostat 200 mg + Bortezomib 0.9 mg/m^2NA
Vorinostat 300 mg + Bortezomib 1.3 mg/m^258
Vorinostat 400 mg + Bortezomib 0.9 mg/m^258
Vorinostat 400 mg + Bortezomib 1.1 mg/m^2128
Vorinostat 400 mg + Bortezomib 1.3 mg/m^232

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Objective Response Rate Assessed by Response Evaluation Criteria for Solid Tumors (RECIST)

Per Response Evaluation Criteria in Solid Tumours Criteria (RECIST v1.0) for target lesions and are assessed by MRI: Complete Response (CR), disappearance of all target lesions; Partial Response (PR), at least 30% decrease in sum of longest diameter of target lesions; Objective Response (OR) = CR+ PR. (NCT00121225)
Timeframe: Up to 5 years

Interventionparticipants (Number)
Arm I2

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Comparison of VEGF Serum Levels to Response to Vorinostat

Blood specimens were collected from participants on Day 1 Cycle 1 prior to treatment (baseline), Day 1 3-4 hours following Vorinostat ingestion, Day 8 and Day 15. VEGF serum concentrations were detected using the Luminex multiplexed assay, where the median fluorescence intensity results were analyzed by a weighted five-parameter logistic method. The values were averaged across all time points per participant. (NCT00121225)
Timeframe: Baseline, Day 1, Day 8 and Day 15

Interventionpg (Mean)
Arm 1 Vorinostat203

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Time to Progression Assessed by RECIST

(NCT00121225)
Timeframe: Up to 5 years

Interventionmonths (Median)
Arm 1 Vorinostat4

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Difference in HP1 and MacroH2A Nuclear Foci Expression Between Progressive Minus Stable Disease Outcomes

Macro H2A and HP1 expression levels were compared through analysis of log fold changes in antibody expression in a multivariate general linear model between progressive disease and stable disease outcomes. (NCT00121225)
Timeframe: Baseline and day 15

Interventionlog fold change (Mean)
MacroH2A1.1MacroH2A1.2HP1
Arm 1 Vorinostat0.149-0.748-0.077

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Number of Patients With p53 Allelic Variations (72R or 72P)

Participants were assessed for p53 allelic variation at baseline (NCT00121225)
Timeframe: Baseline

Interventionparticipants (Number)
Wild TypeMutant
Arm 1 Vorinostat2011

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Number of Participants Who Responded to Treatment

"Disease burden as assessed by the pre-specified Severity Weighted Assessment Tool (SWAT) measurement. A Response is defined as equal to or greater than 50% improvement in SWAT score.~SWAT Score is determined by the Lesions classified as patch, plaque, or tumor. The sum of percent of total body surface area (%TBSA) by lesion type is derived and multiplied by a factor of 1 (for patch), 2 (for plaque), or 4 (for tumor). The skin score total is derived by summing the skin score subtotals for patches, plaques and tumors. The skin score total is dimensionless and can range from 0 to 400" (NCT00127101)
Timeframe: Every 28 days for up to 6 Months of Treatment

,,,,,
InterventionParticipants (Number)
ResponseNo Response
Cohort 103
Cohort 205
Cohort 2a03
Cohort 2b12
Cohort 623
Cohort 712

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Maximum Tolerated Dose (MTD) as Determined by the Number of Participants With Dose Limiting Toxicities

Number of patients with Dose Limiting Toxicities (DLT). A DLT is an adverse event that determined the treatment dose level was not tolerable for that patient in Cycle 1. (NCT00127101)
Timeframe: Day 1 to day 28

,,,,,
InterventionParticipants (Number)
DLTNo DLT
Cohort 103
Cohort 223
Cohort 2a03
Cohort 2b03
Cohort 605
Cohort 712

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Cmax of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration

Cmax is a measure of the maximum amount of drug in the plasma after the dose is given. (NCT00127127)
Timeframe: Day 19: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM (Geometric Mean)
Vorinostat 100 mg Twice-daily0.29
Vorinostat 200 mg Twice-daily0.84
Vorinostat 400 mg Once-daily0.86
Vorinostat 500 mg Once-daily1.09

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Cmax of Vorinostat After a Single Oral Dose in a Fed State

Cmax is a measure of the maximum amount of drug in the plasma after the dose is given. (NCT00127127)
Timeframe: Day 3: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM (Geometric Mean)
Vorinostat 100 mg FED0.21
Vorinostat 200 mg FED0.59
Vorinostat 400 mg FED0.93
Vorinostat 500 mg FED1.35

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Maximum Concentration (Cmax) of Vorinostat After a Single Oral Dose in a Fasted State

Cmax is a measure of the maximum amount of drug in the plasma after the dose is given. (NCT00127127)
Timeframe: Day 1: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM (Geometric Mean)
Vorinostat 100 mg FASTED0.49
Vorinostat 200 mg FASTED0.77
Vorinostat 400 mg FASTED1.19
Vorinostat 500 mg FASTED1.06

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Number of Participants Who Discontinued Study Treatment Due to an Adverse Event

An adverse event is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. (NCT00127127)
Timeframe: Up to approximately 4 years

InterventionParticipants (Count of Participants)
Vorinostat 100 mg0
Vorinostat 200 mg1
Vorinostat 400 mg0
Vorinostat 500 mg1

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Number of Participants Who Experienced One or More Adverse Events

An adverse event is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. (NCT00127127)
Timeframe: Up to approximately 4 years

InterventionParticipants (Count of Participants)
Vorinostat 100 mg4
Vorinostat 200 mg6
Vorinostat 400 mg3
Vorinostat 500 mg6

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Number of Participants With a Dose-Limiting Toxicity (DLT) During Cycle 1

A DLT was defined as an event considered to be related to study treatment and included: 1) Grade 4 neutropenia refractory to treatments persisting more than 5 days; 2) Grade 3 or more severe neutropenic fever; 3) Grade 3 thrombocytopenia requiring blood transfusions or Grade 4 thrombocytopenia; 4) Grade 4 hemoglobin decrease; 5) Grade 3 or more severe non-hematological toxicities other than anorexia, nausea/vomiting, and fatigue. (For the diarrhea, it was defined as not to use the frequency for the grading. For the alanine aminotransferase [ALT]/aspartate aminotransferase [AST]), it was defined as the case of over 300 IU/L; 6) Grade 3 or more severe anorexia, nausea/vomiting, and fatigue refractory to treatments; and 7) compliance of the study drug, while administrating 14 consecutive days, was less than 50% due to the drug-related adverse experience. (NCT00127127)
Timeframe: Up to 26 days

InterventionParticipants (Count of Participants)
Vorinostat 100 mg0
Vorinostat 200 mg3
Vorinostat 400 mg0
Vorinostat 500 mg2

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t½ of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration

t½ is the elimination half-life of study drug. t½ is the time it takes for half of the study drug in the blood plasma to dissipate. (NCT00127127)
Timeframe: Day 19: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg Twice-daily1.95
Vorinostat 200 mg Twice-daily1.42
Vorinostat 400 mg Once-daily1.98
Vorinostat 500 mg Once-daily1.30

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t½ of Vorinostat After a Single Oral Dose in a Fed State

t½ is the elimination half-life of study drug. t½ is the time it takes for half of the study drug in the blood plasma to dissipate. (NCT00127127)
Timeframe: Day 3: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg FED1.62
Vorinostat 200 mg FED1.36
Vorinostat 400 mg FED2.01
Vorinostat 500 mg FED1.60

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Time to Maximum Concentration (Tmax) of Vorinostat After a Single Oral Dose in a Fasted State

Tmax is a measure of the time to reach the maximum concentration in the plasma after the drug dose. (NCT00127127)
Timeframe: Day 1: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg FASTED0.84
Vorinostat 200 mg FASTED1.59
Vorinostat 400 mg FASTED2.49
Vorinostat 500 mg FASTED1.91

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Tmax of Vorinostat After a Single Oral Dose in a Fed State

Tmax is a measure of the time to reach the maximum concentration in the plasma after the drug dose. (NCT00127127)
Timeframe: Day 3: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg FED5.66
Vorinostat 200 mg FED3.00
Vorinostat 400 mg FED3.53
Vorinostat 500 mg FED3.17

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AUC0-inf of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration

AUC0-inf is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. (NCT00127127)
Timeframe: Day 19: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM·hours (Geometric Mean)
Vorinostat 100 mg Twice-daily1.33
Vorinostat 200 mg Twice-daily2.76
Vorinostat 400 mg Once-daily5.41
Vorinostat 500 mg Once-daily6.33

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Apparent Terminal Half-Life (t½) of Vorinostat After a Single Oral Dose in a Fasted State

t½ is the elimination half-life of study drug. t½ is the time it takes for half of the study drug in the blood plasma to dissipate. (NCT00127127)
Timeframe: Day 1: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg FASTED1.08
Vorinostat 200 mg FASTED1.83
Vorinostat 400 mg FASTED1.90
Vorinostat 500 mg FASTED1.93

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Area Under the Plasma Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of Vorinostat After a Single Oral Dose in a Fasted State

AUC0-inf is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. (NCT00127127)
Timeframe: Day 1: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM·hours (Geometric Mean)
Vorinostat 100 mg FASTED1.20
Vorinostat 200 mg FASTED2.31
Vorinostat 400 mg FASTED3.96
Vorinostat 500 mg FASTED3.47

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Tmax of Vorinostat After 14 Days of Once-Daily or Twice-Daily Administration

Tmax is a measure of the time to reach the maximum concentration in the plasma after the drug dose. (NCT00127127)
Timeframe: Day 19: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionHours (Mean)
Vorinostat 100 mg Twice-daily4.66
Vorinostat 200 mg Twice-daily3.30
Vorinostat 400 mg Once-daily4.34
Vorinostat 500 mg Once-daily4.61

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AUC0-Inf of Vorinostat After a Single Oral Dose in a Fed State

AUC0-inf is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. (NCT00127127)
Timeframe: Day 3: pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 hours post-dose

InterventionμM·hours (Geometric Mean)
Vorinostat 100 mg FED0.98
Vorinostat 200 mg FED2.22
Vorinostat 400 mg FED4.30
Vorinostat 500 mg FED5.93

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Number of Participants Who Experienced Adverse Events (AEs) Characterized as Grade 3 or Grade 4 According to the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE)

An AE was defined as any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with the use of the Sponsor's product whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the Sponsor's product is also an AE. Reporting of AEs per NCI CTCAE is based on 5 grades of severity; Grade 1 (mild; no treatment needed), Grade 2 (moderate; minimal treatment needed), Grade 3 (severe, not life threatening; hospitalization needed), Grade 4 (life threatening; urgent treatment needed) and Grade 5 (death).The final analysis for Grade 3 or 4 AEs was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. Per protocol number of participants who experienced Grade 3/4 AEs per NCI CTCAE is reported here for all randomized participants who received ≥1 dose of study treatment. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionParticipants (Count of Participants)
Vorinostat165
Placebo146

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Percentage of Participants With ≥10% Change From Baseline in FVC at Week 12

Pulmonary function test was conducted using a spirometer for assessment of FVC. FVC is the volume of air forcibly exhaled from the lungs after taking the deepest breath possible. Baseline measurement was taken before treatment initiation. Per protocol percentage of participants with ≥10% change (percent change calculated: [Week 12 - Baseline]/Baseline*100) in FVC from baseline to Week 12 post treatment initiation is reported here for all randomized participants who had a valid baseline and ≥1 post-baseline value for FVC. (NCT00128102)
Timeframe: Baseline, Week 12

InterventionPercentage of participants (Number)
Vorinostat24.76
Placebo21.63

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Progression Free Survival (PFS)

PFS was defined as the time from randomization to the first documented progressive disease (PD) per meso-modified-Response Evaluation Criteria in Solid Tumors (Meso-modified RECIST) based on independent radiology review or death due to any cause, whichever occurred first. Meso-modified RECIST was created and validated for disease measurement in pleural mesothelioma. Per meso-modified RECIST, PD was defined as ≥20% increase in the total tumor measurement over the nadir measurement or the appearance of ≥1 new lesions. The final analysis for PFS per Meso-modified RECIST by independent radiology review was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. PFS analysis per Meso-modified RECIST by independent radiology review is reported here for all randomized participants. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionWeeks (Median)
Vorinostat6.3
Placebo6.1

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Number of Participants Who Discontinued Study Treatment Due to an AE

An AE was defined as any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with the use of the Sponsor's product whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the Sponsor's product is also an AE. The final analysis for participants who discontinued study treatment due to an AE was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. Per protocol number of participants who discontinued study treatment due to an AE is reported here for all randomized participants who received ≥1 dose of study treatment. As specified by the protocol, participants who discontinued study treatment due to an AE remained on study until investigator notification to discontinue. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionParticipants (Count of Participants)
Vorinostat60
Placebo49

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Percentage of Participants With ≥50% Change Together With a >10 mm Change From Baseline in the LCSS-Meso Dyspnea Score at Week 12

LCSS-Meso provides participant-reported outcome measures of symptom burden and quality of life. LCSS-Meso includes the disease-related item dyspnea or shortness of breath. The LCSS-Meso item dyspnea is measured on a visual analog scale (VAS) using 100 mm and assigned an individual score based on symptom intensity. Dyspnea VAS score ranges from 0 mm (lowest; no dyspnea) to 100 mm (highest; worst dyspnea). Higher scores indicate dyspnea worsening. Baseline measurement was taken before treatment initiation. Per protocol percentage of participants with ≥50% change (percent change calculated: [Week 12 - Baseline]/Baseline*100) and >10 mm absolute change in LCSS-Meso dyspnea score from baseline to Week 12 post treatment initiation is reported here for all randomized participants who had a valid baseline and ≥1 post-baseline value for the LCSS-Meso dyspnea score available. (NCT00128102)
Timeframe: Baseline, Week 12

InterventionPercentage of participants (Number)
Vorinostat15.05
Placebo16.39

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Number of Participants Who Experienced an AE

An AE was defined as any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with the use of the Sponsor's product whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the Sponsor's product is also an AE. The final analysis for participants who experienced an AE was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. Per protocol number of participants who experienced an AE is reported here for all randomized participants who received ≥1 dose of study treatment. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionParticipants (Count of Participants)
Vorinostat327
Placebo311

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Objective Response Rate (ORR)

ORR was defined as the percentage of participants in the analysis population who had a complete response (CR: disappearance of all target lesions with no evidence of tumor elsewhere) or a partial response (PR: ≥30% reduction in the total tumor measurement) per Meso-modified RECIST based on independent radiology review. Meso-modified RECIST was created and validated for disease measurement in pleural mesothelioma. The final analysis for ORR per Meso-modified RECIST by independent radiology review was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. Per protocol percentage of participants who had a CR or a PR per Meso-modified RECIST by independent radiology review is reported here as the ORR for all randomized participants who had valid baseline data for ORR analysis available. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionPercentage of Participants (Number)
Vorinostat0.63
Placebo0.31

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Overall Survival (OS)

OS was defined as the time from randomization to death due to any cause. Participants without documented death at the time of final analysis were censored at the date of the last follow up. The final analysis for OS was planned and performed at the time of the protocol pre-specified final statistical analysis with a data cut-off of 15-July-2011. OS analysis is reported here for all randomized participants. (NCT00128102)
Timeframe: Up to ~72 months (through pre-specified final statistical analysis cut-off date of 15-July-2011)

InterventionWeeks (Median)
Vorinostat30.7
Placebo27.1

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Percent Change From Baseline in Forced Vital Capacity (FVC) at Week 12

Pulmonary function test was conducted using a spirometer for assessment of FVC. FVC is the volume of air forcibly exhaled from the lungs after taking the deepest breath possible. Baseline measurement was taken before treatment initiation. Per protocol percent change in FVC from baseline to Week 12 post treatment initiation (percent change calculated: [Week 12 - Baseline]/Baseline*100)] is reported here for all randomized participants who had a valid baseline and ≥1 post-baseline value for FVC available. (NCT00128102)
Timeframe: Baseline, Week 12

InterventionPercent Change (Mean)
Vorinostat-6.0
Placebo-5.6

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Percent Change From Baseline in Lung Cancer Symptom Scale, Modified for Mesothelioma (LCSS-Meso) Dyspnea Score at Week 12

LCSS-Meso provides participant-reported outcome measures of symptom burden and quality of life. LCSS-Meso includes the disease-related item dyspnea or shortness of breath. The LCSS-Meso item dyspnea is measured on a visual analog scale (VAS) using 100 mm and assigned an individual score based on symptom intensity. Dyspnea VAS score ranges from 0 mm (lowest; no dyspnea) to 100 mm (highest; worst dyspnea). Higher scores indicate dyspnea worsening. Baseline measurement was taken before treatment initiation. Per protocol percent change in the LCSS-Meso dyspnea score from baseline to Week 12 post treatment initiation (percent change calculated: [Week 12 - Baseline]/Baseline*100)] is reported here for all randomized participants who had a valid baseline and ≥1 post-baseline value for the LCSS-Meso dyspnea score available. (NCT00128102)
Timeframe: Baseline, Week 12

InterventionPercent Change (Mean)
Vorinostat141.8
Placebo174.7

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Objective Tumor Response Rate

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR (NCT00132002)
Timeframe: Up to 8 weeks

Interventionpercentage of participants (Number)
Arm 10

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Overall Survival

Estimated using the product-limit method of Kaplan and Meier. (NCT00132002)
Timeframe: From the initial date of treatment to time of death, up to 5 years.

InterventionMonths (Median)
Arm 124

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Progression-free Survival

Estimated using the product-limit method of Kaplan and Meier. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. (NCT00132002)
Timeframe: From start of treatment to the time of documented progression, assessed up to 5 years

InterventionMonths (Median)
Arm 12.6

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Assess Number of Patients Who Achieve Confirmed and Unconfirmed Complete Response (CR) or Partial Response (PR)

Complete Response(CR) is a complete disappearance of all disease with the exception of nodes. No new lesions. previously enlarged organs must have regressed and not be palpable. Bone marrow(BM) must be negative if positive at baseline. Normalization of markers. CR Unconfirmed (CRU) does not qualify for CR above, due to a residual nodal mass or an indeterminate BM. Partial Response(PR) is a 50% decrease in the SPD for up to 6 identified dominant lesions, including spleenic and hepatic nodules from baseline. No new lesions and no increase in the size of liver, spleen or other nodes. (NCT00132028)
Timeframe: after every 3 cycles on treatment

Interventionparticipants (Number)
Complete Response (CR)Partial Response (PR)Unconfirmed Complete Response (UCR)Unconfirmed Partial Response (UPR)No Response
SAHA (Vorinostat)010024

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Progression-Free Survival

Measured from date of registration to date of first observation of progression or death, or last contact date. Progression is defined as a 50% increase in sum of products of greatest diameters (SPD) of target measurable lesions over the smallest sum observed (over baseline if no decrease during therapy) using the same techniques as baseline; appearance of a new lesion/site; unequivocal progression of non-measurable disease in the opinion of the treating physician; death due to disease without prior documentation of progression. (NCT00132028)
Timeframe: after every 3 cycles on treatment, then every 6 months for 2 years, then annually for a total of 5 years.

Interventionmonths (Median)
SAHA (Vorinostat)4.8

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Overall Survival

Measured from date of registration to death, or last contact date (NCT00132028)
Timeframe: after every 3 cycles on treatment, then every 6 months for 2 years, then annually for a total of 5 years.

Interventionmonths (Median)
SAHA (Vorinostat)15.7

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Objective Response Rate (PR + CR) Using RECIST/WHO Response Criteria

"Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR., or similar definition that is accurate and appropriate." (NCT00134043)
Timeframe: Up to 3 years

,
Interventionpercentage of participants (Number)
PR (Partial Response)CR (Complete Response)Stable disease
DTCs (Well-differentiated Thyroid Carcinomas)0056
MTC (Medullary Thyroid Cancer)000

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Toxicity

Number of participants experiencing adverse events possibly related to SAHA from first dose of treatment until 30 days from the last dose of treatment. (NCT00138203)
Timeframe: From first dose of treatment until 30 days from the last dose of treatment

InterventionParticipants (Count of Participants)
SAHA16

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Response Per RECIST Criteria

Per Response Evaluation Criteria In Solid Tumors and assessed by CT: Complete Response(CR), Disappearance of all target lesions; Partial Response(PR),>=30% decrease in the sum of the longest diameter of target lesions; Overall Response(OR) = CR + PR. (NCT00138203)
Timeframe: Time from treatment initiation until the end of treatment. The median number of cycles was 3 (range 1-27)

Interventionparticipants (Number)
SAHA0

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Overall Survial

Overall survial of subjects from the start of treatment to the time of death (NCT00138203)
Timeframe: From treatment start to time of death

Interventionmonths (Median)
SAHA7.1

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Time to Progression

Time to progression per Response Evaluation Criteria In Solid Tumors and assessed by CT: Complete Response(CR), Disappearance of all target lesions; Partial Response(PR),>=30% decrease in the sum of the longest diameter of target lesions; Overall Response(OR) = CR + PR. (NCT00138203)
Timeframe: From start of treatment to progression (average was 3.7 months)

Interventionmonths (Median)
SAHA2.3

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Survival

Estimated using Kaplan-Meier survival curve. (NCT00238303)
Timeframe: From study registration to date of death due to any cause or last follow-up (up to 5 years)

Interventionmonths (Median)
Stratum 1 (Not Undergoing Surgery)5.7
Stratum 2 (Undergoing Surgery)10.2
Stratum 3 (Not Undergoing Surgery)2.2

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Time to Progression

"Estimated using Kaplan-Meier survival curve.~Definition of progression:~Bidimensionally measurable disease: >25% increase in product of perpendicular diameters of contrast enhancement or mass or appearance of new lesions.~Evaluable disease (i.e., contrast enhancing mass on MRI and/or CT that is not bidimensionally measurable but clearly evaluable for response to therapy): unequivocal increase in size of contrast enhancement or increase in mass effect as agreed upon independently by primary physician and quality control physicians: appearance of new lesions." (NCT00238303)
Timeframe: From registration to disease progression (up to 5 years)

Interventionmonths (Median)
Stratum 1 Patients That Started Treatment1.9
Stratum 2 (Undergoing Surgery)3.7
Stratum 3 (Not Undergoing Surgery)1.4

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Confirmed Tumor Response

"A confirmed tumor response will be defined as an objective status of complete response (CR), partial response (PR), or regression (REGR) on two consecutive evaluations, which include neuroimaging, lasting during a period of at least 6 weeks. Confidence intervals for the true proportion will be calculated using the exact binomial method.~Bidimensionally measurable disease:≥50% reduction in product of perpendicular diameters of contrast enhancement or mass with no new lesions with the patient being on stable or decreased steroid dose.~Evaluable disease (i.e., contrast enhancing mass on MRI and/or CT that is not bidimensionally measurable but clearly evaluable for response to therapy): unequivocal reduction in size of contrast-enhancement or decrease in mass effect as agreed upon independently by primary physician and quality control physicians; no new lesions. Patient should be on stable or decreased steroid dose." (NCT00238303)
Timeframe: Assessed up to 5 years

Interventionpercentage of participants (Number)
Stratum 1 (Not Undergoing Surgery)3.0
Stratum 3 (Not Undergoing Surgery)0

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Proportion of Successes (Patients Alive and Progression-free)

"Estimated using the Binomial point estimator (number of successes divided by the total number of evaluable patients) and the Binomial 95% confidence interval estimated by the exact method.~Definition of progression:~Bidimensionally measurable disease: >25% increase in product of perpendicular diameters of contrast enhancement or mass or appearance of new lesions.~Evaluable disease (i.e., contrast enhancing mass on MRI and/or CT that is not bidimensionally measurable but clearly evaluable for response to therapy): unequivocal increase in size of contrast enhancement or increase in mass effect as agreed upon independently by primary physician and quality control physicians: appearance of new lesions." (NCT00238303)
Timeframe: At 6 months

Interventionpercentage of participants (Number)
Stratum 1 Patients That Started Treatment15.2
Stratum 2 (Undergoing Surgery)26.7
Stratum 3 (Not Undergoing Surgery)10

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Stable Disease (SD) as Best Response Based on Response Criteria in Solid Tumors (RECIST)

Stable disease is defined as less than a radiographic partial response, but not progressive disease (NCT00251589)
Timeframe: Every 57 days beginning with Cycle 3, or more frequently if appropriate

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk6
Vorinostat 300 mg q.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk1
Vorinostat 300 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk1
Vorinostat 400 mg q.d. 21d/4wk + Erlotinib 150 mg q.d. 7d/wk1

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Disease Progression After Week 8 Based on Response Criteria in Solid Tumors (RECIST)

First documentation of Progressive Disease (PD) occurring > 8 weeks on study. (NCT00251589)
Timeframe: Every 57 days beginning with Cycle 3 (Week 8), or more frequently if appropriate

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk3
Vorinostat 300 mg q.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 300 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 400 mg q.d. 21d/4wk + Erlotinib 150 mg q.d. 7d/wk0

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Dose Limiting Toxicity (DLT) Occurring in Cycle 1 of the Phase I Portion of the Study

Adverse event(s) that determined the treatment dose level was not tolerable for that patient in Cycle 1 of the Phase I portion of the study. (NCT00251589)
Timeframe: Day 1 to 28 in the Phase I portion of the study

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 300 mg q.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk2
Vorinostat 300 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk2
Vorinostat 400 mg q.d. 21d/4wk + Erlotinib 150 mg q.d. 7d/wk1

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Dose Limiting Toxicity Occurring in Cycle 1 of the Phase II Portion of the Study

Adverse event(s) that determined the treatment dose level was not tolerable for that patient in Cycle 1 of the Phase II portion of the study. (NCT00251589)
Timeframe: Day 1 to 28 in the Phase II portion of the study

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk3

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Dose Limiting Toxicity Occurring in Cycles 2 and Beyond of the Phase II Portion of the Study

Adverse event(s) that determined the treatment dose level was not tolerable for that patient in Cycles 2 and beyond of the Phase II portion of the study. (NCT00251589)
Timeframe: After day 28 in the Phase II portion of the study

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk3

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Progression-free Survival

Progression-free survival was measured from the start of the treatment to the time when the criteria for progression was met or death due to any cause (whichever is first recorded). (NCT00251589)
Timeframe: Day 1 to disease progression or death

InterventionDays (Mean)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk57

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Progressive Disease (PD) as Best Response Based on Response Criteria in Solid Tumors (RECIST)

Progressive disease is defined as a ≥20% increase in the sum of the longest diameter, the appearance of one or more new lesions and/or unequivocal progression of non-target lesions by conventional or spiral CT or MRI (NCT00251589)
Timeframe: Every 57 days beginning with Cycle 3, or more frequently if appropriate

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk7
Vorinostat 300 mg q.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 300 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 400 mg q.d. 21d/4wk + Erlotinib 150 mg q.d. 7d/wk0

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Unconfirmed Partial Response (UPR) Based on Response Criteria in Solid Tumors (RECIST)

An unconfirmed partial response is defined as a partial response that has not been confirmed by a follow up CT scan (or MRI) at least 4 weeks after the criteria for response are first met. (A partial response is defined as an at least 30% reduction in the sum of the longest diameter of the target lesions. Non-target lesions must be at least stable) (NCT00251589)
Timeframe: Every 57 days beginning with Cycle 3, or more frequently if appropriate

InterventionParticipants (Number)
Vorinostat 200 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 300 mg q.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 300 mg b.i.d. 3d/wk + Erlotinib 150 mg q.d. 7d/wk0
Vorinostat 400 mg q.d. 21d/4wk + Erlotinib 150 mg q.d. 7d/wk0

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2-Year Overall Survival

Estimated using the product-limit method of Kaplan and Meier. (NCT00253630)
Timeframe: Until Death from any cause, up to 2 years

Interventionpercentage of participants (Number)
Treatment (Vorinostat)77

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2-Year Progression Free-Survival

Estimated using the product-limit method of Kaplan and Meier. Progression defined as any new lesion or increase by greater than 50% of previously involved sites from nadir. (NCT00253630)
Timeframe: Until death or progression, up to 2 years

Interventionpercentage of participants (Number)
Treatment (Vorinostat)37

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Response Rate

Radiological assessment by CT and/or PET scan after every three cycles (every 3 months). Response assessed by the standard Cheson criteria (Cheson et al, J Clin Oncol 17:1244, 1999). Complete Remission (CR) - (a) FDG-avid or PET positive prior to therapy; mass of any size permitted if PET negative (b) Variably FDG-avid or PET negative; regression to normal size on CT; Partial Remission (PR) - 50% or greater decrease in SPD of up to 6 largest dominant masses; no increase in size of other nodes (a) FDG-avid or PET positive prior to therapy; one or more PET positive at previously involved site (b) Variably FDG-avid or PET negative; regression on CT. Response Rate = CR + PR. (NCT00253630)
Timeframe: Up to 3 years

Interventionpercentage of participants (Number)
Treatment (Vorinostat)29

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Number of Participants With Adverse Events

Grades 3 & 4 adverse events definitely, probably or possibly related to treatment, graded by the National Cancer Institute Common Terminology Criteria for Adverse Events version 3.0. (NCT00253630)
Timeframe: Up to 3 years

InterventionParticipants (Count of Participants)
ANCAnorexiaFatigueHemoglobinHypokalemiaHyponatremiaHypophosphatemiaInfection -Skin (cellulitis)INRLeukocytes (total WBC)LymphopeniaMyalgiaMucositis/stomatitisPlateletsThrombosis/thrombus/embolism
Treatment (Vorinostat)6134112124511102

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Response Rate

Tumor response is assessed by Response Evaluation Criteria In Solid Tumors (RECIST) version 1.0. Response included complete response (CR) and partial response (PR). CR is defined as the disappearance of all target lesions. PR is defined as at least a 30% decrease in the sum of the longest diameters of target lesions, taking as reference the baseline sum longest diameter. (NCT00258349)
Timeframe: Tumor assessment was obtained at baseline, after 6 weeks (week 6 = last week of Cycle 2), and after every 4 cycles of therapy

Interventionpercentage of participants (Number)
Vorinostat +Trastuzumab0

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Time to Progression

Tumor response is assessed by Response Evaluation Criteria In Solid Tumors (RECIST) version 1.0. Disease progression is defined as at least a 20% increase in the sum of the longest diameters of target lesions, taking as reference the smallest sum longest diameter recorded since the baseline measurements, or the appearance of one or more new lesion(s). Time to progression is defined as time from registration to disease progression. (NCT00258349)
Timeframe: Tumor assessment was obtained at baseline, after 6 weeks (week 6 = last week of Cycle 2), and after every 4 cycles of therapy

Interventionmonths (Median)
Vorinostat +Trastuzumab1.5

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Overall Survival

Overall survival is defined as time from registration to death from any cause. Patients who were alive were censored as the last date of known alive. (NCT00258349)
Timeframe: Survival was assessed every 3 months for first 2 years from protocol entry, then every 6 months until 3 years from study entry

Interventionmonths (Median)
Vorinostat +Trastuzumab9.3

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Change in Tissue Apoptosis After 3 Days of Treatment

Change in cleaved caspase-3 (a marker of tissue apoptosis) by IHC compared to baseline in the treated (19 evaluable samples) or untreated patients (12 evaluable samples) were analyzed between groups. Cleaved caspase-3 is a protein in cells involved in apoptosis (cell death). (NCT00262834)
Timeframe: Baseline and after 3 day of vorinostat

Interventionpercentage of change (Mean)
Vorinostat0
Tissue Only0

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Change in Tissue Histone Acetylation After 3 Days of Treatment

To evaluate change from baseline in tissue histone acetylation in patients with primary breast cancer who received three days of Short Term Oral Suberoylanilide Hydroxamic Acid (SAHA) 300 mg PO bid immediately prior to definitive breast surgery or other primary treatment. This is measured by Cumulative Methylation Index, which is reported as the sum of all %M for all genes. %M= (methylated copies divided by methylated + unmethylated copies) x 100. (NCT00262834)
Timeframe: Baseline and after 3 day of Vorinostat

InterventionCumulative Methylation Index (Number)
Arm I38.3

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Change in Tissue Proliferation After 3 Days of Treatment

Change in Ki-67 (a marker of tissue proliferation) by IHC compared to baseline in the treated (22 evaluable samples) or untreated patients (15 evaluable samples) were analyzed between groups. Ki-67 is a protein in cells that increases as cellsprepare to divide into new cells. A staining process can measure the percentage of tumor cells that are positive for Ki-67. The more positive cells there are, the more quickly they are dividing and forming new cells. (NCT00262834)
Timeframe: After 3 days of vorinostat

Interventionpercentage of change (Mean)
Vorinostat-3
Tissue Only-4

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Number of Participants With Adverse Events

Participants were evaluated for adverse events due to vorinostat to assess if it was safe to give the drug prior to surgery. 17 of 25 participants who received vorinostat experienced at least 1 adverse event believed to be related to the study drug; no adverse events were severe, and the treatment was considered safe. (NCT00262834)
Timeframe: After 3 days of vorinostat

Interventionparticipants (Number)
Vorinostat17

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Objective Response

"Objective response is measured using the international criteria proposed by the Response Evaluation Criteria in Solid Tumors (RECIST) Committee. Changes in only the largest diameter (unidimensional measurement) of the tumor lesions are used in RECIST criteria.~Complete Response (CR) - Disappearance of all target lesions, Partial Response (PR) - at least a 30% decrease in the sum of the longest diameter (LD) of target lesions, Progressive Disease (PD) - At least a 20% increase in the sum of the LD of target lesions, taking as reference the smallest sum LD recorded since the treatment started or the appearance of one or more new lesions, Stable Disease (SD) - Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference the smallest sum LD since the treatment started." (NCT00278395)
Timeframe: 1 year

Interventionparticipants (Number)
Best Objective Response Rate (ORR)Progressive Disease
Vorinostat47

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Time to Treatment Failure (TTF)

Time to treatment failure (TTF) was defined as the time from registration to until the date of treatment discontinuation of any reason. Patients receiving treatment at the time of analysis were considered censored. The median TTF with 95% CI was estimated using the Kaplan Meier method. (NCT00305773)
Timeframe: Duration of treatment (up to 17 cycles)

Interventiondays (Median)
Arm A (Once Daily Vorinostat)42
Arm B (Thrice Daily Vorinostat)46

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Overall Survival (OS)

Overall survival (OS) was defined as the time from registration to death of any cause. Surviving patients were censored at the date of last follow-up. The median OS with 95% CI was estimated using the Kaplan Meier method. (NCT00305773)
Timeframe: Duration of study (up to 2 years)

Interventiondays (Median)
Arm A (Once Daily Vorinostat)105
Arm B (Thrice Daily Vorinostat)153

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Number of Participants With Severe (Grade 3, 4 or 5) Adverse Events

"Adverse events were graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 3.~Description of Grades:~Grade 1: Mild Grade 2: Moderate Grade 3: Severe Grade 4: Life-threatening Grade 5: Death" (NCT00305773)
Timeframe: Duration of study (up to 2 years)

Interventionparticipants (Number)
Arm A (Once Daily Vorinostat)10
Arm B (Thrice Daily Vorinostat)17

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Confirmed Complete Response (CR) Rate

"The confirmed complete response rate was estimated by the number of participants with CR divided by the total number of evaluable participants.~According to the International Working Group (IWG) Criteria for response in AML, to be considered a CR, the following must be met for at least 4 weeks: ANC > 1500/mL, platelets > 100000/mL, no circulating blasts, bone marrow cellularity >20% (biopsy), trilineage maturation, < 5% bone marrow blasts, no auer rods and no extramedullary disease." (NCT00305773)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
Arm A (Once Daily Vorinostat)0
Arm B (Thrice Daily Vorinostat)4.5

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Number of Participants With at Least One Dose Limiting Toxicity Associated With Vorinostat Concurrently Administered With Isotretinoin

Defined as the occurrence of one or more of the following toxicities as graded by the Common Terminology Criteria for Adverse Events (CTCAE) version 3.0 (NCT00324740)
Timeframe: Course 1, up to 28 days

InterventionParticipants (Count of Participants)
Dose Level 1: Vorinostat (300mg) and Isotretinoin (0.25 mg/kg)1
Dose Level 2 Vorinostat (300mg)and Isotretinoin (0.375 mg/kg)0
Dose Level 2 Vorinostat (300mg)and Isotretinoin (0.5 mg/kg)0

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Maximum Tolerated Dose of Vorinostat in Combination With Isotretinoin

Hematologic: Any Grade 3/4 Thrombocytopenia and/or Grade 3/4 Neutropenia Non-Hematologic: Any >/= Grade3 non-hematologic toxicity considered by the investigator to be possibly related to study drug and/or any non-hematologic toxicity that results in a dose-delay of more than three weeks. (NCT00324740)
Timeframe: Once 2 DLT events occur in patients, the preceding dose will be designated the maximum tolerated dose (MTD).

Interventionmg/kg BID (Number)
Treatment (Vorinostat and Isotretinoin)0.5

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Progression-free Survival Assessed by Response Evaluation Criteria for Solid Tumors (RECIST) (Phase II)

Estimated by Kaplan-Meier method (NCT00324870)
Timeframe: At 6 months

Interventionpercent (Number)
Arm I48.6

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Objective Response Rate

Percentage of participants that obtain the best objective response, stable disease. (NCT00330161)
Timeframe: Up to 3 years

Interventionpercentage of participants (Number)
Treatment (Vorinostat)7

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Median Survival

Median overall survival. (NCT00330161)
Timeframe: Up to 3 years

Interventionmonths (Median)
Treatment (Vorinostat)11.7

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Progression-free Survival

Median time to progression was determined. (NCT00330161)
Timeframe: From the start of treatment to time of progression, assessed up to 3 years

Interventionmonths (Median)
Treatment (Vorinostat)2.8

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Incidence of Toxicity

The percentage of eligible participants that experience grade 3 or 4 toxicities. (NCT00330161)
Timeframe: Up to 3 years

Interventionpercentage of participants (Number)
Treatment (Vorinostat)48

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Objective Tumor Response Rate

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI or CT: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR (NCT00363883)
Timeframe: Response assessed after every 2 cycles (6 weeks) up to 26 weeks

Interventionpercentage of patients (Number)
Treatment (Vorinostat)0

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Progression-free Survial

Will be estimated using the product-limit method of Kaplan and Meier. Progression defined using RECIST v1.0 criteria, at least a 20% increase in the sum of the longest diameter of target lesions, or the appearance of one or more new lesions. (NCT00363883)
Timeframe: assessed up to 26 weeks

Interventionmonths (Median)
Treatment (Vorinostat)1.1

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Overall Survival

Will be estimated using the product-limit method of Kaplan and Meier. (NCT00363883)
Timeframe: Up to 26 weeks

Interventionmonths (Median)
Treatment (Vorinostat)4.3

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Number of Participants With Objective Response (OR)

The Objective Response Rate. Response and progression were evaluated in this study using the new international criteria proposed by the Response Evaluation Criteria in Solid Tumors (RECIST). Changes in only the largest diameter (unidimensional measurement) of the tumor lesions are used in the RECIST criteria. For the purposes of this study, patients were evaluated for response every 8 weeks. In addition to a baseline scan, confirmatory scans were also obtained ≥ 4 weeks following initial documentation of objective response. (NCT00365599)
Timeframe: 24 weeks

Interventionparticipants (Number)
Vorinostat and Tamoxifen8

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Number of Participants With Serious Adverse Events (SAEs)

Safety evaluation according to descriptions and grading scales found in the revised NCI Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. (NCT00365599)
Timeframe: 4 years, 7 months

Interventionparticipants (Number)
Vorinostat and Tamoxifen4

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Time to Progression (TTP)

The median response duration in months. Response and progression were evaluated in this study using the new international criteria proposed by the Response Evaluation Criteria in Solid Tumors (RECIST). (NCT00365599)
Timeframe: Up to 30 months

Interventionmonths (Median)
Vorinostat and Tamoxifen10.3

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Overall Survival(OS)

Assessed by Kaplan-Meier survival analysis and 95% confidence intervals will be calculated using Greenwood's formulae. (NCT00368875)
Timeframe: Time from first treatment day until death, assessed up to 12 months

Interventionmonths (Median)
Phase I29.4

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Progression-free Survival (PFS),

Assessed by Kaplan-Meier survival analysis and 95% confidence intervals will be calculated using Greenwood's formulae. (NCT00368875)
Timeframe: From first treatment day until objective or symptomatic progression, assessed up to 12 months

Interventionmonths (Median)
Phase I + Phase II11.9

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Objective Response Rate (CR + PR)

Estimated and a 95% confidence interval will be estimated via binomial proportions. Per Response Evaluation Criteria in Solid Tumors (RECIST) for target lesions and assessed by CT scan: Complete response (CR): Disappearance of all target lesions; Partial Response (PR): >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR+PR. (NCT00368875)
Timeframe: Up to 12 months

Interventionpercentage of participants (Number)
Phase I + Phase II49

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Area Under the Curve (AUC(0-infinity) at Day 21 (400 mg)

Area Under Curve (AUC(0-infinity))=Area under the plasma concentration versus time curve (AUC) from time zero to 24 hours. It is obtained from AUC (0 - 24) plus AUC (24 - ∞) (NCT00373490)
Timeframe: Day 21 (400 mg)

InterventionμM·hr (Geometric Mean)
Vorinostat 400 mg8.3

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Maximum Concentration (Cmax) at Day 21 (400 mg)

(NCT00373490)
Timeframe: Day 21 (400 mg)

InterventionμM (Geometric Mean)
Vorinostat 400 mg2.04

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Maximum Concentration (Cmax) at Day 1 (600 mg and 400 mg)

(NCT00373490)
Timeframe: Day 1 (600 mg and 400 mg)

InterventionμM (Geometric Mean)
Vorinostat 600 mg1.17
Vorinostat 400 mg1.62

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Area Under the Curve (AUC(0-infinity)) at Day 3 (600 mg)

Area Under Curve (AUC(0-infinity))=Area under the plasma concentration versus time curve (AUC) from time zero to 24 hours. It is obtained from AUC (0 - 12) plus AUC (12 - ∞) (NCT00373490)
Timeframe: Day 3 (600 mg)

InterventionμM·hr (Geometric Mean)
Vorinostat 600 mg4.15

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Area Under the Curve (AUC(0-infinity)) at Day 1 (600 mg and 400 mg)

Area Under Curve (AUC(0-infinity))=Area under the plasma concentration versus time curve (AUC) from time zero to extrapolated infinite time (o- ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). At 600 mg, t=12 hours and at 400 mg, t=24 hours. (NCT00373490)
Timeframe: Day 1 (600 mg and 400 mg)

InterventionμM·hr (Geometric Mean)
Vorinostat 600 mg3.94
Vorinostat 400 mg7.75

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Number of Participants With a Dose Limiting Toxicity (DLT)

Dose Limiting Toxicity = Drug-related side effects that are serious enough to prevent an increase in dose or level of that treatment (NCT00373490)
Timeframe: 21 Days (first cycle)

InterventionParticipants (Number)
Vorinostat 600 mg0
Vorinostat 400 mg2

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Maximum Concentration (Cmax) at Day 3 (600 mg)

(NCT00373490)
Timeframe: Day 3 (600 mg)

InterventionμM (Geometric Mean)
Vorinostat 600 mg1.32

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Maximum Tolerated Dose of Vorinostat Administered in Combination With Standard Doses of Gemcitabine Plus Either Cisplatin or Carboplatin in Patients With Advanced Stage Non-Small Cell Lung Cancer Who Have Not Received Chemotherapy for Advanced Disease

"Maximum tolerated dose (MTD) was defined as the highest dose level in which fewer than 2 patients among the first 6 enrolled experience a DLT (as defined in Outcome Measure 1) during the first cycle of treatment.~The MTD was 400 mg for up to 10 days in 21-day cycles." (NCT00423449)
Timeframe: every 21 days (every cycle), up to 126 days (6 cycles)

Interventionmg (Number)
All Participants400

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Number of Participants With Dose-limiting Toxicities (DLT) Due to Vorinostat Administered in Combination With Standard Dose of Gemcitabine Plus Either Cisplatin or Carboplatin

DLT = any Common Terminology Criteria for Adverse Events Grade 3/4 drug related non-hematologic toxicity EXCEPT Grade 3 nausea/vomiting responsive to therapy, Grade 3 Fatigue responsive to management, transient electrolyte disorders that were corrected, any Grade 4 drug related hematologic toxicity EXCEPT lymphopenia/neutropenia, unless the neutropenia was febrile and/or was an infection requiring treatment, OR Any Grade 4 neutropenia lasting >=7 days, failure of absolute neutrophil count or platelets to recover, or any drug-related AE that led to a dose reduction of >=1 study drugs. (NCT00423449)
Timeframe: every 21 days (every cycle), up to 126 days (6 cycles)

InterventionParticipants (Number)
Vorinostat 300 7/21+ Gemcitabine 1000 + Cisplatin0
Vorinostat 300 7/21+ Gemcitabine 1250 + Cisplatin1
Vorinostat 400 7/21+ Gemcitabine 1250 + Cisplatin0
Vorinostat 400 10/21+ Gemcitabine 1250 + Cisplatin0
Vorinostat 400 14/21+ Gemcitabine 1250 + Cisplatin1

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Number of Participants With Laboratory Adverse Experiences (Safety and Tolerability)

"An adverse experience was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the sponsor's product, whether or not considered related to the use of the product. Any worsening (any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the sponsor's product, was also an adverse experience.~The AEs could have been any grade from 1 to 5 in severity (mild, moderate, severe, life-threatening, death, respectively)." (NCT00423449)
Timeframe: every 21 days (every cycle), up to 126 days (6 cycles)

InterventionParticipants (Number)
Vorinostat 300 7/21+ Gemcitabine 1000 + Cisplatin2
Vorinostat 300 7/21+ Gemcitabine 1250 + Cisplatin4
Vorinostat 400 7/21+ Gemcitabine 1250 + Cisplatin7
Vorinostat 400 10/21+ Gemcitabine 1250 + Cisplatin13
Vorinostat 400 14/21+ Gemcitabine 1250 + Cisplatin2

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Number of Participants With Clinical Adverse Experiences (Safety and Tolerability)

"An adverse experience (AE) was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the sponsor's product, whether or not considered related to the use of the product. Any worsening (any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the sponsor's product, was also an adverse experience.~The AEs could have been any grade from 1 to 5 in severity (mild, moderate, severe, life-threatening, death, respectively)." (NCT00423449)
Timeframe: every 21 days (every cycle), up to 126 days (6 cycles)

InterventionParticipants (Number)
Vorinostat 300 7/21+ Gemcitabine 1000 + Cisplatin4
Vorinostat 300 7/21+ Gemcitabine 1250 + Cisplatin6
Vorinostat 400 7/21+ Gemcitabine 1250 + Cisplatin17
Vorinostat 400 10/21+ Gemcitabine 1250 + Cisplatin27
Vorinostat 400 14/21+ Gemcitabine 1250 + Cisplatin7

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Number of Participants With a Dose Limited Toxicity at First Cycle

Dose Limited Toxicity = Drug-related side effects that are serious enough to prevent an increase in dose or level of that treatment. (NCT00424775)
Timeframe: 25 Days (first cycle)

InterventionParticipants (Number)
Vorinostat (300 mg)3

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Area Under the Curve (AUC(0-24 hr)) at Day 4

Area Under the Curve (AUC (0-24 hr)) = Area under the plasma concentration versus time curve (AUC) from time zero to 24 hour. (NCT00424775)
Timeframe: Day 4

InterventionµM hr (Mean)
Vorinostat (300 mg)9.76

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Area Under the Curve (AUC(0-24 hr)) at Day 5

Area Under the Curve (AUC (0-24 hr)) = Area under the plasma concentration versus time curve (AUC) from time zero to 24 hour. (NCT00424775)
Timeframe: Day 5

InterventionµM hr (Mean)
Vorinostat (300 mg)6.26

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Maximum Concentration (Cmax) at Day 4

Maximum Concentration (Cmax) = the maximum plasma concentration of the drug (NCT00424775)
Timeframe: Day 4

InterventionµM (Mean)
Vorinostat (300 mg)1.54

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Maximum Concentration (Cmax) at Day 5

Maximum Concentration (Cmax) = the maximum plasma concentration of the drug (NCT00424775)
Timeframe: Day 5

InterventionµM (Mean)
Vorinostat (300 mg)1.96

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Overall Survival

Defined as the time from date of randomization to death due to any cause. Patients without documented death at the time of the final analysis will be censored at the date of the last follow-up. (NCT00473889)
Timeframe: Start of treatment to death

InterventionMonths (Median)
Vorinostat + Paclitaxel + Carboplatin11.0
Placebo + Paclitaxel + Carboplatin14.0

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Progression Free Survival

Defined as the time from randomization to the first documented disease progression or death due to any cause, whichever occurs first. Disease progression is defined as at least a 20% increase in sum of the longest diameter of all target lesions, the appearance of a new lesion, or an increase in non-target lesions. (NCT00473889)
Timeframe: Start of treatment to disease progression or death

InterventionMonths (Median)
Vorinostat + Paclitaxel + Carboplatin4.3
Placebo + Paclitaxel + Carboplatin5.5

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Number of Participants Who Had a Disease Response to Treatment

Response to treatment is defined as a complete response (CR) or partial response (PR) to treatment. Confirmation of response required a second assessment performed at least 4 weeks after the initial assessment. (PR is defined as at least a 30% reduction in sum of the longest diameter of all target lesions and no increase in non-target lesions). (NCT00473889)
Timeframe: Every 42 days from start of treatment until disease response

,
InterventionParticipants (Number)
ResponderNon-Responder
Placebo + Paclitaxel + Carboplatin3687
Vorinostat + Paclitaxel + Carboplatin2897

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Number of Participants Experiencing Dose Limiting Toxicity (DLT) Events

Participants who received at least one dose of vorinostat in combination with decitabine intravenous (IV) at a dose of 20 mg/m^2 daily for 5 days along with oral vorinostat 400 mg once daily for 7 to 14 days in a 28-day cycle concurrently or sequentially, were evaluated to determine the maximum tolerable dose (MTD) determined by the number of participants experiencing dose limiting toxicity (DLT) events defined as any Grade 3 or 4 non-hematological toxicity (reported adverse event) and/or myelosuppression lasting >42 days. (NCT00479232)
Timeframe: Day 1 to 28 of Cycle 1

Interventionparticipants (Number)
Concurrent, Vorinostat 400mg qd x 7d/4wk + Decitabine0
Concurrent, Vorinostat 400mg qd x 7d/2wk + Decitabine0
Concurrent, Vorinostat 400mg qd x 14d/4wk + Decitabine (MTD)0
Sequential, Vorinostat 400mg qd x 7d/4wk + Decitabine0
Sequential, Vorinostat 400mg qd x 10d/4wk + Decitabine0
Sequential, Vorinostat 400mg qd x 14d/4wk + Decitabine (MTD)1

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Objective Response Rate in Participants Treated With Vorinostat + Decitabine With Intermediate-high Risk Myelodysplastic Syndrome (MDS) or Untreated Acute Myelogenous Leukemia (AML)

Objective Response Rate was measured in participants with intermediate-high risk MDS or untreated AML who were treated with vorinostat and decitabine either on a concurrent or sequential regimen. The Objective response was defined as any confirmed complete remission or any confirmed partial remission for AML participants and complete remission, confirmed partial remission or confirmed hematologic improvement for MDS participants. (NCT00479232)
Timeframe: Approximately 6 months

Interventionpercentage of participants (Number)
Untreated AML or Intermediate, Concurrent35.0
Untreated AML or Intermediate, Sequential13.6

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Objective Response Rate in Participants Treated With Vorinostat + Decitabine With Refractory or Relapse Acute Myelogenous Leukemia (AML)

Objective Response Rate was measured in participants with refractory or relapse AML (acute myelogenous leukemia) in combination with Decitabine who were treated with vorinostat and decitabine on either a concurrent or sequential regimen. The Objective response was defined as any confirmed complete remission or any confirmed partial remission for AML participants and complete remission, confirmed partial remission or confirmed hematologic improvement for Myelodysplastic Syndrome (MDS) participants. (NCT00479232)
Timeframe: Approximately 6 months

Interventionpercentage of participants (Number)
Refractory or Relapsed AML, Concurrent7.1
Refractory or Relapsed AML, Sequential0.0

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Response Rate

"Each patient will be assigned one of the following categories: 1) complete response, 2) partial response, 3) stable disease, 4) progressive disease, 5) early death from malignant disease, 6) early death from toxicity, 7) early death because of other cause, or 9) unknown (not assessable, insufficient data).~Patients with confirmed CR or PR according to the RECIST criteria were considered to have responded to treatment." (NCT00481078)
Timeframe: Assessed every two cycles

Interventionpercentage of responding patients (Number)
Arm I (Vorinostat, Paclitaxel, Carboplatin)34
Arm II (Placebo, Paclitaxel, Carboplatin)12.5

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Progression-free Survival

Evaluated using the Kaplan-Meier method. Compared between arms using the log-rank test. (NCT00481078)
Timeframe: Up to 1 year

InterventionMonths (Median)
Arm I (Vorinostat, Paclitaxel, Carboplatin)6
Arm II (Placebo, Paclitaxel, Carboplatin)4.1

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Overall Survival

Evaluated using the Kaplan-Meier method. Compared between arms using the log-rank test. (NCT00481078)
Timeframe: Up to 1 year

InterventionMonths (Median)
Arm I (Vorinostat, Paclitaxel, Carboplatin)13
Arm II (Placebo, Paclitaxel, Carboplatin)9.7

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Number of Responders and Number of Non-responders Defined by International Working Group Response Criteria

Number of responders is defined as the number of patients in the analysis population who have complete response (CR), partial response (PR), or hematologic improvement (HI) per International Working Group Response Criteria during the course of the study. Confirmation of CR or PR will require a second assessment performed 4 weeks or more after the initial assessment. Confirmation of HI will require a second assessment performed 8 weeks or more after the initial assessment. Number of non-responders is defined as the number of patients who did not achieve CR, PR or HI in the study. (NCT00486720)
Timeframe: 2 Years

,
InterventionParticipants (Number)
ResponderNon-responder
Vorinostat Once Daily Dose Schedule09
Vorinostat Thrice Daily Dose Schedule012

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Safety and Tolerability as Assessed by the Number of Participants With Adverse Events.

(NCT00486720)
Timeframe: Every 21 days while on therapy and at 30 days after the last dose of study therapy

,
InterventionParticipants (Number)
With one or more adverse eventsWith no adverse eventsWith drug-related adverse eventsWith serious adverse eventsWith serious drug-related adverse events
Vorinostat Once Daily Dose Schedule90420
Vorinostat Thrice Daily Dose Schedule1201152

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Duration of Response

Median follow up of living patients (NCT00561418)
Timeframe: Up to 5 years

Interventionmonths (Median)
Vorinostat (SAHA)23.2

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Clinical Benefit

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT00561418)
Timeframe: Up to 3 years

Interventionpatients (Number)
Complete Response (CR)Partial Response (PR)Stable Disease(SD)Not evaluable
Vorinostat (SAHA)13325

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Safety and Tolerability of Vorinostat (SAHA) After Autologous Stem Cell Transplantation

NCI CTCAE version 3.0 was used to assess Adverse Events (AE) Grade 1=Mild AE Grade 2=Moderate AE Grade 3=Severe AE Grade 4=Life-threatening or disabling AE (NCT00561418)
Timeframe: Up to 3 years

Interventionpatients (Number)
Fatigue (Grade 1, 2)Lymphopenia (Grade 1-4)Thrombocytopenia (Grade 1-3)Leukopenia (Grade 1-3)Anemia (Grade 1-3)
Vorinostat (SAHA)1211111010

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Pathological Complete Response (CR) Rate in Patients With Her2/Neu Positive Locally Advanced Breast Cancer.

Pathological Complete Response (CR) defined as absence of invasive cancer at surgery (NCT00574587)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Stratum A (HER2-positive)13
Stratum B: Triple Negative4
Stratum C: ER-Positive, HER2-negative0

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Levels of Testosterone in Blood From Radical Prostatectomy Specimens

(NCT00589472)
Timeframe: Up to 1 year

Interventionng/dL (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)319

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Levels of PSA in Blood From Radical Prostatectomy Specimens

(NCT00589472)
Timeframe: Up to 1 year

Interventionng/mL (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)9.44

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Levels of DHT in Blood From Radical Prostatectomy Specimens

(NCT00589472)
Timeframe: Up to 1 year

Interventionng/dL (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)24

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Gleason Score

A Gleason score is the sum of two numbers. Pathologist determines where the cancer is most prominent and assigns the primary grade, the secondary grade is assigned based on where the cancer is next most prominent. A score from one to five is assigned for each area based on how aggressive the tumor appears. A tumor with cell that appear close to normal is assigned a low Gleason score (six or below). A tumor with cells that appear clearly different from those of a normal prostate is assigned a high Gleason score (seven or above). A system of grading prostate cancer tissue based on how it looks under a microscope. Gleason scores range from 2 to 10 and indicate how likely it is that a tumor will spread. A low Gleason score means the cancer tissue is similar to normal prostate tissue and the tumor is less likely to spread; a high Gleason score means the cancer tissue is very different from normal and the tumor is more likely to spread. (NCT00589472)
Timeframe: Baseline

Interventionunits on a scale (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)8

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Levels of DHEA in Blood From Radical Prostatectomy Specimens

(NCT00589472)
Timeframe: Up to 1 year

Interventionng/dL (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)256

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Levels of DHEA-S in Blood From Radical Prostatectomy Specimens

(NCT00589472)
Timeframe: Up to 1 year

Interventionmcg/dL (Median)
Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy)90

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Efficacy (Response Rate) of Vorinostat Combined With RICE Chemotherapy

(NCT00601718)
Timeframe: 3-5 weeks post end of treatment

InterventionParticipants (Count of Participants)
Treatment (Enzyme Inhibitor, Monoclonal Antibody, Chemotherapy19

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Ability to Proceed to Peripheral Blood Stem Cell Collection Following Treatment

(NCT00601718)
Timeframe: 1-3 weeks post end of treatment

InterventionParticipants (Count of Participants)
Treatment (Enzyme Inhibitor, Monoclonal Antibody, Chemotherapy20

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Maximum Tolerated Dose of Vorinostat

(NCT00601718)
Timeframe: 28 days post last dose of study drug

Interventionmg twice daily X 5 days (Number)
Treatment (Enzyme Inhibitor, Monoclonal Antibody, Chemotherapy500

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Safety and Toxicity According to CTCAE v3.0

Common dose limiting toxicities. (NCT00601718)
Timeframe: 3-5 weeks post end of treatment

InterventionParticipants (Count of Participants)
InfectionHypokalemiaTransaminitisGrade 3 related gastrointestinal toxicity
Treatment (Enzyme Inhibitor, Monoclonal Antibody, Chemotherapy2229

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Change in Standard Uptake Value (SULmax) From Baseline to Day 15 on FDG-PET

Change in standard uptake value (SULmax) as measured by percentage reduction of SULmax. The standard uptake value used for the PET analysis was SULmax, which is the standard uptake value normalized for lean body mass. (NCT00616967)
Timeframe: Baseline and day 15

Interventionpercentage reduction in SULmax (Median)
Responders63
Non-Responders32.9

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Cumulative Methylation Index (CMI) at Day 15

(NCT00616967)
Timeframe: Day 15

InterventionCMI (Median)
Responders10
Non-Responders44

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Number of Participants Who Experience Death During Treatment

(NCT00616967)
Timeframe: Up to 12 weeks

InterventionParticipants (Count of Participants)
Run-in Phase (Arm 0)0
Placebo (Arm I)0
Vorinostat (Arm II)0

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Number of Participants With Clinical Complete Response (cCR)

cCR in the breast on physical is defined as the absence of any palpable abnormality on breast exam Iie: no skin or breast thickening, mass or associated skin or nipple changes) (NCT00616967)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Placebo (Arm I)16
Vorinostat (Arm II)15

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Safety as Measured by Number of Participants Who Experience Adverse Events

Number of participants who experience adverse events as defined by NCI CTCAE version 3.0 (NCT00616967)
Timeframe: up to 30 days post-treatment

InterventionParticipants (Count of Participants)
Run-in Phase (Arm 0)6
Placebo (Arm 1)31
Vorinostat (Arm 2)31

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Change in Cumulative Methylation Index (CMI)

Change of CMI from baseline to Day 15 (D15), defined as log(D15 CMI + 1/baseline CMI + 1). The CMI was calculated as a sum of all gene-specific methylation indexes within a panel of 10 genes which included: HIST1H3C, AKR1B1, GPX7, HOXB4, TMEFF2, RASGRF2, COL6A2, ARHGEF7, TM6SF1, and RASSF1A. (NCT00616967)
Timeframe: Change from baseline to Day 15

InterventionCMI (Median)
Tissue CMI change from baselineSerum CMI change from baseline
Combined Arm I and Arm II140

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Pathological Complete Response (pCR) Rate

The primary end point was pCR, defined as no viable invasive cancer in breast and axilla. All other cases were defined as non-pCR. The pCR rate was determined in each arm separately by performing an intent-to-treat (ITT) analysis of all randomized patients. Patients with unknown pCR status were considered non-responders. Computation of associated 90% confidence intervals did not account for the sequential design. (NCT00616967)
Timeframe: Time of breast cancer surgery

InterventionParticipants (Count of Participants)
Arm I9
Arm II8

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Absolute Change From Baseline in Ki-67

(NCT00616967)
Timeframe: Change from baseline to Cycle 1-Day 15

Interventionpercent change in Ki-67 (Mean)
Responders7.0
Non-Responders12.0

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Change From Baseline in QTcF at 1 Hour

Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 1 hour

Interventionmilliseconds (Mean)
Vorinostat0.22
Placebo-1.23

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Change From Baseline in QTcF at 0.5 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 0.5 hours

Interventionmilliseconds (Mean)
Vorinostat1.78
Placebo-1.22

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Change From Baseline in QTcF at 12 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 12 hours

Interventionmilliseconds (Mean)
Vorinostat1.35
Placebo-1.31

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Change From Baseline in QTcF at 2 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 2 hours

Interventionmilliseconds (Mean)
Vorinostat1.09
Placebo-1.98

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Change From Baseline in QTcF at 3 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 3 hours

Interventionmilliseconds (Mean)
Vorinostat1.32
Placebo-1.52

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Change From Baseline in QTcF at 4 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The placebo-corrected change from baseline in QTcF was calculated by subtracting the QTcF change from baseline for placebo at each timepoint from the QTcF change from baseline for vorinostat at each timepoint. (NCT00632931)
Timeframe: Baseline and 4 hours

Interventionmilliseconds (Mean)
Vorinostat4.95
Placebo-1.49

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Change From Baseline in QTcF at 8 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 8 hours

Interventionmilliseconds (Mean)
Vorinostat-3.56
Placebo-7.89

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Change From Baseline in QTcF at 24 Hours

The Fridericia correction of the QT interval (QTcF) was determined at each time point from five replicate measurements. The change from baseline in QTcF was calculated by subtracting the QTcF value at each timepoint from the QTcF baseline (predose) value. (NCT00632931)
Timeframe: Baseline and 24 hours

Interventionmilliseconds (Mean)
Vorinostat1.53
Placebo-4.89

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Overall Survival

Estimated using Kaplan-Meier survival curve. (NCT00641706)
Timeframe: From study registration to date of death due to any cause or last follow-up (up to 5 years)

Interventionmonths (Median)
Arm A (Not Undergoing Surgery)3.2
Arm B (Undergoing Surgery)8.7

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Proportion of Confirmed Tumor Response Defined as an Objective Status of Confirmed Response (CR), Partial Response (PR), or Regression (REGR) on Two Consecutive Evaluations

"Confidence intervals for the true proportion will be calculated using the exact binomial method.~Measurable patients must achieve at least a 50% reduction in the product of perpendicular diameters of contrast enhancement or mass with no new lesions with the patient being on stable or decreased steroid dose.~Evaluable patients must achieve unequivocal reduction in size of contrast-enhancement or decrease in mass effect as agreed upon independently by primary physician and quality control physicians; no new lesions. Patient should be on stable or decreased steroid dose." (NCT00641706)
Timeframe: Assessed up to 5 years

Interventionproportion of patients (Number)
Arm A (Not Undergoing Surgery)0.027

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Time to Progression

Estimated using Kaplan-Meier survival curve. Patients who died were considered to have disease progression at the time of death unless there was documented evidence that no progression occurred before death. For patients with bidimensionally measurable disease (measurable disease), progression is defined as > 25% increase in product of perpendicular diameters of contrast enhancement or mass or appearance of new lesions. For patients without bidimensionally measurable disease (evaluable disease), progression is defined as unequivocal increase in size of contrast enhancement or increase in mass effect as agreed upon independently by primary physician and quality control physicians or appearance of new lesions. (NCT00641706)
Timeframe: From study registration to date of progression (up to 5 years)

Interventionmonths (Median)
Arm A (Not Undergoing Surgery)1.5
Arm B (Undergoing Surgery)4.2

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Progression-free Survival at 6 Months

Estimated using the Binomial point estimator (number of successes divided by the total number of evaluable patients). A patient is classified as a success if alive and progression-free at 6 months. For patients with bidimensionally measurable disease (measurable disease), progression is defined as > 25% increase in product of perpendicular diameters of contrast enhancement or mass or appearance of new lesions. For patients without bidimensionally measurable disease (evaluable disease), progression is defined as unequivocal increase in size of contrast enhancement or increase in mass effect as agreed upon independently by primary physician and quality control physicians or appearance of new lesions. (NCT00641706)
Timeframe: At 6 months

Interventionpercentage of patients (Number)
Arm A (Not Undergoing Surgery)0
Arm B (Undergoing Surgery)29

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Number of Participants Experiencing Dose-Limiting Toxicities (DLTs)

DLTs consisted of hematologic or non-hemtologic toxicities. Hematologic DLT was any grade (gr) 4 neutropenia lasting ≥7 days, gr 4 thrombocytopenia or gr 5 hematologic toxicity. Non-hematologic DLT was any gr 3, 4 or 5 non-hematologic toxicity with the exception of (1) gr 3 nausea, vomiting, diarrhea or dehydration not compliant with medical care, lasting <48 hours (2) gr 3 acidosis/alkalosis returning to ≤ gr 2 by 48 hours of medical care (3) gr 3 liver function test elevation without symptoms, lasting ≤5 days (4) Gr 3 amylase elevation without symptoms (5) Gr 3 hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia or hyphosphatemia responding to medical care (6) Gr 3 hypercholeresterolemia or hypertriglyceridemia. A drug-related AE causing dose modification of study drug is also considered a DLT. Per protocol DLTs were analyzed in the first 28-day treatment cycle. The number of participants experiencing DLTs is reported here for all participants who got ≥1 dose of study drug. (NCT00642954)
Timeframe: Cycle 1 (Up to 28 days)

InterventionParticipants (Count of Participants)
Level 1: Vorinostat 300 mg + Lenalidomide 10 mg0
Level 2: Vorinostat 400 mg + Lenalidomide 10 mg0
Level 3: Vorinostat 400 mg + Lenalidomide 15 mg0
Level 4: Vorinostat 400 mg + Lenalidomide 20 mg0
Level 5: Vorinostat 400 mg + Lenalidomide 25 mg1

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Number of Participants Experiencing Best Overall Response Determined by Complete Response (CR), Near Complete Response (NCR), Very Good Partial Response (VGPR), Partial Response (PR), Minimal Response (MR), Stable Disease (SD) or Progressive Disease (PD)

Best overall tumor response consisted of CR (negative M-protein immunofixation [IF], <5% bone marrow [BM] plasma cells, no soft tissue plasmacytomas [STP]), NCR (positive M-protein IF, <5% BM plasma cells, no STP), VGPR (≥90% M-protein decrease, <5% BM plasma cells, no STP), PR (≥50% M-protein, BM plasma cells, STP decrease), MR (25-49% M-protein, BM plasma cells, STP decrease), SD (<25% decrease-25% increase in M-protein, BM plasma cells; <25% decrease-increase in definite STP) or PD (≥25% M-protein, BM plasma cells increase; new STP, lesions). Per protocol participants experiencing best overall response by CR, NCR, VGPR, PR, MR, SD or PD were analyzed as a single prespecified analysis at the time of protocol-specified final statistical analysis with a 3-Sep-2012 data cut-off. The number of participants experiencing best overall response by CR, NCR, VGPR, PR, MR, SD or PD is reported here for all participants who got ≥1 dose of study drug and had a post baseline efficacy assessment. (NCT00642954)
Timeframe: Up to ~55 months (through pre-specified final statistical analysis cut-off date of 3-Sep-2012)

,,,,
InterventionParticipants (Count of Participants)
CRNCRVGPRPRMRSDPD
Level 1: Vorinostat 300 mg + Lenalidomide 10 mg0011011
Level 2: Vorinostat 400 mg + Lenalidomide 10 mg0101011
Level 3: Vorinostat 400 mg + Lenalidomide 15 mg0000111
Level 4: Vorinostat 400 mg + Lenalidomide 20 mg0011001
Level 5: Vorinostat 400 mg + Lenalidomide 25 mg1025251

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Progression Free Survival (PFS) at 7 Months

Progression-free survival defined as time from date of randomization to first occurrence of having documented disease progression or death due to any cause, whichever comes first. Progression based on tumor assessments according to Response Evaluation Criteria in Solid Tumors (RECIST). Participants were followed from baseline to disease progression with PFS evaluation at 7 months. (NCT00656617)
Timeframe: PFS Evaluation at 7 months

Interventionpercentage of participants (Number)
Idarubicin + Ara-C + Vorinostat65

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Participant Response

Number of participants with response assessed according RECIST: Complete Response (CR) defined as normalization of marrow (< 5% blasts) and of peripheral blood counts (neutrophil count > 1.109/L, platelet count > 100 x 109/L). Partial response (PR) defined as for CR in terms of peripheral counts but with reduction of marrow blasts by >50% compared to pretreatment values but above <5%. Complete Response without platelet recovery (CRp) = CR, but platelets <100 x 109/L. Progressive disease (PD) defined as increase of blasts to > 10% after an initial response. (NCT00656617)
Timeframe: Monitoring with each 4 week cycle, up to 18 cycles of treatment

Interventionparticipants (Number)
Complete Response (CR)Partial Response (PR)Complete Response without platelet recovery (CRp)Progressive Disease (PD)No response
Idarubicin + Ara-C + Vorinostat67011024

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Radiological Response Rate as Assessed by CT

Count of participants with stable disease or partial response. Patients were evaluated for treatment response per RECIST criteria (version 1.0). (NCT00662311)
Timeframe: 12 weeks post-treatment, then every 3 months for 2 years, and then every 6 months for a year thereafter

InterventionParticipants (Count of Participants)
12 Weeks6 Months9 Months12 Months15 Months18 Months21 Months24 Months27 Months33 Months39 Months
Vorinostat 200 mg43311111100

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Safety and Toxicity of Vorinostat at the MTD as Assessed by NCI CTCAE Version 3.0

Count of participants with a grade 3 or higher toxicity. Toxicities were assessed using the NCI CTCAE (v3.0). Grade 3 or higher toxicities were considered worse. (NCT00662311)
Timeframe: Weekly during treatment, 30 days post-treatment, and 12 weeks post-treatment

InterventionParticipants (Count of Participants)
Vorinostat 200 mg4

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Progression-free Survival

Kaplan-Meier estimate. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0). (NCT00662311)
Timeframe: 1 year

Interventionprogression free survival probability (Number)
Vorinostat 200 mg0.20

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MTD of Vorinostat When Administered in Combination With Paclitaxel and Radiotherapy Therapy as Assessed by NCI Common Toxicity Criteria for Adverse Events (CTCAE) Version 3.0 (Phase I)

Defined as the highest dose level at which no more than 1 of 6 patients experiences dose-limiting toxicity (DLT). Toxicity was graded according to the National Institutes of Health Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. A DLT was defined as any Grade 3 or higher non-hematologic adverse event with the exception of alopecia, fatigue, or anorexia. Nausea and/or vomiting that persisted > 48 hours despite optimal medical management at grade 3 or higher was considered a DLT. Hematologic dose-limiting toxicity was defined as either: Grade 4 neutropenia lasting for ≥ 7 days in duration, Grade > 3 febrile neutropenia with/without infection, Grade 4 thrombocytopenia or Grade 5 hematologic toxicity. (NCT00662311)
Timeframe: 8 weeks

Interventionmg (Number)
Vorinostat 200 mgNA

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Overall Survival

Kaplan-Meier estimate (NCT00662311)
Timeframe: 1 year

Interventionsurvival probability (Number)
Vorinostat 200 mg0.60

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Duration of Response

(NCT00662311)
Timeframe: Up to 3 years

Interventionmonths (Median)
Vorinostat 200 mg10

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Complete Response Rate to Rituximab and a Combination of Vorinostat With Cyclophosphamide, Etoposide, and Prednisone in Elderly Pts With Relapsed Diffuse Large B-cell Lymphoma Who Aren't Candidates for Autologous Stem Cell Transplantation.

"Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR., or similar definition that is accurate and appropriate." (NCT00667615)
Timeframe: through study completion, an average of 1 year

Interventionpercentage of participants with CR (Number)
Relapsed or Refractory Diffuse Large B-cell Lymphoma32

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Maximum Tolerated Dose (MTD) of Vorinostat Given Orally for 10 Days in Combination With Cyclophosphamide, Etoposide, Prednisone and Rituximab for Elderly Patients With Relapsed Diffuse Large B-cell Lymphoma

Maximum Tolerated Dose (MTD) of Vorinostat reflects the highest dose of Ridaforolimus and Vorinostat that did not cause a new Grade 2 toxicity in >= 50% of participants (NCT00667615)
Timeframe: through study completion, an average of 1 year

Interventionmg/m2 (Number)
Relapsed or Refractory Diffuse Large B-cell Lymphoma300

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Number of Participants Alive at Day 30 (Poor-risk Group)

(NCT00673153)
Timeframe: At day 30

InterventionParticipants (Count of Participants)
Arm I8

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Relapse-free Survival (Good- and Poor-risk Group)

(NCT00673153)
Timeframe: At relapse

InterventionParticipants (Count of Participants)
Arm I7

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Number of Participants Achieving CR or CRi With Induction Therapy (Good-risk Group)

(NCT00673153)
Timeframe: after completion of induction therapy, administered every 21-42 days for up to two courses

InterventionParticipants (Count of Participants)
Arm I6

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Number of Participants Achieving CR or CRi With Induction Therapy (Poor-risk Group)

(NCT00673153)
Timeframe: after completion of induction therapy, administered every 21-42 days for up to two courses

InterventionParticipants (Count of Participants)
Arm I1

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Number of Participants Alive at Day 30 (Good-risk Group)

(NCT00673153)
Timeframe: At day 30

InterventionParticipants (Count of Participants)
Arm I20

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The Maximum Tolerated Dose (MTD) of Niacinamide in the Combination of Vorinostat and Niacinamide

(NCT00691210)
Timeframe: 3 years

Interventionmg/kg (Number)
Vorinostat (SAHA) and Niacinamide: Level 1-5100

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The Greatest Number of Cycles Received in Each Treatment Group

The highest number of cycles received by an individual participant in the treatment groups. Each cycle was 21 days long. (NCT00691210)
Timeframe: up to 45 weeks

Interventioncycles (Number)
Vorinostat (SAHA) and Niacinamide: Level 19
Vorinostat (SAHA) and Niacinamide: Level 212
Vorinostat (SAHA) and Niacinamide: Level 315
Vorinostat (SAHA) and Niacinamide: Level 410
Vorinostat (SAHA) and Niacinamide: Level 514
Vorinostat, Niacinamide and Etoposide: Level 13
Vorinostat, Niacinamide and Etoposide: Level 24

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Best Response

Number of participants per category: Partial Response (PR), Stable Disease (SD), Progressive Disease (PD). PR: Regression of measurable disease and no new sites. SD: Failure to attain Complete Response (CR), /PR or PD. Relapsed or Progressive Disease: Any new lesion or increase by ≥ 50% of previously involved sites from nadir. (NCT00703664)
Timeframe: Up to 9 years

,,
InterventionParticipants (Count of Participants)
Partial ResponseStable DiseaseProgressive Disease
Cohort A - MCL757
Cohort B - MCL022
Cohort C - DLBCL3823

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Progression-free Survival (PFS)

Median progression-free survival in months per cohort. (NCT00703664)
Timeframe: Up to 9 years

Interventionmonths (Median)
Cohort A - MCL7.6
Cohort C - DLBCL1.8

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Duration of Partial Response

Median duration of response per cohort. (NCT00703664)
Timeframe: Up to 9 years

Interventionmonths (Median)
Cohort A - MCL4.2
Cohort C - DLBCL2.1

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Duration of Stable Disease

Median duration of stable disease per cohort. (NCT00703664)
Timeframe: Up to 9 years

Interventionmonths (Median)
Cohort A - MCL3.8
Cohort B - MCL3.8
Cohort C - DLBCL1.3

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Overall Response Rate (ORR)

ORR: Complete Response (CR) + Partial Response (PR) assessed according to the Revised Response Criteria for Malignant Lymphoma. (NCT00703664)
Timeframe: Up to 9 years

Interventionpercentage of participants (Number)
Cohort A - MCL31.8
Cohort B - MCL0
Cohort C - DLBCL7.7

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Overall Response Rate (Complete and Partial Response)

Response was assessed according to the 2007 Cheson criteria using CT scans or PET: Complete Response (CR), Disappearance of all evidence of disease; Partial Response (PR), >=50% decrease in the Sum of the Product of Diameters (SPD) of up to 6 largest dominant masses and no increase in the size of other nodes; Overall Response (OR) = CR + PR. (NCT00720876)
Timeframe: After every 3 cycles, up to 1 year after the start of treatment

Interventionpercentage of participants (Number)
Vorinostat and Rituximab46

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Progression-free Survival

ProgressionRelapse is defined using the 2007 Cheson criteria, as appearance of any new lesion more than 1.5 cm in any axis during or at the end of therapy; or at least a 50% increase for nadir in the SPD of any previously involved nodes; or at least a 50% increase in the longest diameter of any singe previously identified node more than 1 cm in its short axis. Estimated using the product-limit method of Kaplan and Meier. (NCT00720876)
Timeframe: Until disease progress elapse, up to 1 year after the start of treatment

InterventionMonths (Median)
Vorinostat and Rituximab29.2

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Number of Participants With Grade 3 and 4 Toxicities

Grade 3 & 4 toxicities at least possible related to study drugs during any cycle of treatment. Toxicity graded according to Common Terminology Criteria for Adverse Events version 3.0. (NCT00720876)
Timeframe: 3 weeks after the stop of treatment

InterventionParticipants (Count of Participants)
Neutrophil count decreasedPlatelet count decreasedHemoglobin decreasedLymphocyte count decreasedHypotensionChillsFatigueDehydrationDiarrheaKidney infectionPneumoniaSepsisUrinary tract infectionLocalized edemaAlanine aminotransferase increasedAspartate aminotransferase increasedBlood glucose increasedSerum phosphate decreasedSerum potassium decreasedMuscle weaknessSyncopeHypoxiaPneumonitisThrombosisVascular access complication
Vorinostat and Rituximab3517219311211111332111141

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Time to Tumor Progression (Phase II)

Progression free survival time will be defined from date of registration to date of progression or death. (NCT00731731)
Timeframe: Up to 5 years

Interventionmonths (Median)
Phase II8.05

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Incidence of Adverse Events, as Per NCI CTCAE Version 3.0 (Phase II)

"The maximum grade for each type of treatment-related adverse event will be recorded for each patient, and frequency tables for each arm will be reviewed to determine patterns. In addition, we will review all adverse event data that is graded as 3, 4, or 5 and classified as either unrelated or unlikely to be related to study treatment in the event of an actual relationship developing." (NCT00731731)
Timeframe: Up to 5 years

Interventionparticipants evaluable for toxicity (Number)
Phase I, Dose Level 012
Phase I, Dose Level 13
Phase II107

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Incidence of Adverse Events, Based on CTC (Common Toxicity Criteria) Severity Grade

Safety variables will be summarized by descriptive statistics. Adverse Events (AEs) that occur will be reported for each phase and dose level and described in terms of incidence and severity. Parameters will be described based on the CTC severity grading. Distribution by CTC severity grade and clinical relevance will be given. (NCT00731731)
Timeframe: Up to 5 years

Interventionparticipants evaluable for toxicity (Number)
Phase I, Dose Level 012
Phase I, Dose Level 13
Phase II107

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Overall Survival at 15 Months (Phase II)

The primary endpoint will be survival status at 15 months (OS15). In addition, survival will be estimated using a Kaplan-Meier curve. For this analysis, patients who are still alive at the time of analysis have survival time censored at the last contact date. (NCT00731731)
Timeframe: Time from study registration to the date of death from any cause, assessed up to 5 years

Interventionpercentage of phase II patients (Number)
Phase II54.6

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Concentration of Vorinostat in Tumor Tissue

Concentration of vorinostat in tumor tissue will be measured after 7 days of use of Vorinostat. (NCT00735826)
Timeframe: Day 7 from Baseline

Interventionng/mg (Median)
Vorinostat Intratumoral Concentrations42.6

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Changes in Tumor Markers on Tumors of the Lung, Esophagus, or Head and Neck, After 7 Days of Treatment With Vorinostat

Immunohistochemical score, defined as: 0, no tumor cells staining positive; 1+, 0% to 50% of tumor cells staining positive; 2+, 50% to 75% of tumor cells staining positive; and 3+, 75% to 100% of tumor cells staining positive. The change in the score before and after treatment is percentage - 0-100 (NCT00735826)
Timeframe: Baseline to Day 7

Interventionpercentage of change (Median)
Changes in Ki-67 expression by immunohistochemicalChanges in cyclin D1 expression by immunohistochemChanges in cyclin E expression by immunohistochemi
Vorinostat674040

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Effects of Vorinostat Treatment on Induction of Apoptosis or Necrosis in Treated vs. Untreated Tumors

vorinostat's effects on induction of apoptosis or necrosis in treated vs untreated tumors and on p21, p27, EGFR, and phospho-EGFR expression aerodigestive tract tumors. Immunohistochemical score is defined as follows: 0, no tumor cells staining positive; 1+, 0% to 50% of tumor cells staining positive; 2+, 50% to 75% of tumor cells staining positive; and 3+, 75% to 100% of tumor cells staining positive. (NCT00735826)
Timeframe: Baseline to day 7

Interventionscore on a scale (Mean)
Necrosis1

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Event-free Survival

"Time from treatment start until disease progression, death, or discontinuation of treatment for adverse event (toxicity)~Estimated using the Kaplan-Meier method. A logrank test will be used to compare progression-free survival between Group I and Group II. A p-value less that 0.05 will be considered statistically significant." (NCT00764517)
Timeframe: Up to 5 years

InterventionMonths (Median)
Previously Untreated39.0
Relapsed19.5

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Objective Response Rate

ORR defined as the percentage of patients who achieved a complete response (CR) or a partial response (PR). Assessed per the revised Cheson criteria. Response definitions per revised International Working Group Response Criteria. 95% confidence interval will be provided. Definitions: Complete response (CR) = disappearance of all evidence of disease; Partial response (PR) = regression of measurable disease and no new sites. (NCT00764517)
Timeframe: 2 years

Interventionpercentage of participants (Number)
Previously Untreated97
Relapsed39

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Progression-free Survival

"Time from treatment start until disease progression or death.~Estimated using the Kaplan-Meier method. A logrank test will be used to compare progression-free survival between Group I and Group II. A p-value less that 0.05 will be considered statistically significant." (NCT00764517)
Timeframe: Up to 5 years

InterventionMonths (Median)
Previously UntreatedNA
Relapsed19.5

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Tolerability of Treatment

Tolerability is determined to be the percentage of patients who completed the full duration of treatment (all 6 cycles) regardless of adverse event status. % tolerability shows the rate of patients that tolerated the treatment for the full duration. (NCT00764517)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Previously Untreated62
Relapsed22

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Toxicities as Assessed Using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) Version 4.0

Toxicity is determined percentage of patients that experienced an adverse event (AE) grade 3 or higher during the time frame, assessed using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. Grade refers to the severity of the AE increasing from Grade 1 to 5. Generally, Grade 1 = Mild; Grade 2 = Moderate; Grade 3 = Severe or medically significant but not immediately life-threatening; Grade 4 = Life-threatening consequences; Grade 5 = Death related to AE. (NCT00764517)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Previously Untreated90
Relapsed83

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Part I: Number of Participants Experiencing Dose Limiting Toxicity (DLT)

"A DLT was defined as any of the following (per Common Terminology Criteria for Adverse Events [CTCAE] version 3.0):~Grade 3 (severe)-4 (life-threatening) neutropenia with fever ≥ 38.5ºC~Grade 3-4 neutropenia with an infection requiring antibiotic or antifungal treatment~Grade 4 neutropenia lasting at least 5 days~Grade 4 thrombocytopenia~Other Grade 4 hematologic toxicity, including a decrease in hemoglobin, only at the discretion of the principal investigator~Grade 3 or 4 non-hematologic event, except which are manageable by supportive care or non-prohibited therapies" (NCT00771472)
Timeframe: Day 1 to Day 28

Interventionparticipants (Number)
Vorinostat1

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Part I: Maximum Drug Concentration (Cmax)

"Blood samples taken as follows:~Day 1 & Day 28 of Cycle 1: pre dose, and 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 10, 12 and 24 hours after dosing of vorinostat." (NCT00771472)
Timeframe: Days 1 & 28 of Cycle 1

InterventionµM (Geometric Mean)
Day 1 (n=6)Day 28 (n=5)
Vorinostat0.831.17

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Part I: The Amount of Time it Takes for the Drug Concentration to Decrease by Half (T1/2)

"Blood samples taken as follows:~Day 1 & Day 28 of Cycle 1: pre dose, and 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 10, 12 and 24 hours after dosing of vorinostat." (NCT00771472)
Timeframe: Days 1 & 28 of Cycle 1

Interventionhours (Geometric Mean)
Day 1 (n=5)Day 28 (n=4)
Vorinostat1.942.30

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Part I: Total Drug Exposure (Area Under the Concentration Curve, AUC[0-24 Hours])

"Blood samples taken as follows:~Day 1 & Day 28 of Cycle 1: pre dose, and 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 10, 12 and 24 hours after dosing of vorinostat." (NCT00771472)
Timeframe: Days 1 & 28 of Cycle 1

InterventionµM*hr (Geometric Mean)
Day 1 (n=6)Day 28 (n=5)
Vorinostat4.595.59

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Part I: Time at Which Cmax Occurs (Tmax)

"Blood samples taken as follows:~Day 1 & Day 28 of Cycle 1: pre dose, and 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 10, 12 and 24 hours after dosing of vorinostat." (NCT00771472)
Timeframe: Days 1 & 28 of Cycle 1

Interventionhours (Median)
Day 1 (n=6)Day 28 (n=5)
Vorinostat2.913.73

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Parts I & II: Number of Participants Experiencing Clinical or Laboratory Adverse Experiences (AE)

A laboratory AE is defined as any unfavorable & unintended change in the chemistry of the body temporally associated with the use of study product, whether or not considered related to the use of the product. A clinical AE is defined similarly but also includes changes in structure or function of the body. (NCT00771472)
Timeframe: Day 1 up until 30 days post study completion or early termination (up to approximately 506 days)

Interventionparticipants (Number)
Clinical AEsLaboratory AEs
Vorinostat106

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Objective Response Rate

Objective response rate was measured as the proportion of patients who achieved a confirmed partial response or better during the course of the study. Response to study therapy was assessed using EBMT Criteria and confirmed by Independent Adjudication Review. (NCT00773747)
Timeframe: Baseline and at the end of each 21-day Cycle assessed up to 32 months (final study analysis)

InterventionPercentage of Participants (Number)
Vorinostat + Bortezomib56.2
Placebo + Bortezomib40.6

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Overall Survival

Overall survival was measured from the start of the treatment to death due to any cause. Overall Survival is represented as the number of deaths per 100-person- months and was computed by dividing the number of participants with an event of death that occurred during the study follow-up period by the total duration of follow-up (in 100 months) for all the participants in each cohort since participants had different lengths of follow-up. (NCT00773747)
Timeframe: From randomization up to 32 months (final study analysis)

InterventionEvents/100-person Months (Number)
Vorinostat + Bortezomib1.7
Placebo + Bortezomib1.9

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Progression-Free Survival (PFS)

Progression-free survival was measured from the start of the treatment to the time when the criteria for progression was met or death due to any cause (whichever is first recorded). Response to study therapy was assessed using European Blood and Marrow Transplantation Group (EBMT) Criteria. A stratified Cox proportional hazards model was used with Efron's likelihood approximation to account for ties in event times. (NCT00773747)
Timeframe: From randomization to event of disease progression or death assessed up to 32 months (final study analysis)

InterventionMonths (Median)
Vorinostat + Bortezomib7.63
Placebo + Bortezomib6.83

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Time to Progression

Time to progression was measured from the start of the treatment to the time when the criteria for progression was met or death due to myeloma (whichever is first recorded). Response to study therapy was assessed using European Blood and Marrow Transplantation Group (EBMT) Criteria. A stratified Cox proportional hazards model was used with Efron's likelihood approximation to account for ties in event times. (NCT00773747)
Timeframe: Baseline and at the end of each 21-day Cycle assessed up to 32 months (final study analysis)

InterventionMonths (Median)
Vorinostat + Bortezomib7.73
Placebo + Bortezomib7.03

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Number of Participants With Grade 3-5 Clinical or Laboratory Adverse Events (AEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. Grades come from the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. Per protocol, clinical and laboratory AEs are presented as a combined total for each grade. (NCT00773747)
Timeframe: Up to 722 days

,
InterventionParticipants (Count of Participants)
Grade 3Grade 4Grade 5
Placebo + Bortezomib2408517
Vorinostat + Bortezomib27210811

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Overall Survival (OS)

OS was defined as the time from allocation to death due to any cause. To report the median survival (in months) and the associated 95%CIs were reported using Kaplan-Meier method was used. Participants without documented death at the time of final analysis were censored at the date of the last follow up. (NCT00773838)
Timeframe: Up to approximately 40 months (through End of Trial data cut-off of 09-Apr-2012)

InterventionMonths (Median)
Vorinostat + Bortezomib11.23

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Time To Disease Progression (TTP) as Determined by IAC Per EBMT Criteria

TTP was defined as the time from allocation to the first documented disease progression (PD) as determined by IAC per EBMT criteria or death due to myeloma, whichever occurred first. PD: >25% increase in level of serum Mparaprotein, which must also be an absolute increase of at least 5g/L (500 mg/dL) and confirmed on a repeat investigation or 25% increase in 24-hour urinary light chain excretion, which must also be an absolute increase of at least 200mg/24hour and confirmed on a repeat investigation or >25% increase in plasma cells in a bone marrow aspirate or on trephine biopsy, which must also be an absolute increase of at least 10% or definitive increase in size of existing LBLs or STP or development of hypercalcemia (corrected serum calcium >11.5 mg/dL or 2.8 mmol/L not attributable to any other cause). To report the median TTP (in months) and associated 95% CIs Kaplan-Meier method was used. (NCT00773838)
Timeframe: Up to approximately 30 months (through Final Analysis data cut-off of 16-May-2011)

InterventionMonths (Median)
Vorinostat + Bortezomib3.47

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Objective Response Rate (RR)

Objective RR was defined as percentage (%) of participants with complete response (CR: disappearance of original monoclonal (M) paraprotein from blood & urine on at least 2 determinations for at least 6 weeks (WKs) by immunofixation studies, <5% plasma cells in bone marrow on at least 1 determination, no increase in size/number of lytic bone lesions (LBLs) & disappearance of soft tissue plasmacytomas (STP) for at least 6 WKs on skeletal survey (SS) if available) or partial response (PR: ≥50% reduction in serum M protein for at least 2 determinations 6 WKs apart, if present, reduction in 24-hour urinary light chain excretion by ≥90% or ≤200 mg for at least 2 determinations 6 WKs apart, ≥50% reduction in STP size for at least 6 WKs, & no increase in size/number of LBLs on SS if available) as assessed by Independent Adjudication Committee (IAC) per European Blood & Marrow Transplant (EBMT) criteria. To report RR & 95% confidence intervals (CIs), exact test of binomial parameter was used. (NCT00773838)
Timeframe: Up to approximately 30 months (through Final Analysis data cut-off of 16-May-2011)

InterventionPercentage of Participants (Number)
Vorinostat + Bortezomib11.3

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Number of Participants Who Discontinued Study Treatment Due to an AE

An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the Sponsor's product, is also an AE. The number of participants who discontinued study treatment due to an AE were reported. (NCT00773838)
Timeframe: Up to approximately 18 months

InterventionParticipants (Count of Participants)
Vorinostat + Bortezomib28

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Number of Participants Who Experienced an Adverse Event (AE)

An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the Sponsor's product, is also an AE. The number of participants who experienced an AE were reported. (NCT00773838)
Timeframe: Up to approximately 22 months

InterventionParticipants (Count of Participants)
Vorinostat + Bortezomib142

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TTP as Assessed by Investigator Per EBMT Criteria

TTP was defined as the time from allocation to the first documented PD as assessed by investigator per EBMT criteria or death due to myeloma, whichever occurred first. PD: >25% increase in level of serum Mparaprotein, which must also be an absolute increase of at least 5g/L (500 mg/dL) and confirmed on a repeat investigation or 25% increase in 24-hour urinary light chain excretion, which must also be an absolute increase of at least 200mg/24hour and confirmed on a repeat investigation or >25% increase in plasma cells in a bone marrow aspirate or on trephine biopsy, which must also be an absolute increase of at least 10% or definitive increase in size of existing LBLs or STP or development of hypercalcemia (corrected serum calcium >11.5 mg/dL or 2.8 mmol/L not attributable to any other cause). To report the median TTP (in months) and associated 95% CIs Kaplan-Meier method was used. (NCT00773838)
Timeframe: Up to approximately 30 months (through Final Analysis data cut-off of 16-May-2011)

InterventionMonths (Median)
Vorinostat + Bortezomib3.07

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Progression-Free Survival (PFS) as Determined by IAC Per EBMT Criteria

PFS was defined as the time from allocation to the first documents PD as determined by IAC per EBMT criteria or death due to any cause, whichever occurs first. PD: >25% increase in level of serum M-paraprotein, which must also be an absolute increase of at least 5g/L (500 mg/dL) and confirmed on a repeat investigation or 25% increase in 24-hour urinary light chain excretion, which must also be an absolute increase of at least 200mg/24hour and confirmed on a repeat investigation or >25% increase in plasma cells in a bone marrow aspirate or on trephine biopsy, which must also be an absolute increase of at least 10% or definitive increase in size of existing LBLs or STP or development of hypercalcemia (corrected serum calcium >11.5 mg/dL or 2.8 mmol/L not attributable to any other cause). To report the median PFS (in months) and associated 95%CIs Kaplan-Meier method was used. (NCT00773838)
Timeframe: Up to approximately 30 months (through Final Analysis data cut-off of 16-May-2011)

InterventionMonths (Median)
Vorinostat + Bortezomib3.13

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PFS as Assessed by Investigator Per EBMT Criteria

PFS was defined as the time from allocation to the first documents PD as assessed by investigator per EBMT criteria or death due to any cause, whichever occurs first. PD: >25% increase in level of serum M-paraprotein, which must also be an absolute increase of at least 5g/L (500 mg/dL) and confirmed on a repeat investigation or 25% increase in 24-hour urinary light chain excretion, which must also be an absolute increase of at least 200mg/24hour and confirmed on a repeat investigation or >25% increase in plasma cells in a bone marrow aspirate or on trephine biopsy, which must also be an absolute increase of at least 10% or definitive increase in size of existing LBLs or STP or development of hypercalcemia (corrected serum calcium >11.5 mg/dL or 2.8 mmol/L not attributable to any other cause). To report the median PFS (in months) and associated 95%CIs Kaplan-Meier method was used. (NCT00773838)
Timeframe: Up to approximately 30 months (through Final Analysis data cut-off of 16-May-2011)

InterventionMonths (Median)
Vorinostat + Bortezomib2.83

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Number of Subjects With Progressive Disease (PR)

Number of patients with greater than 20% worsening in measurable disease by RECIST criteria (NCT00785798)
Timeframe: 2 years

Interventionparticipants (Number)
Vorinostat and Pegylated Liposomal Doxorubicin Intervention10

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Overall Response Rate

number of patients responding (NCT00785798)
Timeframe: end of study (up to 2 years)

InterventionParticipants (Count of Participants)
Vorinostat and Pegylated Liposomal Doxorubicin Intervention17

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Number of Participants With Dose Limiting Toxicity for Determination Phase I (Schedule A) MTD of Vorinostat

MTD of Vorinostat defined as highest dose level in which 6 patients have been treated with less than 2 instances of DLT. Continual reassessment during each 21-day cycle to assess DLT. Vorinostat was administered orally on days 5 to 14 (Schedule A), first at 300 mg orally once daily (total doses of 3000 mg over 10 days per cycle), and next at 200 mg orally twice daily (total doses of 4000 mg over 10 days per cycle. The dose of Vorinostat escalated in successive 3+3 cohorts of participants to determine the MTD. (NCT00787527)
Timeframe: 21 Days

Interventionparticipants (Number)
Schedule A - Vorinostat Once Daily1
Schedule A - Vorinostat Twice Daily2

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Phase I Maximum Tolerated Dose (MTD) of Vorinostat

MTD of Vorinostat when administered in combination with Cyclophosphamide, Doxorubicin, Vincristine, Prednisone (CHOP) defined as highest dose level in which 6 patients have been treated with less than 2 instances of dose limiting toxicity (DLT). Continual reassessment during each 21-day cycle to assess dose limiting toxicity. Two schedules of Vorinostat were investigated: Phase I A) daily doses on days 5 to 14, or Phase II B) three times a day on days -2 to 3 of standard CHOP every 21 days. Vorinostat was administered orally on days 5 to 14 (Schedule A), first at 300 mg orally once daily (total doses of 3000 mg over 10 days per cycle), and next at 200 mg orally twice daily (total doses of 4000 mg over 10 days per cycle); and for Phase II Schedule B Vorinostat administered orally 300 mg orally three times daily from days -2 to 3 (4500 mg over 5 days per cycle). (NCT00787527)
Timeframe: 21 Days

Interventionmg/day (Number)
Schedule A - Vorinostat Once or Twice Daily300

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Phase II MTD of Vorinostat

MTD of Vorinostat when administered in combination with Cyclophosphamide, Doxorubicin, Vincristine, Prednisone (CHOP) defined as highest dose level in which 6 patients have been treated with less than 2 instances of dose limiting toxicity (DLT). Continual reassessment during each 21-day cycle to assess dose limiting toxicity. Two schedules of Vorinostat were investigated: Phase I A) daily doses on days 5 to 14, or Phase II B) three times a day on days -2 to 3 of standard CHOP every 21 days. Vorinostat was administered orally on days 5 to 14 (Schedule A), first at 300 mg orally once daily (total doses of 3000 mg over 10 days per cycle), and next at 200 mg orally twice daily (total doses of 4000 mg over 10 days per cycle); Schedule B Vorinostat administered orally 300 mg orally three times daily from days -2 to 3 (4500 mg over 5 days per cycle). (NCT00787527)
Timeframe: 21 Days

Interventionmg/three times daily (Number)
Schedule B - Vorinostat Three Times Daily300

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Toxicity

Graded using the NCI Common Terminology Criteria for Adverse Events (CTCAE) version 3.0 (NCT00798720)
Timeframe: 30 days post-treatment

Interventionparticipants (Number)
Thrombocytopenia Grade 3Thrombocytopenia Grade 4Lymphopenia Grade 3Fatigue Grade 3Fatigue Grade 4Vomiting Grade 3Dizziness Grade 3Syncope Grade 3Neuropathy Grade 3Hyponatremia Grade 3
Vorinostat + Bortezomib7134122223

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Median Overall Survival

(NCT00798720)
Timeframe: 5 years

Interventionmonths (Median)
Vorinostat + Bortezomib4.7

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Three-month Progression-free Survival

"Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum of the longest diameter recorded since the treatment started or the appearance of one or more new lesions." (NCT00798720)
Timeframe: Three-months post-treatment

Interventionpercentage of participants (Number)
Vorinostat + Bortezomib11.1

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Response Rate

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST) for target lesions and assessed by MRI, CT, or chest x-ray: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR+PR. (NCT00798720)
Timeframe: Until disease progression, up to 2 years

Interventionparticipants (Number)
Partial responseStable diseaseProgressive disease
Vorinostat + Bortezomib0513

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Number of Patients With Response

Computed tomography scans and/or Positron emission tomography (PET) scans obtained every two cycles to evaluate response using International Workshop Criteria of Complete Response, Partial Response, Progressive Disease, or Stable Disease. (NCT00810576)
Timeframe: Every two 21-day cycles

Interventionparticipants (Number)
Complete ResponsePartial ResponseProgressive DiseaseStable Disease
Vorinostat + Bortezomib0010

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Percent Survival at 2-years

To determine 2-year overall survival rate (NCT00810602)
Timeframe: two years

Interventionpercentage of subjects (Number)
Vorinostat Prophylaxis73

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100-day Cumulative Incidence of Grade 2-4 Acute Graft Versus Host Disease (GVHD)

Assess if the addition of Vorinostat to standard GVHD prophylaxis regimen can reduce the rate of grades 2-4 acute GVHD when compared to 48% in a cohort of identically treated RIC HSCT patients without vorinostat. A reduction of incidence to less than 25% will be considered successful. (NCT00810602)
Timeframe: 100 days

Interventionpercentage of participants (Number)
Vorinostat Prophylaxis22

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Number of Serious Adverse Events

The safety and feasibility will be partially measured by the number of serious adverse events (SAE) recorded by participants receiving at least one dose of Vorinostat. (NCT00810602)
Timeframe: 100 days

InterventionNumber of Serious Adverse Events (Number)
Vorinostat Prophylaxis33

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Percent Cumulative Incidence of Relapse at 2 Years.

Determine the cumulative incidence of relapse at 2 years. (NCT00810602)
Timeframe: two years

Interventionpercentage of participants (Number)
Vorinostat Prophylaxis16

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Number of Patients by Best Clinical Response

Assessed by the International Working Group response criteria: Complete Remission - <5% myeloblasts with normal maturation of all cell lines; Partial Remission - bone marrow blasts decreased by > 50% over pre-treatment but still >5%; and Hematologic Improvement - hemoglobin increase by > 1.5g/dl or decreased transfusions by at least 4/8 week period, platelet absolute increase of >30 X 10^9/L for those starting at >20 X 10^9/L . For those < 20 X 10^9 /L at baseline increase by 100%. (NCT00818649)
Timeframe: At Completion of Course 3 (Day 63)

InterventionPatients (Number)
Complete RemissionProgressive DiseaseStable Disease
Evaluable Patients165

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The Primary Endpoint of the Study is to Establish the Maximum Tolerated Dose of Vorinostat When Given Concurrently With Palliative Radiation.

maximum tolerated dose of vorinostat when given concurrently with radiation (NCT00821951)
Timeframe: 1 Year

Interventionmg (Number)
Vorinostat and Radiotherapy400

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Maximum Tolerated Dose (MTD) of Vorinostat + Chemoradiation

MTD is maximum dose at which 6 patients are treated and there is at most 1 patient with dose limiting toxicities (DLT). Toxicities graded according to the Common Terminology Criteria for Adverse events (CTCAE). (NCT00831493)
Timeframe: Toxicity assessment at 6 weeks following chemoradiation (6 weeks)

Interventionmg (Number)
Vorinostat + Radiation Therapy200

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Toxicity as Assessed by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) v3.0

The first three months of therapy will be used as the time period in which toxicity will be evaluated and stopping rules for unacceptable toxicity will be implemented. Rules for stopping the study will be based on the rate of withdrawal due to significant toxicity (grade IV, non-hematological, non-metabolic, nonperipheral neuropathy). (NCT00839956)
Timeframe: The first three months of therapy

InterventionParticipants (Count of Participants)
Arm I (Bortezomib and Vorinostat)0

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Median Follow-up Survival for All Patients

(NCT00839956)
Timeframe: Up to 5 years

Interventionyears (Median)
Arm I (Bortezomib and Vorinostat)5.15

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Survival for All Patients

(NCT00839956)
Timeframe: Up to 5 years

InterventionParticipants (Count of Participants)
Arm I (Bortezomib and Vorinostat)25

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Time to Disease Progression in Patients Who Progressed

Patients will be followed for initial response to therapy and for progression of disease. Response criteria will be scored according to International Myeloma Working Group uniform response criteria. (NCT00839956)
Timeframe: Up to 5 years

Interventionyears (Median)
Arm I (Bortezomib and Vorinostat)2.1

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Number of Participants With an Adverse Event (AE)

The number of participants with ≥1 AE is reported. An AE is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study product(s), whether or not considered related to the use of the product(s). (NCT00858234)
Timeframe: Up to 346 days (up to 30 days after the final dose of study treatment)

InterventionParticipants (Count of Participants)
Vorinostat + Bortezomib9

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Number of Participants With Dose-Limiting Toxicity (DLT) During Cycle 1

The number of participants with ≥1 DLT during Cycle 1 is reported. A DLT is defined as an event considered by the investigator to be related to study treatment, and either: 1) a Grade 3 or 4 non-hematologic event (except for manageable toxicity by supportive care or non-prohibited therapies, or a transient increase in alanine aminotransferase [ALT]/aspartate aminotransferase [AST]); or 2) a Grade 4 hematologic toxicity except neutropenia or hemoglobin decreased (neutropenia was a DLT if it was Grade 3-4 with fever ≥38.5°C; Grade 3-4 with an infection requiring antibiotic/antifungal therapy; or Grade 4 and lasting ≥5 days). (NCT00858234)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
Vorinostat + Bortezomib1

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Area Under the Plasma Concentration-Time Curve From 0 to 24 Hours Postdose (AUC0-24hr) of Vorinostat Administered With Bortezomib on Days 1 and 11

The AUC0-24hr of vorinostat in plasma on Days 1 and 11 is reported in participants who also received bortezomib. (NCT00858234)
Timeframe: Predose and 0.8, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose on Days 1 and 11

InterventionµM*hr (Least Squares Mean)
Day 1Day 11
Vorinostat + Bortezomib5.415.84

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Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event (AE)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered study treatment and which did not necessarily have to have a causal relationship with this treatment. The number of participants who discontinued from study drug due to an adverse event was reported. (NCT00875056)
Timeframe: Up to 536 days

InterventionParticipants (Count of Participants)
Follicular Lymphoma (FL)6
Indolent Non-FL B-NHL or MCL1
Other Disease2

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Number of Participants Who Experienced an Adverse Event (AE)

An AE was defined as any untoward medical occurrence in a participant administered study treatment and which did not necessarily have to have a causal relationship with this treatment. The number of participants who experienced an AE was presented. (NCT00875056)
Timeframe: Up to approximately 29 months

InterventionParticipants (Count of Participants)
Follicular Lymphoma (FL)39
Indolent Non-FL B-NHL or MCL11
Other Disease6

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Objective Response Rate (ORR)

ORR was defined as the percentage of participants who had a Complete Response (CR: Normal liver/spleen physical exam, all lymph nodes and nodal masses are normal, and there is no bone marrow involvement), a Complete Response/unconfirmed (CRu: Normal liver/spleen physical exam, plus at least a 75% decrease in the sum of the products of the greatest diameters of nodal masses if any are greater than 1.5 cm in their greatest diameter, normal or indeterminate bone marrow involvement), or a Partial Response (PR: Either normal physical exam, lymph nodes, and lymph node masses plus positive bone marrow involvement; OR normal physical exam or decrease in liver/spleen size plus at least a 50% decrease in the diameters of lymph nodes and nodal masses) as assessed using the international working group Non-Hodgkin's lymphoma standardized response criteria described by Cheson, BD in 1999. The percentage of participants who experienced a CR, CRu, or PR is presented. (NCT00875056)
Timeframe: Up to 650 days

InterventionPercentage of participants (Number)
Follicular Lymphoma (FL)48.7
Indolent Non-FL B-NHL or MCL27.3

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Time to Response for Relapsed/Refractory FL

Time to Response is defined as the time from allocation until the time of an initial response. Data was censored on the efficacy data cutoff date of 25 February, 2011. (NCT00875056)
Timeframe: Up to 650 days

InterventionDays (Median)
Follicular Lymphoma (FL)NA

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Time to Treatment Failure for Relapsed/Refractory FL

Time to Treatment Failure is defined as the time from allocation until the date of any treatment failure, including documented disease progression, or discontinuation of the study medication for any reason. Data was censored on the efficacy data cutoff date of 25 February, 2011. (NCT00875056)
Timeframe: Up to 650 days

InterventionDays (Median)
Follicular Lymphoma (FL)323

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Level of Methylation

the percentage of methylated DNA (NCT00882206)
Timeframe: Day 33

Interventionpercentage of DNA (Mean)
Decitabine / Vorinostat86.1

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Response to Treatment

Response includes both complete remission (defined as <5% leukemic blasts in the bone marrow) and partial remission (defined as a greater than 35% reduction in the bone marrow leukemia blast percentage at day 33) (NCT00882206)
Timeframe: Day 33

Interventionparticipants (Number)
Decitabine / Vorinostat6

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Level of Methylation

the percentage of methylated DNA (NCT00882206)
Timeframe: Day 5

Interventionpercentage of DNA (Mean)
Decitabine / Vorinostat79.82

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Level of Methylation

the percentage of methylated DNA (NCT00882206)
Timeframe: Day 0

Interventionpercentage of DNA (Mean)
Decitabine / Vorinostat84.98

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Number of Participants With Dose-limiting Toxicity (Phase I)

(NCT00895934)
Timeframe: 42 days

Interventionparticipants (Number)
Dose 10
Dose 20
Dose 30
Dose 41

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Number of Participants With Dose-limiting Toxicity After the Vorinostat Dose

(NCT00895934)
Timeframe: Up to 3 years

Interventionparticipants (Number)
Phase 1 Dose-Finding Cohorts 1-34
Phase 2/Selected Dose18

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Disease Relapse

(NCT00895934)
Timeframe: up to 2 years

InterventionParticipants (Count of Participants)
Phase 2/Selected Dose5

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Number of Participants With Complete Remission

Efficacy Defined as Best Response Achieved During Study Treatment Measured by Complete Remission (CR) Rate (NCT00895934)
Timeframe: up to 3 years

InterventionParticipants (Count of Participants)
Phase 2/Selected Dose18

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Vorinostat Maximum Tolerated Dose (MTD) [Phase Ib]

The Vorinostat MTD is determined by the number of patients who experience a dose limiting toxicity (DLT). See subsequent primary outcome measure for the DLT definition. The MTD is defined as the highest dose at which fewer than one-third of patients experience a DLT. If no DLTs are observed, the MTD is not reached. (NCT00910000)
Timeframe: The DLT observation period in determining the MTD was the 21-day cycle 1 length.

Interventionmg/day (Number)
All Phase Ib ParticipantsNA

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Response

Response was based on RECIST 1.0 criteria. Per RECIST 1.0 for target lesions, complete response (CR) is complete disappearance of all target lesions and partial response (PR) is at least a 30% decrease in the sum of longest diameter (LD) of target lesions, taking as reference baseline sum LD. Progressive disease (PD) is at least a 20% increase in sum LD from the smallest LD recorded on treatment. Stable disease (SD) is neither sufficient increase to qualify as PD nor sufficient shrinkage to qualify for PR. For CR or PR, changes in tumor measurements must be confirmed by repeat assessments performed 4 weeks +/- 2 weeks after the response criteria are first met. PR or better overall response assumes at a minimum incomplete response/stable disease (SD) for the evaluation of non-target lesions and absence of new lesions. Participants who received therapy but did not have their disease re-evaluated were considered unevaluable. (NCT00910000)
Timeframe: Disease was assessed radiographically (CT or MRI scan) every 2 cycles on treatment; Phase Ib participants received up to 8 cycles of treatment. The median number of cycles started was 2 (range 1-8).

,,,,,
Interventionparticipants (Number)
Complete ResponsePartial ResponseStable DiseaseProgressive DiseaseUnevaluable
Dose Level 1A03000
Dose Level 1B00003
Dose Level 1C01001
Dose Level 1D02001
Dose Level 2A00102
Dose Level 2D00001

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Dose Limiting Toxicity (DLT) [Phase Ib]

"Dose-limiting toxicity was based on the Common Terminology Criteria for Adverse Events version 3.0 (CTCAE v3.0) and defined as any of the following:~Any CTCAE grade 3 or 4 non-hematologic event except manageable gastrointestinal toxicity and fatigue.~Any of the following hematologic events (excluding neutropenia lasting < 5 days):~i) febrile neutropenia defined as grade 3-4 neutropenia with fever ≥ 38.5°C and/or infection.~ii) any grade 4 neutropenia lasting 5 days or more. iii) grade 4 thrombocytopenia (plt count < 25x 109/L) iv) failure of ANC to recover to ≥ 1000/μL or platelets to recover to ≥ 50,000/μL within 14 days of therapy v) grade 4 anemia~Any clinically significant abnormal laboratory value that results in dose delay of >14 days.~<75% of vorinostat dosing taken by the patient during the first cycle due to any toxicity." (NCT00910000)
Timeframe: The DLT observation period in determining the MTD was the 21-day cycle 1 length.

Interventionparticipants with DLT (Number)
Dose Level 1A0
Dose Level 2A2
Dose Level 1B2
Dose Level 1C2
Dose Level 1D0
Dose Level 2D1

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Maximum Tolerated Dose (MTD) of Vorinostat That Can be Combined With Fludarabine Phosphate, Cyclophosphamide and Rituximab (FCR) (Phase I)

"The MTD of vorinostat in combination with FCR will be defined as the dose level immediately below the dose level at which greater than or equal to 2 patients out of 6 of a cohort experience dose-limiting toxicity. Toxicities will be assessed using the National Cancer Institute Common Terminology Criteria for Adverse Events version 3.0.~Doses of vorinostat analyzed to reach the MTD were 200 mg, 300 mg and 400 mg." (NCT00918723)
Timeframe: 28 days

Interventionmg (Number)
MTD for Vorinostat During Induction Therapy400
MTD for Vorinostat During Maintenance Therapy400

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Overall Survival

Overall survival (OS): The percentage of people in a study who are still alive at for a certain period of time after they started treatment. (NCT00918723)
Timeframe: 2 years

Interventionpercentage of participants (Number)
Treatment (Induction and Maintenance Chemotherapy)90

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Percentage of Patients With Progression-free Survival at 2 Years

"Progression-free survival (PFS): The length of time during and after the treatment that a patient lives with the disease but it does not get worse.~Progressive disease is specified by the NCI (National Cancer Institute) working group guidelines and additional CT (computerized tomography) scan requirements:~Lymphadenopathy, > 50% increase in the sum of the products of at least two lymph nodes on two consecutive determinations; one lymph node must be at least 2 cm.~An increase in the liver or spleen size by 50% or more by CT scan or the de novo appearance of hepatomegaly or splenomegaly.~An increase in the number of blood lymphocytes by 50% or more with at least 5000 B lymphocytes per microliter.~Transformation to a more aggressive histology or occurrence of cytopenia (neutropenia, anemia, or thrombocytopenia) attributable to CLL." (NCT00918723)
Timeframe: 2 years

Interventionpercentage of participants (Number)
Treatment (Induction and Maintenance Chemotherapy)87

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To Estimate the Rate of Conversion of Partial Response (PR) to Complete Response (CR) After Fludarabine, Cyclophosphamide and Rituximab (FCR) Plus Vorinostat

Responses were measured after completion of FCR+ vorinostat induction therapy (within 21 days of starting maintenance) and again after completion of maintenance therapy (24 months after the start of maintenance therapy). Maintenance therapy began within 3 months after completion of induction therapy with FCR+vorinostat. Criteria for response are specified by the National Cancer Institute (NCI) working group guidelines; in addition, patients were required to meet computed tomography (CT) criteria as described in the protocol. Response categories include Complete Response (CR), Partial Response (PR), Nodular Partial Response (nPR), Stable Disease (SD) or Progressive Disease (PD). (NCT00918723)
Timeframe: After completion of maintenance therapy (24 months after start of maintenance)

Interventionpercentage of participants (Number)
Conversion from PR to CRConversion from nPR (nodular PR) to CR
Treatment (Induction and Maintenance Chemotherapy)50100

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Overall Survival

The distribution of survival time will be estimated using the method of Kaplan-Meier. (NCT00937495)
Timeframe: Time from registration to death due to any cause, assessed up to 2 years

Interventionmonths (Median)
Treatment (Vorinostat, Bortezomib)16.4

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Progression Free Survival

Progression-free survival is defined as the time from registration to the time of progression or death, whichever comes first. The distribution and median of progression-free survival times will be estimated using the method of Kaplan-Meier. (NCT00937495)
Timeframe: Up to 2 years

Interventionmonths (Median)
Treatment (Vorinostat, Bortezomib)1.5

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Confirmed Tumor Responses

"The number of confirmed tumor responses is defined as a complete response (CR) or partial response (PR) according to Response Evaluation Criteria in Solid Tumors (RECIST) on two consecutive evaluations at least six weeks apart.~Complete Response (CR): Disappearance of all target lesions. Partial Response (PR): At least a 30% decrease in the sum of the longest dimension (LD) of target lesions taking as reference the baseline sum LD." (NCT00937495)
Timeframe: Up to 2 years

Interventionparticipants (Number)
Complete Response (CR)Partial Response (PR)
Treatment (Vorinostat, Bortezomib)00

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Phase II: Radiographic Response.

The percentage of participants with a complete or partial response as determined by modified Response Assessment in Neuro-Oncology (RANO) criteria. A confirmation of response was not required. Complete Response (CR) was defined as complete disappearance on MR/CT of all enhancing tumor and mass effect, off all corticosteroids (or receiving only adrenal replacement doses) and accompanied by a stable or improving neurologic examination. Partial Response (PR) was defined as greater than or equal to 50% reduction in tumor size on MR/CT by bi-dimensional measurement, on a stable or decreasing dose of corticosteroids and accompanied by a stable or improving neurologic examination. Tumor assessments were done at baseline, the end of the first cycle (4 weeks), then the end of every second cycle (every 8 weeks) thereafter. (NCT00939991)
Timeframe: 3 years

Interventionpercentage of participants (Number)
Phase II56

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Phase I: Determination of the Maximum Tolerated Dose (MTD)

The MTD is based upon dose-limiting toxicities (DLTs) experienced during Cycle 1 of treatment. The MTD is the dose level at which 0/6 or 1/6 patients experience DLT with at least two patients experiencing DLT at the next higher dose level. Using Common Terminology Criteria for Adverse Events (CTCAE) version 3.0, DLTs are defined as: Grade 4 neutropenia lasting greater than 5 days; Grade 3 thrombocytopenia; the occurrence of non-hematologic Grade 3 or greater drug-related adverse events excluding Grade ≥ 3 elevation in alkaline phosphatase, Grade ≥ 3 nausea or vomiting unless occurring despite the use of standard anti-emetics or Grade 3 diarrhea unless occurring despite standard anti-diarrheal therapy; > 14 day delay to re-treat due to failure to resolve drug-related toxicity to re-treatment criteria or pre-treatment baseline. (NCT00939991)
Timeframe: Cycle 1 (28 days)

Interventionmg (Number)
Phase I Dose Escalation400

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Phase II: 6-month Progression-free Survival (PFS)

Phase II: Percentage of participants surviving six months from the start of study treatment without progression of disease. PFS was defined as the time from the date of study treatment initiation to the date of the first documented progression according to RANO criteria, or to death due to any cause. Per RANO, progression is a ≥ 25% increase in the sum of the products of perpendicular diameters of enhancing lesions, any new lesion or clinical deterioration. (NCT00939991)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Phase II53.8

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Phase II: Median Overall Survival (OS)

Phase II: Time in months from the start of study treatment to date of death due to any cause. Patients alive as of the last follow-up had OS censored at the last follow-up date. Median OS was estimated using a Kaplan-Meier curve. (NCT00939991)
Timeframe: 3 years

Interventionmonths (Median)
Phase II12.5

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Phase II: Median Progression-free Survival (PFS)

Phase II: Time in months from the start of study treatment to the date of first progression according to RANO criteria, or to death due to any cause. Per RANO, progression is a ≥ 25% increase in the sum of the products of perpendicular diameters of enhancing lesions, any new lesion or clinical deterioration. Patients alive who had not progressed as of the last follow-up had PFS censored at the last follow-up date. Median PFS was estimated using a Kaplan-Meier curve. (NCT00939991)
Timeframe: 3 years

Interventionmonths (Median)
Phase II6.7

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Overall Survival

(NCT00942266)
Timeframe: Every 12 weeks

Interventionmonths (Median)
Arm I: Low-dose Vorinostat6.5
Arm II: High-dose Vorinostat6.7

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Response Rate

"Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI:~Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT00942266)
Timeframe: Every 8 weeks; up to 100 weeks.

Interventionpercentage of participants (Number)
Arm I: Low-dose Vorinostat2.3
Arm II: High-dose Vorinostat100

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Disease Control Rate (Stable Disease or Objective Response)

"Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI:~Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT00942266)
Timeframe: At 2 months

Interventionpercentage of participants (Number)
Arm I: Low-dose Vorinostat53
Arm II: High-dose Vorinostat53

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Fluorouracil Steady-state Pharmacokinetics

Blood samples will be collected for determination of plasma 5-FU steady state concentration at 6 hours after start of 5-FU continuous infusion. The mean per treatment arm are presented. (NCT00942266)
Timeframe: Day 1

Interventionng/ml (Mean)
Arm I: Low-dose Vorinostat389.4
Arm II: High-dose Vorinostat423.5

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Vorinostat Pharmacokinetics

Blood samples (5 ml of blood each) will be collected in red-top vacutainers (no anticoagulant) at 0 (pre- vorinostat), 0.5, 1, 2, 3, 4, 6, and 8 hours after the vorinostat dose on the first day of 5-FU infusion on cycle 1 (day 2 of cycle 1). Mean area under the curve is presented with 95% CI. (NCT00942266)
Timeframe: day 2 (cycle 1)

Interventionhr∙μM (Mean)
Arm I: Low-dose Vorinostat12.6
Arm II: High-dose Vorinostat14.7

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Median Progression-free Survival

Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. (NCT00942266)
Timeframe: Every 8 weeks, up to 100 weeks.

Interventionmonths (Median)
Arm I: Low-dose Vorinostat2.4
Arm II: High-dose Vorinostat2.9

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Toxicity

"Number of participants with an adverse event.~Please refer to the adverse event reporting for more detail." (NCT00942266)
Timeframe: Daily

Interventionparticipants (Number)
Arm I: Low-dose Vorinostat42
Arm II: High-dose Vorinostat15

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Survival at Day 60

Assessment of survival for outcome done on 60 days following therapy and includes participants alive for at least 60 days. Survival is calculated from start of therapy until death from any cause. (NCT00948064)
Timeframe: Phase I, Baseline to 60 days following first treatment.

Interventionparticipants (Number)
Vorinostat With Azacitidine, Phase I24

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Survival at Day 60

Assessment of survival for outcome done on 60 days following therapy and includes participants alive for at least 60 days. Survival is calculated from start of therapy until death from any cause. (NCT00948064)
Timeframe: Phase II, Baseline to 60 days following first treatment.

Interventionparticipants (Number)
Vorinostat With Azacitidine, Phase II43
Azacitidine, Phase II18

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Response Rate

Number of participants with Complete Response (CR) in AML requiring disappearance of all signs and symptoms related to disease, normalization of peripheral counts (absolute neutrophil count 10^9/L or more, platelet count 100 x 10^9/L or more), and a marrow with 5% or less marrow blasts; a hematologic improvement (HI) defined as a CR except for a platelet count increase by 50% to above 30 x 10^9/L. For MDS, the International Working Group criteria used to assess response. (NCT00948064)
Timeframe: 12-18 Months

,,
Interventionparticipants (Number)
Complete ResponseHematologic ImprovementNo ResponseNot Evaluable
Azacitidine, Phase II81171
Vorinostat With Azacitidine, Phase I90210
Vorinostat With Azacitidine, Phase II111391

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Progression Free Survival (PFS) at 7 Months From Registration

Progression free survival was defined as the duration of time from registration on study to time of objective disease progression. Death was regarded as a progression event. Progression was defined by the Response Evaluation Criteria in Solid Tumors (RECIST) as at least a 20% increase in the sum of the longest diameter of target lesions, or the appearance of one or more new lesions as seen on radiologic evaluation. (NCT00948688)
Timeframe: 7 months

Interventionmonths (Median)
Vorinostat, 5-FU, Radiation TherapyNA

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Progression Free Survival

Progression free survival for this endpoint was defined as the duration of time from beginning of the patients' initial chemotherapy to time of objective disease progression. Death was regarded as a progression event. Progression was defined by the Response Evaluation Criteria in Solid Tumors (RECIST) as at least a 20% increase in the sum of the longest diameter of target lesions, or the appearance of one or more new lesions as seen on radiologic evaluation. (NCT00948688)
Timeframe: 2 years

Interventionmonths (Median)
Vorinostat, 5-FU, Radiation Therapy9.375

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Overall Survival

Percentage of participants still alive at 1 year after enrollment on study (NCT00948688)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Vorinostat, 5-FU, Radiation Therapy6

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Number of Participants Experiencing Unacceptable Toxicity

All participants who receive at least one dose of study treatment were evaluable for toxicity. Unacceptable toxicity is based on the Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. Most grade 3 (severe) or 4 (life-threatening) events are considered to be unacceptable toxicities -- exceptions include nausea or vomiting, fatigue, and alopecia. Hematologic toxicities need to be either grade 4 or last for protocol-defined durations to be considered unacceptable. (NCT00948688)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Vorinostat 200 mg1
Vorinostat 100 mg1

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Maximally Tolerated Dose (MTD) of Vorinostat in Combination With Infusional 5-FU and Radiation Therapy.

The maximum tolerated dose (MTD) is defined as one dose level below the dose level at which participants experience an unacceptable rate of dose-limiting toxicity. (NCT00948688)
Timeframe: 6 weeks

Interventionmilligrams per day (Number)
Vorinostat, 5-FU, Radiation TherapyNA

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Resectability Rate

Percentage of patients able to undergo surgical resection after protocol therapy. (NCT00948688)
Timeframe: 5 months

InterventionParticipants (Count of Participants)
Vorinostat, 5-FU, Radiation Therapy2

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Response Rate

Participants who have either a complete response (disappearance of all target lesions), partial response (at least 30% decrease in sum of longest diameter of target lesions) or stable disease (decrease in size of less than 30% or increase in size of less than 20%). (NCT00948688)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Vorinostat, 5-FU, Radiation Therapy6

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Changes in the Physicians Serial Assessment of Erythroderma Score

(NCT00958074)
Timeframe: Baseline to 30 days post-treatment

,
InterventionParticipants (Count of Participants)
No changeReductionResolution
Cohort I (>=65 Years Old)200
Cohort II (<65 Years Old)032

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Objective Response

Defined as either no evidence of clinical disease or marked improvement (>= 50%) decrease in the modified Severity-Weighted Assessment Tool (mSWAT) skin assessment score compared to baseline. (NCT00958074)
Timeframe: After at least 14 days. With Confirmation after additional 28 days.

Interventionpercentage of total (Number)
Cohort I (>=65 Years Old)0
Cohort II (<65 Years Old)57

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Objective Response Rate of Extracutaneous Manifestations of CTCL (Lymph Node Enlargement, Sezary Cells in Peripheral Blood);

Assessed by changes in the sum of the products in the greatest diameters of enlarged lymph nodes by serial computed tomography (CT) or positron emission tomography (PET)/CT scans. (NCT00958074)
Timeframe: Up to 30 days post-treatment

,
Interventionparticipants (Number)
Overall ResponseStable DiseaseProgressive Disease
Cohort I (>=65 Years Old)020
Cohort II (<65 Years Old)031

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Number of Participants With Overall Response as Measured by Sezary Cell Count

Overall response defined by a clinically significant decrease in Sezary cell count (>50% decrease from baseline). (NCT00958074)
Timeframe: Baseline to 30 days post-treatment

,
Interventionparticipants (Number)
Overall responseStable disease
Cohort I (>=65 Years Old)20
Cohort II (<65 Years Old)13

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Occurrences of Dose Adjustment as Measured by Safety/Toxicity

Toxicities will be graded in severity according to the guidelines outlined in the National Cancer Institute-Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 3.0. (NCT00958074)
Timeframe: Up to 30 days post-treatment

,
InterventionOccurrences (Number)
Dose delayDose reductionTreatment discontinuation
Cohort I (>=65 Years Old)111
Cohort II (<65 Years Old)210

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Overall Survival (Phase II)

From date of registration to date of death due to any cause. Patients last known to be alive are censored at date of last contact. (NCT00972478)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
Ph II: R-CHOP+Vorinostat86

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Toxicity of Vorinostat-R-CHOP in Patients With Newly Diagnosed DLBCL

Incidence of toxicity as assessed by the Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. For each patient, worst grade of each event type is reported. Grade 3 = Severe, Grade 4 = Life-threatening, Grade 5 = Fatal. (NCT00972478)
Timeframe: Up to week 26

,
InterventionParticipants (Number)
Abdominal painAcute kidney injuryAlanine aminotransferase increasedAnemiaAnorexiaAspartate aminotransferase increasedAtrial fibrillationBladder spasmBronchial infectionCD4 lymphocytes decreasedCPK increasedCarbon monoxide diffusing capacity decreasedColitisCreatinine increasedCystitis noninfectiveDehydrationDepressionDiarrheaDisseminated intravascular coagulationDizzinessDuodenal perforationDysphagiaDyspneaElectrocardiogram QT corrected interval prolongedFatigueFebrile neutropeniaFecal incontinenceGastrointestinal disorders - Other, specifyGeneralized muscle weaknessHematuriaHiccupsHyperglycemiaHypoalbuminemiaHypocalcemiaHypokalemiaHyponatremiaHypophosphatemiaHypotensionInfections and infestations - Other, specifyJejunal perforationLeft ventricular systolic dysfunctionLeukocytosisLung infectionLymphocyte count decreasedMucosal infectionMucositis oralMulti-organ failureMyalgiaMyocardial infarctionNauseaNeutrophil count decreasedObstruction gastricPainParonychiaPeripheral motor neuropathyPlatelet count decreasedPneumonitisRecurrent laryngeal nerve palsyRespiratory failureSepsisSinus tachycardiaSinusitisSmall intestinal obstructionStoma site infectionSyncopeUrinary tract infectionUrinary tract painUrine output decreasedVasovagal reactionVisceral arterial ischemiaVomitingWeight lossWhite blood cell decreased
Ph I: R-CHOP+Vorinostat (400mg D1-9)1004100000001102121100013300210011201010000401110180001400030000000101007
Ph II: R-CHOP+Vorinostat31122211111110014020011119241120143086233111420130223371110221111111114320102332

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Safe Dose of Vorinostat to be Used in Combination With R-CHOP Assessed by CTCAE Version 4.0 (Phase I)

Safe dose of Vorinostat (in combination with R-CHOP) at which 3/10 or fewer patients have doselimiting toxicities (DLT). Toxicities graded according to the NCI Common Terminology Criteria for Adverse Events Version 4.0 (CTCAE 4.0). DLT apply only during cycle 1 and should be drug-related (possible, probable, or definite). (NCT00972478)
Timeframe: 21 days

Interventionmg PO Once daily Days 1-9 (Number)
Ph I: R-CHOP+Vorinostat (400mg D1-9)400

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Response Rate (Complete Response [CR]+Partial Response [PR]) (Phase II)

Objective disease status is evaluated according to the 2007 revised Cheson et al. criteria. Complete Response(CR) is a complete disappearance of all disease with the exception of nodes. No new lesions. previously enlarged organs must have regressed and not be palpable. Bone marrow (BM) must be negative if positive at baseline. Normalization of markers. Partial Response (PR) is a 50% decrease in the sum of products of greatest diameters (SPD) for up to 6 identified dominant lesions, including spleenic and hepatic nodules from baseline. No new lesions and no increase in the size of liver, spleen or other nodes. (NCT00972478)
Timeframe: Up to week 26

Interventionpercentage of participants (Number)
Ph II: R-CHOP+Vorinostat81

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Progression-free Survival (Phase II)

From date of registration to date of first documentation of progressive disease, or death due to any cause. Patients last known to be alive and progression free are censored at date of last contact. (NCT00972478)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
Ph II: R-CHOP+Vorinostat73

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Objective Response Rate

Clinical response was assessed by clinical, serologic, and radiographic means. (NCT00976183)
Timeframe: 2 years or 24 months

Interventionparticipants (Number)
Vorinostat12

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Number of Participants With Progression Free Survival (PFS) up to 24 Months

Progression-free survival was defined as the length of time from the date of initial induction chemotherapy until clinical, radiological, or CA-125 progression (NCT00976183)
Timeframe: 2 years or 24 months

Interventionparticipants (Number)
Vorinostat18

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Toxicity of Vorinostat Bortezomib Maintenance Therapy After Autologous Transplant

Number of patients on maintenance therapy post-transplant who experienced grade 3 or higher toxicity per NCI-Common Terminology Criteria for Adverse Events, version 3. The first three months of bortezomib and vorinostat therapy will be used as the time period to evaluate toxicity for stopping rules of the study. Toxicity that meets stopping rules will be determined based on the number of patients that are withdrawn from study for significant toxicity (grade IV, non-hematological, non-metabolic, non-peripheral neuropathy). (NCT00992446)
Timeframe: 3 months after start of maintenance therapy

InterventionParticipants (Count of Participants)
Treatment (Chemotherapy, ASCT, Bortezomib, Vorinostat))19

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Median Time to Disease Progression

median days from transplant to relapse/progression (NCT00992446)
Timeframe: time post ASCT to progression

Interventionyears (Median)
Treatment (Chemotherapy, ASCT, Bortezomib, Vorinostat))1.05

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Event-free Survival

Number of patients alive without disease progression/relapse (NCT00992446)
Timeframe: 6.64 Years Post-Transplant

InterventionParticipants (Count of Participants)
Alive without disease porgressionalive with disease progression
Treatment (Chemotherapy, ASCT, Bortezomib, Vorinostat))145

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Overall Survival

Number of patients alive who received maintenance therapy (NCT00992446)
Timeframe: 6.64 Years Post-Transplant

Interventionparticipants (Number)
AliveDead
Treatment (Chemotherapy, ASCT, Bortezomib, Vorinostat))163

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γ-globin to β-globin Ratio

Levels of peripheral blood γ-globin to β-globin messenger RNA were estimated based on established methods. The ratio of γ-globin to β-globin was then calculated. (NCT01000155)
Timeframe: Measured at baseline and end of treatment, up to 16 weeks.

InterventionChange in γ-globin to β-globin ratio (Median)
Vorinostat0.89

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Percent Fetal Hemoglobin (HbF%) Induction Success Rate

Success will be defined by comparing the maximum HbF% on study drug to the HbF% at baseline. An absolute increase in HbF% of 4% of more, or an increase to 100% or more of baseline in patients with HbF under 4% at baseline will be considered a success. HbF% induction success rate is calculated as the count of successes divided by the count of patients in the analysis population. (NCT01000155)
Timeframe: HbF% was measured at baseline and weekly on treatment. Median duration of treatment was 3 months.

Interventionproportion of patients (Number)
Vorinostat0.20

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F-Cell Percentage Level

F-cell percentage levels were estimated based on established methods. (NCT01000155)
Timeframe: Measured at baseline and end of treatment, up to 16 weeks.

InterventionF-cell percentage (Median)
BaselineEnd of Treatment
Vorinostat9.812.1

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Maximum Tolerated Dose (MTD) of Vorinostat in Combination With Escalating Doses of Erlotinib and Temozolomide

"Phase I assessment MTD Vorinostat in combination with escalating doses of Erlotinib and Temozolomide using conventional phase I design where 3 enrolled into first dose level, monitored for 3 weeks and if no dose-limiting toxicity (DLT) seen, 3 more enrolled at next dosage level. If 2/6 participants experience DLT, the previous (lower) dosage level declared MTD of vorinostat in combination with Erlotinib and Temozolomide.~A maximum of 4 dosage levels utilized with deescalation by 2 dose levels if DLT is seen at the starting dose level. If no DLT noted after dose escalation to Level 4, these doses utilized as MTD for phase II." (NCT01110876)
Timeframe: Evaluated with each 28 day (+2 days) cycle, up to 24 weeks

Interventionmg (Number)
Vorinostat (mg) twice/dayErlotinib (mg)
Phase I Group 1: Vorinostat + Erlotinib + Temozolomide200200

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Clinical Benefit Rate

The Clinical Benefit Rate is the number of patients with either Complete Response (CR), Partial Response (PR), or Stable Disease (SD) for ≥ 6 months (NCT01118975)
Timeframe: Radiological evaluations are performed every 12 weeks to determine disease status

Interventionparticipants (Number)
Phase II - Vorinistat 400mg + Lapatinib1

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Dose Limiting Toxicities

Safety and tolerability were assessed. Adverse events and dose limiting toxicities were recorded during an escalting dose pilot phase. (NCT01118975)
Timeframe: 6 weeks

InterventionDose limiting toxicities (Number)
Pilot Phase0

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Overall Response Rate (ORR)

Overall Response Rate (ORR) (NCT01120834)
Timeframe: 2 cycles

InterventionParticipants (Count of Participants)
All Subjects1

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Overall Survival

Kaplan-Meier survival curves will be used to describe overall survival. Overall survival time will be censored on the last date the patient was known to be alive. (NCT01153672)
Timeframe: Time elapsed from the first day of study treatment until death, assessed up to approximately 5 years

Interventionmonths (Median)
Treatment (Enzyme Inhibitor Therapy, AI Sensitization Therapy)28.8

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Rate of Clinical Benefit According to RECIST

Conventional imaging (CT, bone scan) was performed at baseline and at week 8 and tumor response assessed by RECIST criteria (NCT01153672)
Timeframe: Up to approximately 5 years

Interventionpercentage of evaluable participants (Number)
Treatment (Enzyme Inhibitor Therapy, AI Sensitization Therapy)15

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Progression-free Survival

Kaplan-Meier survival curves will be used to describe progression-free survival. For progression-free survival, patients without documented disease progression or death will be treated as censored observations on the date of the last tumor assessment. (NCT01153672)
Timeframe: Time elapsed from the first day of study treatment, until disease progression or death, assessed up to approximately 5 years

Interventionmonths (Median)
Treatment (Enzyme Inhibitor Therapy, AI Sensitization Therapy)2.8

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Percentage of Patients That Experience Adverse Events as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0

(NCT01153672)
Timeframe: Up to approximately 5 years

Interventionpercentage of participants (Number)
Treatment (Enzyme Inhibitor Therapy, AI Sensitization Therapy)37.5

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Duration of Response

Duration of response will be summarized for responders. (NCT01153672)
Timeframe: Up to approximately 5 years

Interventionweeks (Median)
Treatment (Enzyme Inhibitor Therapy, AI Sensitization Therapy)25.4

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Maximum Tolerated Dose (MTD)

MTD denoted as the highest dose at which no more than one of six patients experienced a dose limiting toxicity (DLT), and expanded to a total of 12 patients. Any drug-related grade 3 or 4 toxicity occurring during the first three weeks of treatment (except nausea, vomiting, diarrhea, serum lipid elevation, or transient electrolyte abnormality that resolved to a grade of 0-2 with medical management) was considered a dose limiting toxicity (DLT). Assessed by National Cancer Institute (NCI) Common Terminology for Adverse Events (CTCAE) version 4.0. (NCT01169532)
Timeframe: First 3 weeks of treatment

Interventionmilligrams (Number)
Ridaforolimus qd days 1-5 every weekVorinostat bid days 1-3 every week
Treatment (Ridaforolimus and Vorinostat)20100

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Progression Free Survival

Kaplan Meier curves will be used. Proportions, 95% confidence intervals, and cumulative incidence curves will be used to characterize response rates. (NCT01169532)
Timeframe: 1 year

Interventionweeks (Median)
Treatment (Ridaforolimus and Vorinostat)17.1

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Overall Survival

Kaplan Meier curves will be used. Proportions, 95% confidence intervals, and cumulative incidence curves will be used to characterize response rates. (NCT01169532)
Timeframe: 1 year

Interventionweeks (Median)
Treatment (Ridaforolimus and Vorinostat)40.7

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Response Duration (RD)

Median point estimate and full range will be documented, since only two patients achieved a response. (NCT01175980)
Timeframe: From the time measurement criteria are met for CR or PR (whichever is first) until the first date that recurrence or progression is objectively documented, assessed up to 60 months after the last dose of vorinostat max. treatment duration= 24 months

Interventionmonths (Median)
Treatment (Vorinostat)30.1

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Stable Disease Duration (SDD)

SDD will be reported as descriptive results as a median point estimate and a 90% confidence interval (CI) estimate. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

Interventionmonths (Median)
Treatment (Vorinostat)11.4

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The Number of Genes Sequenced in the WES Assay as a Measure of the Whole Exome Profile of the Sorted Tumor Population and Matching Germ Line Sample

Reported as descriptive results. The combined CGH array and exome data will be mined to identify genes and pathways that are targeted by select somatic events in each of the patient subsets. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

InterventionGenes sequenced in the WES assay. (Number)
Treatment (Vorinostat)21,522

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Time to Recurrence (TTR)

TTR will be summarized descriptively, reporting N, median, mean, standard deviation, standard error (SE), minimum, maximum, and 90% CI for the mean calculated from the SE and asymptotic normal distribution theory. (NCT01175980)
Timeframe: From the start of the treatment until the RECIST measurement criteria are met for complete response (CR) or partial response (PR) (whichever is first recorded, assessed up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

Interventionmonths (Mean)
Treatment (Vorinostat)8.85

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Unique Probes on the Oligonucleotide CGH Array as a Measure of the Genomic Profile of Each Cell Population.

Genomic profile of each cell population using oligonucleotide CGH arrays. Reported as unique probes on the CGH array. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

Interventionunique probes on the CGH arrays (Number)
Treatment (Vorinostat)442,892

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Number of Participants With Grade 3 or Grade 4 Toxicity as Assessed by the Common Terminology Criteria for Adverse Events Version 4.0

Toxicity will be tabulated via frequency distributions, and also dichotomized to report the proportion (and percentage) of patients experiencing a specified level (e.g., grade 3-4) of toxicity. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

InterventionParticipants (Count of Participants)
AppendicitisAtelectasisBronchial obstructionBronchopulmonary hemorrhageCataractDiarrheaFatigueHeadacheHypertensionHypophosphatemiaHypoxiaLung infectionLymphocyte count decreasedLymphocyte count increasedMenorrhagiaMucositis oralNon cardiac chest painOral painPlatelet count decreasedPNEUMONIAThromboembolic eventWound complication
Treatment (Vorinostat)1111113231117111121121

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Progression-free Survival (PFS)

Distribution will be estimated using standard survival analysis techniques, and the K-M method. From the K-M life tables, both median point estimate and 90% confidence interval (CI) estimate. (NCT01175980)
Timeframe: From start of treatment to time of progression or death, whichever occurs first, assessed up to 60 months after the last dose of vorinostat maximum treatment duration= 24 months

Interventionmonths (Median)
Treatment (Vorinostat)11.4

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Number of Patients With Flow Sort Aneuploid Populations of Tumor Cells From FFPE Tissue

Number of patients with Flow sort aneuploid populations of tumor cells from FFPE tissue. Reported as descriptive results. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

InterventionParticipants (Count of Participants)
Treatment (Vorinostat)0

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Number of Patients With Flow Sort Diploid Populations of Tumor Cells From FFPE Tissue Blocks

Number of patients with Flow sort diploid populations of tumor cells from FFPE tissue blocks reported as a count of participants. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

InterventionParticipants (Count of Participants)
Treatment (Vorinostat)2

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Number of Patients With Flow Sort Tetraploid Populations of Tumor Cells From FFPE Tissue

Number of patients with Flow sort tetraploid populations of tumor cells from FFPE tissue. Reported as descriptive results. (NCT01175980)
Timeframe: Up to 180 days after the last dose of vorinostat maximum treatment duration= 24 months

InterventionParticipants (Count of Participants)
Treatment (Vorinostat)2

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Overall Survival (OS)

"Distribution will be estimated using standard survival analysis techniques, and the K-M method. From the K-M life tables, both point and 90% CI estimates of various statistics of interest can be calculated (e.g., median, 6-month event-free rate, 12-month event-free rate, etc.). Statistical graphs of each K-M curve (with 90% CI lines) will be generated for visual display.~(One year survival rate will be given since OS median was not reached due to too few events)" (NCT01175980)
Timeframe: From the start of treatment until death from any cause, duration for reported probability= 1 year; survival data collected for up to a total of 60 months

Interventionpercentage of participants surviving 1yr (Number)
Treatment (Vorinostat)88

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Complete Clinical Response (CCR)

Complete Clinical Response (CCR) at week 8 as determined by an Modified Severity-Weighted Assessment Tool (mSWAT) score of 0. mSWAT is an objective, quantitative, severity-weighted method to assess the extent of mycosis fungoides (MF) lesions, and is determined by total body surface area (%TBSA) of the lesion by a severity-weighting factor (1 = patch; 2 = plaque; 4 = tumor). O% TBSA produces a product of 0, indicating complete response. (NCT01187446)
Timeframe: Week 8

InterventionParticipants (Count of Participants)
TSEBT Only3
TSEBT Plus Vorinostat3

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Duration of Clinical Benefit (Per Protocol Follow-up)

Duration of clinical benefit represents the period of time that clinical response was maintained. Duration of clinical benefit is reported as the median period of time from the initiation of treatment until progressive disease, as measured by the mSWAT skin assessment, and censored at the final per-protocol assessment (48 weeks) (NCT01187446)
Timeframe: 48 weeks after completion of treatment

InterventionWeeks (Median)
TSEBT Only48
TSEBT Plus Vorinostat28

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Duration of Clinical Benefit (Supplemental Follow-up)

Duration of clinical benefit represents the period of time that clinical response was maintained. Duration of clinical benefit is reported as the median period of time from the initiation of treatment or until progressive disease, as measured by the mSWAT skin assessment. (NCT01187446)
Timeframe: 140 weeks

Interventionweeks (Median)
TSEBT Only125
TSEBT Plus Vorinostat28

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Safety and Tolerability as Measured by Severity and Frequency of Adverse Events

Adverse events occurring at least 10% out of evaluable participants, and it's corresponding rate in the opposing arm. (NCT01187446)
Timeframe: Adverse events were collected through 30 days after the last day of study therapy, or until the patient received an non-study treatment for lymphoma, whichever occurred first.

,
InterventionNumber of patients (Number)
AlopeciaFatigueExtremity PainNauseaDysgeusiaNail ChangesDiarrheaOcular IrritationRadiation DermatitisThrombocytopeniaAnorexiaDizzinessLymphopeniaPedal EdemaSkin PainVomitingXerosis/Dry Skin
TSEBT Only74900400100002101
TSEBT Plus Vorinostat1010684133332221222

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Overall Survival

Time from enrollment to death or last follow-up, whichever occurs first. (NCT01189266)
Timeframe: 2 years after study enrollment

Interventionpercent probability (Number)
Arm 1, Phase I Vorinostat 180 mg/m^222
Arm 2, Phase I Vorinostat 230 mg/m^20
Arm 3, Phase II Evaluation Vorinostat 230 mg/m^23.1

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Incidence of Toxicity During Maintenance Therapy

Proportion of patients who experience any grade 3 or higher CTC AE Version 4 adverse experience (NCT01189266)
Timeframe: Planned 12 months of maintenance with Vorinostat

InterventionParticipants (Count of Participants)
Arm 1, Phase I Vorinostat 180 mg/m^26
Arm 2, Phase I Vorinostat 230 mg/m^24
Arm 3, Phase II Evaluation Vorinostat 230 mg/m^239

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Incidence of Toxicity During Chemoradiation Therapy

Proportion of patients who experience any grade 3 or higher CTC AE Version 4 adverse experience (NCT01189266)
Timeframe: Planned 7 weeks during chemoradiotherapy

InterventionParticipants (Count of Participants)
Arm 1, Phase I Vorinostat 180 mg/m^25
Arm 2, Phase I Vorinostat 230 mg/m^22
Arm 3, Phase II Evaluation Vorinostat 230 mg/m^224

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Maximum Tolerated Dose (MTD) of Vorinostat

The dose of vorinostat in mg/sqm/day to be administered with combination chemotherapy and radiation therapy (NCT01189266)
Timeframe: Planned 7 weeks during chemoradiotherapy

Interventionmg/m^2 (Number)
All Phase 1 Study Participants230

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Event-Free Survival

Time from enrollment to disease progression, diagnosis of a second malignant neoplasm, death or last follow-up, whichever occurs first. (NCT01189266)
Timeframe: 2 years after study enrollment

Interventionpercent probability (Number)
Arm 1, Phase I Vorinostat 180 mg/m^20
Arm 2, Phase I Vorinostat 230 mg/m^20
Arm 3, Phase II Evaluation Vorinostat 230 mg/m^23.1

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Changes in Epstein-Barr Virus (EBV) Viral Load

Differences from baseline (specified follow-up assessment minus baseline) in EBV viral load. (NCT01193842)
Timeframe: Baseline up to 12 months

,,,
InterventionIU/mL (Median)
End of Cycle 2At treatment discontinuation6-month follow-up12-month follow-up
Phase I: VR-DA-EPOCH, Dose Level 10000
Phase I: VR-DA-EPOCH, Dose Level 2-2436.1-1.92-1.92-1.15
Phase II, DA-R-EPOCH0-0.280-2.7
Phase II, VR-DA-EPOCH-0.61-2.9-1.55-0.56

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Changes in Human Herpes Virus (HHV)-8 Viral Load

Differences from baseline (specified follow-up assessment minus baseline) in (HHV)-8 viral load. (NCT01193842)
Timeframe: Baseline up to 12 months

Interventioncopies per 100uL (Median)
12-month follow-up
Phase II: VR-DA-EPOCH0

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Changes in Human Herpes Virus (HHV)-8 Viral Load

Differences from baseline (specified follow-up assessment minus baseline) in (HHV)-8 viral load. (NCT01193842)
Timeframe: Baseline up to 12 months

Interventioncopies per 100uL (Median)
At treatment discontinuation6-month follow-up12-month follow-up
Phase II: DA-R-EPOCH000

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Changes in Human Immunodeficiency Virus (HIV) Viral Load

Differences from baseline (specified follow-up assessment minus baseline) in HIV viral load. Undetectable viral load results were treated as 0 values. (NCT01193842)
Timeframe: Baseline up to 12 months

,
Interventionmedian change in copies per mL (Median)
End of Cycle 2At treatment discontinuation6-month follow-up12-month follow-up
Phase II: DA-R-EPOCH-25-22.5-18-20
Phase II: VR-DA-EPOCH-20-87-200

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Percentage of Participant Experiencing Adverse Events (AEs) for Each Treatment Arm as Assessed by Common Terminology Criteria for Adverse Events Version 4.0 (CTCAE v4.0) (Phase II)

The percentage of participants with AEs and their worst severity will be tabulated for each treatment arm. If a participant has more than one AE, the most severe AE is analyzed. All adverse events will be assessed by the investigator from the first dose of protocol therapy through the post-treatment discontinuation visit. Participants are planned to be treated for a total of 6 cycles (21 day cycle length), or roughly 4 months. After this evaluation, assessment and reporting of AEs will only be required for all grade 5 AEs and any serious AE (SAE) that the investigator considers related to protocol therapy. (NCT01193842)
Timeframe: Up to 5 years

,
Interventionpercentage of participants (Number)
DeathLife-threateningSevereModerateMild
Phase II: DA-R-EPOCH20.028.931.117.80
Phase II: VR-DA-EPOCH28.937.820.08.92.2

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Tumor Response (Phase I)

The percentage of participants whose best tumor response is complete response (CR) or partial response (PR). Based on clinical, radiologic (CT), and pathologic criteria, CR requires 1) complete disappearance of all detectable disease and disease-related symptoms if present before therapy, 2) bone marrow aspirate and biopsy to confirm a CR if initially positive or if clinically indicated by new abnormalities in the peripheral blood counts or blood smear, 3) negative PET results, depending on typically, variably, or unknown pre-treatment FDG status, and 4) spleen and/or liver, if considered to be enlarged before therapy on physical examination or CT scan, not being palpable on physical examination and considered normal size by imaging studies, and nodules related to lymphoma disappeared. PR includes 1) ≥50% decrease in sum of product of diameters (SPD), 2) no increase in size of nodes, liver, or spleen, 3) splenic/hepatic nodules regressed by ≥ 50% SPD, 4) no new sites of disease (NCT01193842)
Timeframe: Up to 2 years post treatment

,,
Interventionpercentage of participants (Number)
Complete responsePartial Response
Phase I: Arm C (VR-CHOP) Dose Level 11000
Phase I: VR-DA-EPOCH, Dose Level 183.316.7
Phase I: VR-DA-EPOCH, Dose Level 283.316.7

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Event-free Survival (EFS) (Phase II)

The percentage of participants surviving without events (relapse or death) one year after starting treatment. (NCT01193842)
Timeframe: 1 year

Interventionpercentage of participants (Number)
Phase II: VR-DA-EPOCH75.6
Phase II: DA-R-EPOCH82.2

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Overall Survival (OS) (Phase II)

The percentage of participants surviving one year after starting treatment. (NCT01193842)
Timeframe: 1 year

Interventionpercentage of participants (Number)
Phase II: VR-DA-EPOCH77.6
Phase II: DA-R-EPOCH86.7

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Percentage of Participants With Complete Response (CR) as Assessed by Response Evaluation Criteria in Solid Tumors (Phase II)

"Percentage of participants with complete response as assessed by Response Evaluation Criteria in Solid Tumors (Phase II) according to treatment arm. Participants are planned to be treated for a total of 6 cycles (21 day cycle length). Participants with CR after Cycle 4 will receive two additional cycles of chemotherapy and complete 6 cycles of chemotherapy. Participants who achieve a partial response (PR) only after Cycle 4 may continue on protocol therapy or they may be removed from the study at the AMC discretion of the physician (local Principal Investigator). Participants with stable disease after 4 cycles (i.e., who did not achieve at least a PR) or progressive disease at any time will be removed from study.~In phase II, there are two arms: Vorinostat RPTD+rituximab-DA-EPOCH arm (VR-DA-EPOCH) and Rituximab-DA-EPOCH arm (DA-R-EPOCH)." (NCT01193842)
Timeframe: Up to 6 months

Interventionpercentage of participants (Number)
Phase II: VR-DA-EPOCH67.5
Phase II: DA-R-EPOCH76.2

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Change in CD8 Cell Counts (Phase I)

Differences from baseline (specified follow-up assessment minus baseline) in absolute CD8 counts. (NCT01193842)
Timeframe: Baseline up to 12 months

,,
Interventioncells/mm^3 (Median)
End of cycle 2Treatment discontinuation6-month follow-up12-month follow-up
Phase I: VR-CHOP, Dose Level 1-172-81-16128
Phase I: VR-DA-EPOCH, Dose Level 135.5-164.5-56604
Phase I: VR-DA-EPOCH, Dose Level 2-115211275154

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Change in Plasma Associated Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) (Phase I)

Differences from baseline (specified follow-up assessment minus baseline) in HIV viral load. Undetectable viral load results were treated as 0 values. (NCT01193842)
Timeframe: Baseline up to 12 months

,,
Interventioncopies per milliliter (Median)
End of cycle 2Treatment discontinuation6-month follow-up12-month follow-up
Phase I: VR-CHOP, Dose Level 128000
Phase I: VR-DA-EPOCH, Dose Level 1-14518-4517-551160
Phase I: VR-DA-EPOCH, Dose Level 2-12.5000

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Pharmacokinetic Clearance (Phase I)

Serial plasma samples for pharmacokinetic analysis were collected at 24-48, 48-72, and 72-96 hours after the start of the first chemotherapy infusion. Doxorubicin, etoposide, and vincristine concentrations were determined using a validated liquid chromatography-tandem mass spectrometry method. The clearance was determined by dividing the drug-infusion rate by the steady-state concentrations, which was the average of the three time points. (NCT01193842)
Timeframe: 24-48, 48-72, and 72-96 hours after the start of the first chemotherapy infusion

,
InterventionLiter/hour (Mean)
DoxorubicinEtoposideVincristine
Phase I: VR-DA-EPOCH, Dose Level 178.63.022.4
Phase I: VR-DA-EPOCH, Dose Level 276.02.416.8

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Changes in Absolute CD4 Cell Counts (Phase I)

Differences from baseline (specified follow-up assessment minus baseline) in absolute CD4 counts. (NCT01193842)
Timeframe: Baseline up to 12 months

,,
Interventioncell/mm^3 (Median)
End of cycle 2Treatment discontinuation6-month follow-up12-month follow-up
Phase I: VR-CHOP, Dose Level 1-218-190-175-84
Phase I: VR-DA-EPOCH, Dose Level 192-3976169
Phase I: VR-DA-EPOCH, Dose Level 2-9-293131

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Cumulative Incidence of Disease Progression in Each Treatment Arm

Cumulative incidence of progression where death from any cause prior to progression and diagnosis of a second malignant neoplasm prior to progression are considered competing events. Disease progression is evaluated according to the COG criteria for measurement of brain tumors and is defined to be a ≥ 25% increase in the product of perpendicular diameters of ANY target lesion, taking as reference the smallest product observed since the start of treatment; OR the appearance of one or more new lesions, OR worsening neurologic status not explained by causes unrelated to tumor progression (e.g., anticonvulsant or corticosteroid toxicity, electrolyte disturbances, sepsis, hyperglycemia, presumed post-therapy swelling etc) PLUS any increase in tumor cross-sectional area (or tumor volume). (NCT01236560)
Timeframe: 1 year after enrollment

Interventionpercent probability (Number)
Feasibility (Vorinostat)67
Arm I (Vorinostat, Phase II Arm A)59
Arm II (Temozolomide, Phase II Arm B)53
Arm III (Bevacizumab, Phase II Arm C)37

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Overall Survival

Time from enrollment to death or last follow-up, whichever occurs first. (NCT01236560)
Timeframe: 1 year after enrollment

Interventionpercent probability (Number)
Feasibility (Vorinostat)33.3
Arm I (Vorinostat, Phase II Arm A)82.2
Arm II (Temozolomide, Phase II Arm B)85.2
Arm III (Bevacizumab, Phase II Arm C)67.3

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Maximum Tolerated Dose (MTD) of Vorinostat

The dose of vorinostat in mg/sq m/day to be administered with combination chemotherapy and radiation therapy. (NCT01236560)
Timeframe: 10 weeks

Interventionmg/sq m (Number)
Feasibility (Vorinostat)230

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Event-free Survival

Time from enrollment to disease progression, diagnosis of a second malignant neoplasm, death or last follow-up, whichever occurs first. Disease progression is evaluated according to the COG criteria for measurement of brain tumors and is defined to be a ≥ 25% increase in the product of perpendicular diameters of ANY target lesion, taking as reference the smallest product observed since the start of treatment; OR the appearance of one or more new lesions, OR worsening neurologic status not explained by causes unrelated to tumor progression (e.g., anticonvulsant or corticosteroid toxicity, electrolyte disturbances, sepsis, hyperglycemia, presumed post-therapy swelling etc) PLUS any increase in tumor cross-sectional area (or tumor volume). (NCT01236560)
Timeframe: 1 year after enrollment

Interventionpercent probability (Number)
Feasibility (Vorinostat)33.3
Arm I (Vorinostat, Phase II Arm A)41.3
Arm II (Temozolomide, Phase II Arm B)59.3
Arm III (Bevacizumab, Phase II Arm C)43.8

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Time to Progression (TTP)

Progression defined by the Modified MacDonald criteria is 25% increase in the sum of products, of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any lesion/site, OR failure to return for evaluation due to health or deteriorating condition (unless clearly unrelated to this cancer). (NCT01266031)
Timeframe: 3, 6, and 12 months from patient registration

,
InterventionMonths (Median)
Overall TTP3 months6 months12 months
Phase II: Bevacizumab4.070.590.290.06
Phase II: Bevacizumab + Vorinostat 400 mg3.710.620.280.15

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Maximum Tolerated Dose (MTD) of Oral Vorinostat Used With Bevacizumab

MTD defined as the dose level at which 1/6 patients experience dose limiting toxicity (DLT), using conventional Phase I design where the MTD was selected using a 3+3 accrual design at each dose level until MTD was determined. Toxicities will be graded according to the Common Terminology Criteria for Adverse events (CTCAE) Version 4.0. (NCT01266031)
Timeframe: 28 day, cycle 1

Interventionmg/day (Number)
Vorinostat + Bevacizumab400

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Number of Participants With Serious and Non-Serious Adverse Events

Here is the count of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT01266031)
Timeframe: Phase I adverse events collected within 4 week (28 day) cycle. Phase II evaluated for adverse events after each cycle for first 2 cycles and subsequently after each 2 cycles of treatment prior to initiating the next cycle.

InterventionParticipants (Count of Participants)
Vorinostat + Bevacizumab6
Bevacizumab38
Bevacizumab + Vorinostat 400 mg47

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Overall Survival (OS)

OS was computed using the number of months from the date of randomization to the date of death, up to 30 months. Participants still alive were censored at the last follow-up date. (NCT01266031)
Timeframe: up to 30 months.

InterventionMonths (Median)
Bevacizumab9.24
Bevacizumab + Vorinostat 400 mg7.80

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Mean Symptom Severity Using the MD Anderson Symptom Inventory-Brain Tumor Module (MDASI-BT) Self Reporting Tool

"Overall mean severity of 22 symptoms. Symptoms are rated 0-10, zero is not present and 10 is as bad as you can imagine. All patients with at least one valid questionnaire will be included in the analyses." (NCT01266031)
Timeframe: Baseline, week 4 (cycle 2), week 8 (cycle 4), and end of therapy, approximately week 52 (cycle 12)

Interventionscore on a scale (Mean)
BaselineCycle 2Cycle 4End of therapy
All Participants1.61.31.92.2

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Percentage of Patients Rating Their Symptoms to be 7 or Greater on a 0-10 Scale Using the Mean Severity of the MD Anderson Symptom Inventory-Brain Tumor Module (MDSAI-BT) Self Reporting Tool

"Percentage of patients rating their symptoms to be 7 or greater on a 0-10 scale using the MD Anderson Symptom Inventory-Brain Tumor Module (MDASI-BT) Self Reporting Tool. Zero is not present and 10 is as bad as you can imagine. All patients with at least one valid questionnaire will be included in the analyses. Differences of at least 2 points will be classified as the minimum clinically meaningful change in the symptom severity and symptom interference measures." (NCT01266031)
Timeframe: Baseline, week 4, week 8, and end of therapy, approximately week 52 (cycle 12)

Interventionpercentage of of participants (Number)
BaselineCycle 2, week 4Cycle 4, week 8End ot therapy, week 52
All Participants2000

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Mean Symptom Interference at the Time of Clinical Evaluation

"Overall mean interference severity of 6 interference items. Interference is rated 0-10, zero is did not interfere and 10 is as bad as you can imagine. All patients with at least one valid questionnaire will be included in the analyses." (NCT01266031)
Timeframe: Baseline, (cycle 2), week 8 (cycle 4), and end of therapy, approximately week 52 (cycle 12)

Interventionscore on a scale (Mean)
BaselineCycle 2Cycle 4End of therapy
All Participants2.21.72.92.9

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Progression Free Survival (PFS) at 6 Months

"PFS is time measured in months to disease progression as assessed at six months from participant registration. Assessments continue every 8 weeks up to 28 days after last dose (follow-up), anticipated trial length one year.~Participants must be assessed at least 4 weeks after surgery to begin treatment in the adaptive randomized Phase 2 portion of the trial. PFS in participants in the surgical arm determined from the date of randomization to the treatment arms and not from the date of registration in the trial.~Study outcome measure period ended June 2015." (NCT01266031)
Timeframe: Baseline until disease progression or death due to any cause, up to six months

InterventionMonths (Median)
Bevacizumab0.29
Bevacizumab + Vorinostat 400 mg0.23

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Response Rate According to Response Evaluation Criteria in Solid Tumors

Per Response Evaluation Criteria in Solid Tumors Criteria (RECIST v1.1) for target lesions and assessed by CT and MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the diameters of target lesions, taking as reference the baseline sum diameters; Overall Response (OR) = CR + PR. (NCT01267240)
Timeframe: Up to 1 year

Interventionparticipants (Number)
Arm I (Capecitabine, Vorinostat)2

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Progression-free Survival

"PFS is defined as the duration of time from start of treatment to time of progression, death, or completion of the 1-year follow-up, whichever occurs first.~Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1), as at least a 20% increase in the sum of the longest diameter of target lesions." (NCT01267240)
Timeframe: From time of treatment initiation to disease progression, death, or completion of the 1 year follow-up, whichever occurs first.

Interventionmonths (Median)
Arm I (Capecitabine, Vorinostat)2.3

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Survival

Overall survival is defined as the length of time from start of treatment to death from any cause. Estimated using the Kaplan-Meier method. (NCT01267240)
Timeframe: Up to 1 year

Interventionmonths (Median)
Arm I (Capecitabine, Vorinostat)10.8

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Number of Subjects Who Achieved Complete Remission of Their Disease

Complete Remission (CR): A CR requires that the following be recorded concurrently: an absolute neutrophil count (segs and bands) > 1000/μL, no circulating blasts, platelets > 100,000/μL; adequate bone marrow cellularity with trilineage hematopoiesis, and < 5% marrow leukemia blast cells. All previous extramedullary manifestations of disease must be absent. If patients continue on with treatment, there can be no evidence of recurrence of ALL for at least 4 weeks. (NCT01312818)
Timeframe: Day 30

Interventionparticipants (Number)
ALL Treated Patients0

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Number of Participants Exhibiting an in Vivo Resting CD4+ T Cell- Associated HIV RNA (RCVL) Increase After Receiving a Single Dose of VOR 400 mg PO

Participants in Arm 1 and 2 were analyzed in Step 2 for an in vivo increase in resting CD4+ T cell- associated HIV RNA (RCVL) after administration of a single dose of VOR 400 mg PO (NCT01319383)
Timeframe: Arm1: Baseline, Visit 5 and Arm 2: Baseline and Visit 3

InterventionParticipants (Count of Participants)
1/Single & Multiple Dose, Step 2, Visit 58
2/Interval Dosing, Visit 34

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Number of Participants Developing Cancer Within 5 Years Following >/= 8 Vorinostat Dose Exposures

Development of a new cancer within the 5 years of taking their last dose of VOR 400 mg PO.All participants receiving one or more doses of VOR 400 mg PO in any and all Arms of the study. Pre-specified to be reported as one group. (NCT01319383)
Timeframe: From last dose Vorinostat to 5 years afterwards

InterventionParticipants (Count of Participants)
1/Single and Multiple Dose, Step 30
2/Interval Doses (Multiple) Step 40

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Number of Participants With Measurable Changes in Plasma HIV-1 RNA

Assess for detectible HIV-1 RNA > 150 copies/mL, confirmed by repeat evaluation, following VOR dose. By standard assay and single copy assay. Pre specified to combine all participants into one arm. (NCT01319383)
Timeframe: 1 week after last VOR dose

InterventionParticipants (Count of Participants)
1/Single & Multiple Dose, Steps 2 and 30
2/Interval Dosing, Steps 2, 3 and 40

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Number of Participants With a Significant in Vivo Response in Resting Cell Infection (RCI) and HIV RNA After Paired Doses

Induction of significant in vivo RCI and RCLV response after 2 doses of VOR 400 mg PO administered 48 hours apart or 72 hours apart (NCT01319383)
Timeframe: Baseline, Visit 6

InterventionParticipants (Count of Participants)
Interval Dosing , Step 3 (48 hr Interval)0
Interval Dosing, Step 3 (72 Hour Interval)6

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Number of Participants Exhibiting an in Vivo Resting CD4+ T-cell-associated HIV RNA (Rc-RNA) Increase Following Multiple (n = 10) Interval Doses

Participants in Arm 2, Step 4 were analyzed for an in vivo increase in the resting CD4+ T cell- associated HIV RNA (RCVL) after administration of 10 doses of VOR 400 mg PO, given 72 hours apart. (NCT01319383)
Timeframe: Baseline, Visit 9

InterventionParticipants (Count of Participants)
Interval Doses (Multiple) Step 43

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Number of Participants Exhibiting an in Vivo Resting CD4+ T-cell-associated HIV RNA (Rc-RNA) Increase Following Each of Two Multiple Dose Cycles (11 Doses/Cycle)

Participants in Arm 1, Step 3 were analyzed for an in vivo increase in the resting CD4+ T cell- associated HIV RNA (RCVL) after 11 doses of VOR 400 mg PO. This cycle was repeated after a 5 - 8 week rest period for a 2nd series and measurement. (NCT01319383)
Timeframe: Baseline, Visit 18, Visit 29

InterventionParticipants (Count of Participants)
Arm 1 - Single and Multiple Dose, Step 30

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Mean Change in Metabolite Levels

Baseline MRS was performed 1-3 days before initiation of treatment. Follow-up MRS studies were performed at day 7. A standard quadrature head coil was used to collect MR data. The change of metabolite level in choline (Cho) and N-acetyl aspartate (NAA) were calculated in ratio by (metabolite after treatment / metabolite before treatment - 1). The reported ratios represent the Cho-to-NAA ratio at day 7 compared with day 0. (NCT01342757)
Timeframe: Baseline to 1 week

InterventionCho/NAA Ratios (Mean)
Metabolic RespondersMetabolic Non-Responders
Arm I-0.150.29

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Measurable Change on Magnetic Resonance Spectroscopy Imaging After Vorinostat Administration

Changes in magnetic resonance spectroscopic imaging signal and semiquantitative analysis of inositol, choline, lactate, and N-acetyl aspartate (NAA) signal are measured. The values for each of these metabolites are normalized to baseline at one and nine weeks. The values of all the metabolites at one week are added and this is the magnetic resonance spectroscopic index for one week. This is done again at nine weeks. The number is unitless and there is no range limit. Positive values represent normalization of tumor metabolism and negative values suggest no improvement or worsening of metabolic character. (NCT01342757)
Timeframe: 9 weeks

InterventionSpectroscopic index (Mean)
Arm I0

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Proportion of Patients With Magnetic Resonance Spectroscopy (MRS) Response to Initial Vorinostat by MRI and MRS Scans as Determined by Spectroscopic Index

Changes in magnetic resonance spectroscopic imaging signal and semiquantitative analysis of inositol, choline, lactate, and N-acetylaspartate signal are measured. The values for each of these metabolites are normalized to baseline at one and nine weeks. The values of all the metabolites at one week are added and this is the magnetic resonance spectroscopic index for one week. This is done again at nine weeks. The number is unitless and there is no range limit. Positive values represent normalization of tumor metabolism and negative values suggest no improvement or worsening of metabolic character. (NCT01342757)
Timeframe: 9 weeks

Interventionparticipants (Number)
Arm I0

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Maximum Tolerated Dose (MTD) (Phase I)

The highest dose tested in which fewer than 33% of patients experience an attributable DLT to the study drug, when at least 6 patients are treated at that dose and are evaluable for toxicity. The MTD is one dose level below the lowest dose in which 33% or more of the patients experience a DLT. The MTD is based on the first cycle of therapy. The recommended Phase II dose is generally the MTD, although secondary considerations of toxicity and dose reductions on subsequent cycles and other secondary considerations may result in the recommended Phase II dose being below the MTD. (NCT01413750)
Timeframe: 4 weeks from start of treatment, up to 1 year

Interventionmg (Number)
Phase I800

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Progression-free Survival (PFS)

"Estimated using the product-limit method of Kaplan and Meier.~PFS defined as time from randomization to progression or death due to any cause.~Progression defined as Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions." (NCT01413750)
Timeframe: From first day of treatment to the first observation of disease progression or death due to any cause, assessed up to 1 year

Interventionmonths (Median)
Phase II: Vorinostat4.1
Phase II: Placebo7.3

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Dose Limiting Toxicity (DLT) (Phase I)

DLT is defined as any grade III or higher non-hematological toxicity except nausea, vomiting or alopecia. Nausea or vomiting (> grade 2) that last longer than 48 hours despite maximal medical therapy. Absolute neutrophil count < 1000/uL lasting longer than 7 days. Grade 4 thrombocytopenia (platelet < 25,000/uL). Grade 3 or 4 neutropenia associated with sepsis or fever > 38 C. Delay in starting cycle 2 by more than 2 weeks due to toxicity.Abnormal non-hematological laboratory criteria (Grade 3 or higher) will be considered a DLT, if clinically significant and drug-related. If baseline value is elevated prior to drug therapy, an increase will not be considered a DLT unless there is an elevation by more than 2 grades, and it is of clinical significance. Dose escalation schedule for vorinostat: 600 mg QD; 800 mg QD. (NCT01413750)
Timeframe: 4 weeks from start of treatment, up to 1 year

Interventionparticipants with DLTs (Number)
Phase I: Dose Level 11
Phase I: Dose Level 20

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Number of Participants Who Experienced a Dose Limiting Toxicity (DLT).

To evaluate the side effects of giving decitabine and vorinostat before and during chemotherapy using the standard drugs vincristine, dexamethasone, PEG-asparaginase and mitoxantrone. (NCT01483690)
Timeframe: 6 weeks

,
InterventionParticipants (Count of Participants)
# of patients with DLT# of patients without DLT# of patients not evaluable
Initial Dose Level221
Modified Dose Level1125

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Disease Response Rate After Treatment.

Bone marrow evaluation was performed on Day 35 of study to evaluate treatment response. CR defined as attaining M1 marrow (<5% blasts) with no evidence of circulating blasts or extramedullary disease in addition to recovery of peripheral blood counts (ANC >750/uL and platelet count >75,000/uL). CRp was defined as attaining an M1 marrow with no evidence of circulating blasts or extramedullary disease in addition to recovery of ANC but insufficient recovery of platelets. CRi was attaining M1 marrow with no evidence of circulating blasts or extramedullary disease but insufficient recovery of ANC with or without sufficient recovery of platelets. PR was defined as no evidence of circulating blasts and achievement of M2 marrow (5-25% blasts) without new sites of disease and with recovery of ANC. SD is for patients who did not meet the criteria for PR, CR, CRp, or CRi. PD is an increase of at least 25% in the absolute number of leukemia cells or development of new sites. (NCT01483690)
Timeframe: 6 weeks

,
InterventionParticipants (Count of Participants)
complete response (CR)complete response without platelet recovery (CRp)complete remission with incomplete recovery (CRi)stable disease (SD)patient not evaluable for response
Initial Dose Level01112
Modified Dose Level13347

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Response Rate (Phase II)

A response is any of complete hematological remission, partial remission, or hematologic improvement. (NCT01522976)
Timeframe: Up to 5 years

Interventionpercentage of patients having a response (Number)
Arm 1: Azacitidine/Lenalidomide49
Arm 2: Azacitidine38
Arm 3: Azacitidine/Vorinostat27

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Relapse-free Survival

RFS is calculated for patients who have achieved a response. RFS will be measured from the date of response to the date of first documentation of relapse from response (as defined in the primary objective), or death due to any cause. The follow-up for patients last known to be alive and without report of relapse is censored at the date of last contact. RFS will be estimated for each of the three arms using the Kaplan-Meier method. (NCT01522976)
Timeframe: Up to 5 years

InterventionDays (Median)
Arm 1: Azacitidine/Lenalidomide435
Arm 2: Azacitidine311
Arm 3: Azacitidine/Vorinostat455

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Overall Survival

OS is calculated for all patients from the date of initial registration to date of death due to any cause. The follow- up for patients last known to be alive is censored at the date of last contact. OS will be estimated for each of the three arms using the Kaplan-Meier method. (NCT01522976)
Timeframe: Up to 5 years

InterventionDays (Median)
Arm 1: Azacitidine/Lenalidomide588
Arm 2: Azacitidine449
Arm 3: Azacitidine/Vorinostat527

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Toxicity Rate

Adverse events that are possibly, probably or definitely related to study drug are reported. (NCT01522976)
Timeframe: Up to 5 years

,,
InterventionParticipants (Number)
Abdominal infectionAbdominal painAcute kidney injuryAdult respiratory distress syndromeAlanine aminotransferase increasedAnemiaAnorectal infectionAnorexiaApneaAscitesAspartate aminotransferase increasedAtaxiaBack painBlood and lymphatic system disorders - OtherBlood bilirubin increasedBronchial infectionCD4 lymphocytes decreasedCardiac arrestCatheter related infectionCecal infectionCholecystitisColitisConfusionConstipationCreatinine increasedDehydrationDeliriumDiarrheaDizzinessDyspneaEpistaxisEsophageal painEsophagitisFallFatigueFebrile neutropeniaFeverFlushingGastric hemorrhageGastrointestinal painGeneral disorders and admin site conditions-OtherGeneralized muscle weaknessHallucinationsHeadacheHeart failureHematomaHematuriaHyperglycemiaHypernatremiaHypertensionHyperuricemiaHypoalbuminemiaHypokalemiaHypomagnesemiaHyponatremiaHypophosphatemiaHypotensionHypoxiaInfections and infestations - Other, specifyIntracranial hemorrhageInvestigations - Other, specifyLeukocytosisLower gastrointestinal hemorrhageLung infectionLymphocyte count decreasedLymphocyte count increasedMucosal infectionMucositis oralNauseaNeutrophil count decreasedPainPapulopustular rashPericardial effusionPlatelet count decreasedPneumonitisPruritusPulmonary edemaPurpuraRash maculo-papularRenal and urinary disorders - Other, specifyRespiratory failureSepsisSinus bradycardiaSkin infectionSoft tissue infectionSudden death NOSSyncopeThromboembolic eventTooth infectionUpper gastrointestinal hemorrhageUpper respiratory infectionUrinary tract infectionVascular disorders - Other, specifyVomitingWeight lossWhite blood cell decreased
Arm 1: Azacitidine/Lenalidomide1101048040100100011100002250514001091600011300001101034151404110041400116911161010113004131021000101148
Arm 2: Azacitidine00000370000000200002000010100020000611000001000001100000100020010191002480004600003002011100001101034
Arm 3: Azacitidine/Vorinostat031054413113101310011111103130311011413211103111122021010423150002231102630006410101113020041110111044

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Pre-study Cytogenetic Abnormalities

Cytogenetic risk group is used to identify cytogenetic abnormalities. (NCT01522976)
Timeframe: Up to 5 years

,,
Interventionparticipants (Number)
Good/very goodIntermediatePoorVery poorMissing
Arm 1: Azacitidine/Lenalidomide351382314
Arm 2: Azacitidine2916102314
Arm 3: Azacitidine/Vorinostat341881913

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Number of Patients With Dose Limiting Toxicity

The number of patients who had a DLT during the dose finding/confirming portion (Phase I) of the trial for the safety of the combination of sorafenib, vorinostat, and bortezomib. (NCT01534260)
Timeframe: up to 9 months

InterventionParticipants (Count of Participants)
Phase I Dose Escalating0

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Phase II - Percentage of Patients With a Partial Response or Greater

Evaluate the overall response rate of patients receiving therapy. Patients are considered as having a response if their overall response is Partial Response or better. The percentage of patients achieving this and the exact 95% confidence interval will be calculated. Responses will be defined using the response criteria determined by the International Working Group for AML. (NCT01534260)
Timeframe: up to 9 months

Interventionpercentage of participants (Number)
Phase II at MTD40.0

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Phase II - Time to Relapse

Will be examined using Kaplan-Meier estimates. Time from date of confirmed complete remission to date of relapse. The observations of patients who died or remained alive and relapse free were censored at date of death or last disease evaluation, respectively. (NCT01534260)
Timeframe: Up to one year

Interventiondays (Median)
Phase II at MTD32

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Complete Remission (CR)

"This study evaluates the clinical efficacy of temozolomide + vorinostat as administered to Groups 1 and 2, assessed as the rate of complete remission [CR, aka morphologic complete remission (mCR)], defined as the morphologic leukemia-free state (MLFS), WITH absolute neutrophil count (ANC) ≥ 1,000/µL AND platelets (PLT) ≥ 100,000/µL. The outcome is reported as the percentage without dispersion of participants in Groups 1 and 2 that demonstrated CR. CR is defined as all of the following.~MLFS = < 5% blasts in bone marrow aspirate containing marrow spicules > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease ANC = ≥ 1,000/µL PLT = ≥ 100,000/µL" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Complete Remission With Incomplete Blood Count Recovery (CRp)

"The rate of complete remission with incomplete blood count recovery (CRp) for Groups 1 and 2 was assessed as the rate of morphologic leukemia-free state (MLFS) but with EITHER residual neutropenia (ANC < 1,000/µL) OR residual thrombocytopenia (PLT < 100,000/µL). MLFS is defined as follows.~MLFS = < 5% blasts in bone marrow aspirate containing marrow spicules > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)1

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Cytogenetic Response (CyR)

"Cytogenetic response (CyR) is defined as complete remission (CR), PLUS a documented decrease or absence of cytogenetic abnormalities, when analyzed microscopically for 20 cellular metaphases (actively dividing cells). The outcome is reported as the percentage without dispersion of participants in Groups 1 and 2 that demonstrated CyR. CR is defined as all of the following.~CR = < 5% blasts in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods; no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Disease-free Survival (DFS) at 2 Years

"Disease-Free Survival (DFS) is defined as survival after complete response (CR) without disease progression. DFS is reported as the percentage without dispersion of participants in Groups 1 and 2 that experienced CR and were alive without progression (ie, without disease) 2 years after induction chemotherapy. CR is defined as all of the following.~CR = < 5% blasts in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods; no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL" (NCT01550224)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Morphologic Leukemia-free State (MLFS)

"The rate of morphologic leukemia-free state (MLFS) is reported as the percentage without dispersion of participants in Groups 1 and 2 that achieve MLFS. The outcome is reported as the percentage without dispersion of participants in Groups 1 and 2 that demonstrated MLFS. This assessment is independent of absolute neutrophil count (ANC) or platelets (PLT) recovery status. MLFS is defined below.~MLFS = < 5% blasts in bone marrow aspirate containing marrow spicules > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)1

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Overall Survival (OS) at 2 Years

Overall Survival (OS) is defined as survival regardless of clinical status. OS is reported as the percentage without dispersion of participants in Groups 1 and 2 that remained alive 2 years after induction chemotherapy. (NCT01550224)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Partial Remission (PR)

"Partial remission (PR) is reported as the percentage without dispersion of participants in Groups 1 and 2 that demonstrated PR. PR is defined as all of the following.~PR = 5% to 25% blasts (must be ≥ 50% reduction of blasts) in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Relapse-Free Survival (RFS) at 2 Years

"Relapse-free survival (RFS) is defined as survival after complete response (CR) or (PR) without further disease progression. RFS is reported as the percentage without dispersion of participants in Groups 1 and 2 that experienced CR or PR, and were alive without progression 2 years after induction chemotherapy. CR and PR are defined as the following.~CR = < 5% blasts in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods; no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL~PR = 5% to 25% blasts (must be ≥ 50% reduction of blasts) in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL" (NCT01550224)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)0
Participant Group 2 (Non-methylated MGMT Promoter)0

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Treatment Failure (TF)

"Treatment failure (TF) is defined as failing to achieve either a complete remission (CR) or partial remission (PR) after induction chemotherapy. The outcome is reported as the percentage without dispersion of participants in Groups 1 and 2 that experienced TF. CR and PR are defined as the following.~CR = < 5% blasts in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods; no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL~PR = 5% to 25% blasts (must be ≥ 50% reduction of blasts) in bone marrow aspirate containing marrow spicules; > 200 nucleated cells no blasts with Auer rods no persistence of extramedullary disease absolute neutrophil count (ANC) ≥ 1,000/µL platelets (PLT) ≥ 100,000/µL" (NCT01550224)
Timeframe: up to 10 weeks

InterventionParticipants (Count of Participants)
Participant Group 1 (Methylated MGMT Promoter)3
Participant Group 2 (Non-methylated MGMT Promoter)20

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Overall Survival

Patients alive at 1 year. (NCT01593670)
Timeframe: 1 Year

InterventionParticipants (Count of Participants)
Patients With High Risk MDS3

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Number of Patients Who Had Natural Killer (NK) Cell Expansion

NK cell expansion is defined as the presence of donor NK cells in the recipient at Day 8 post NK cell infusion. (NCT01593670)
Timeframe: After Cycle 2 (approx. 3 months)

InterventionParticipants (Count of Participants)
Patients With High Risk MDS0

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Number of Patients Who Experienced Grade 3 or Higher Non-hematologic Adverse Events

Adverse events (AEs) will be graded using Common Terminology Criteria for Adverse Events v4.0 (CTCAE). Non-hematologic adverse events are defined as untoward medical occurrences associated with the use of a study drug whether or not considered study drug related, excluding those events involving white blood cells, neutrophils, red blood cells or platelets. In general, grade 3 AEs are defined as 1) being severe or medically significant but,not immediately life-threatening; 2) requiring hospitalization or prolongation of hospitalization; 3) disabling; or 4) limiting self care activities. Grade 4 AEs are defined as 1) having life-threatening consequences; or 2) requiring urgent intervention. Grade 5 AEs are defined as causing death related to an adverse event. (NCT01593670)
Timeframe: Day 1 through Month 3

InterventionParticipants (Count of Participants)
Patients With High Risk MDS7

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Number of Patients Who Became Transfusion Independent

(NCT01593670)
Timeframe: 4-6 Months Post Start of Cycle 1

InterventionParticipants (Count of Participants)
Patients With High Risk MDS0

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The Number of Patients Who Achieved a Clinical Response

Clinical response includes: Complete Response (less than 5% myeloblasts present in the bone marrow and in the peripheral blood a hemoglobin of at least 11g/dl, platelets of at least 100 X 10E9/L, neutrophils of at least 1.0 X 10E9/L, and blasts 0%); Partial Response (all Complete Response criteria if previously abnormal except bone marrow myeloblasts are decreased by more than 50% over pre-treatment, but still greater than 5%); and hematologic improvement (a hemoglobin increase of greater than 1.5g/dl or decreased red blood cell transfusions by at least 4 per 8 week period, a platelet increase of more than 30 X 10E9/L for patients with a baseline of more than 20 X 10E9/L or an increase by 100% for those with a baseline of less than 20 X 10E9/L, and a neutrophil increase of at least 100% and an absolute increase of greater than 0.5 X 10E9/L. (NCT01593670)
Timeframe: After 2 Courses of Treatment (Approx. 3 months)

InterventionParticipants (Count of Participants)
Patients With High Risk MDS5

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Duration of Response

Duration of response will be summarized for responders. (NCT01720602)
Timeframe: Up to 5 years

Interventionweeks (Median)
Treatment (Vorinostat, AI Therapy)29.6

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Response Rate According to RECIST

"A 90% score (Wilson) confidence interval will be computed for the response rate.~Clinical benefit according to Recist score is defined as: Stable Disease, Partial Remission or Complete Remission. Lack of clinical benefit is defined as Progressive Disease (increase in target lesion size by 20% or more)." (NCT01720602)
Timeframe: 8 weeks

Interventionpercentage of patients (Number)
Treatment (Vorinostat, AI Therapy)60

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Rate of Clinical Benefit of Patients Receiving Vorinostat/AI Combination Therapy According to RECIST

"A 90% score (Wilson) confidence interval will be computed for the rate of clinical benefit.~Clinical benefit according to Recist score is defined as: Stable Disease, Partial Remission or Complete Remission. Lack of clinical benefit is defined as Progressive Disease (increase in target lesion size by 20% or more)." (NCT01720602)
Timeframe: 8 weeks

Interventionpercentage of patients (Number)
Treatment (Vorinostat, AI Therapy)60

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Progression-free Survival (PFS)

Progression-free survival is assessed relative to the start of the study therapy. Progression can be determined by RECIST 1.1, elevated tumor markers, worsening clinical symptoms or new lesions identified by FDG-PET or bone scan. (NCT01720602)
Timeframe: From the time of start of study therapy to documented progression - up to 5 years

Interventionmonths (Median)
Treatment (Vorinostat, AI Therapy)2

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Overall Survival

Overall survival is assessed relative to the start of the study therapy to the date of death, from any cause. (NCT01720602)
Timeframe: From the time of start of study therapy to date of documented death

Interventionmonths (Median)
Treatment (Vorinostat, AI Therapy)19

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Quality of Life (QoL) Assessment - Skindex-29 Symptoms Scale Score

"Skindex-29 rates 29 items assessing 3 domains (emotions, symptoms, & functioning) on a linear scale from 0 (never) to all the time (100). Higher scores = higher impact of skin disease.~FACT-G rates 27 items in 4 domains (physical well-being, social/family well-being, emotional well-being, functional well-being) on a 5-point scale from 0 (not at all) to 4 (very much). Higher scores = better QoL.~EuroQoL lvl 3 (Eq-5D-3L) rates mobility, self-care, usual activities, pain/discomfort and anxiety/depression on 3 levels - no problems, some problems, extreme problems. Score is calculated using a set of item weights to derive a single score ranging from -0.109 to 1, with 1 representing full health.~LS mean (and 95% CI) of the overall change from baseline across time points through 6-month assessment (including End of Cycles 1, 3, and 5 time points only) are calculated from MMRM with treatment, disease type, disease stage, and region as fixed effects and baseline score as a covariate." (NCT01728805)
Timeframe: Cycle 1, 3, and 5

,
Interventionscore on a scale (Least Squares Mean)
Skindex-29 Across 6-month AssessmentFACT-G Across 6-month AssessmentEQ-5D-3L Across 6-month Assessment
KW-0761-12.64.60.06
Vorinostat-6.0-2.30.02

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Progression Free Survival

"Progression was defined as follows, based on Olsen (2011):~Lymph nodes: ≥ 50% increase in SPD from baseline of lymph nodes, any new node > 1.5 cm in the long axis or > 1 cm in the short axis if 1-1.5 cm in the long axis that is proven to be N3 histologically, or > 50% increase from nadir in SPD of lymph nodes in those with PR~Skin: ≥ 25% increase in skin disease from baseline, new tumors (T3) in patients with T1, T2 or T4 only skin disease, or in those with CR or PR, increase of skin score of greater than the sum of nadir plus 50% baseline score~Blood: B0 to B2, > 50% increase from baseline and at least 5,000 neoplastic cells/μL36, or > 50% increase from nadir and at least 5,000 neoplastic cells/μL~Viscera: > 50% increase in size (SPD) of any organs involved at baseline, new organ involvement, or > 50% increase from nadir in the size (SPD) of any previous organ involvement in those with PR" (NCT01728805)
Timeframe: From date of randomization at every visit until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 36 months

,
Interventionpercentage of subjects (Number)
Rate (%) of Being Alive w/o Progression at 6 mos.Rate (%) of Being Alive w/o Progression at 12 mos.Rate (%) of Being Alive w/o Progression at 18 mos.Rate (%) of Being Alive w/o Progression at 24 mos.Rate (%) of Being Alive w/o Progression at 30 mos.
KW-076155.338.328.014.14.7
Vorinostat28.815.37.27.27.2

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Overall Response Rate

The ORR was defined as the count of subjects who had a confirmed CR or PR, defined as documented CR or PR per Global Composite Response Score that was confirmed by a subsequent observation at least 4 weeks later. Overall Response Rate was determined based on the response in all compartments (lymph nodes, skin, peripheral blood, and viscera), referencing Olsen, 2011 as follows: Complete Response (CR) = complete disappearance of all clinical evidence of disease; Partial Response (PR) = regression of measurable disease; Stable Disease (SD) = failure to attain CR, PR, or PD; Progressive Disease (PD) = PD in any compartment; Relapse = recurrence of disease in prior CR in any compartment. (NCT01728805)
Timeframe: at the end of cycle 1 (26-28 days), and then every other cycle in Year 1 (cycle 3, 5, 7, 9, 11, 13), and every 16 weeks (cycle 17, 21, etc.) in Year 2 and beyond until progression up to 36 months

,
InterventionParticipants (Count of Participants)
All Subjects ORR (confirmed CR + PR)Disease Type = MF ORR (confirmed CR + PR)Disease Type = SS ORR (confirmed CR + PR)
KW-0761522230
Vorinostat972

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Pruritis Evaluation

"The Itchy QoL is a validated pruritus specific quality of life instrument. It includes 22 pruritus-specific questions covering three major domains: symptoms, functioning, and emotions. The scale ranges from Never (1) to All The Time (5). The subscale scores consist of the average of the responses to the items in a given subscale. The overall score is the average of the responses to all items. Higher Itchy QoL scores indicate worse quality of life.~LS mean (and 95% CI) of the overall change from baseline across time points through 6-month assessment (including End of Cycles 1, 3, and 5 time points only) are calculated from MMRM with treatment, disease type, disease stage, and region as fixed effects and baseline score as a covariate." (NCT01728805)
Timeframe: Cycle 1, 3, and 5

Interventionscore on a scale (Least Squares Mean)
KW-0761-0.5
Vorinostat-0.4

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Six-month Progression-free Survival (PFS6)

The percentage of participants alive and progression-free at 6 months after the start of study treatment will be determined. Based on Response Assessment in Neuro-Oncology (RANO) criteria, progression is defined as a ≥ 25% increase in sum of the products of perpendicular diameters of enhancing lesions; significant increase in T2/FLAIR; any new lesion; clear clinical deterioration not attributable to other causes apart from the tumor; failure to return for evaluation as a result of death or deteriorating condition; or clear progression of non-measurable disease. PFS6 will be calculated from the date study treatment started until the date of progression or death, or the date of last follow-up if participants are alive without progression. Kaplan-Meier methods will be used to estimate survival. (NCT01738646)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Vorinostat & Bevacizumab30

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Radiographic Response

The percentage of participants with a complete or partial response as determined by modified Response Assessment in Neuro-Oncology (RANO) criteria will be determined. Complete Response (CR) is defined as complete disappearance on MR/CT of all enhancing tumor and mass effect, off all corticosteroids (or receiving only adrenal replacement doses) and accompanied by a stable or improving neurologic examination. Partial Response (PR) is defined as greater than or equal to 50% reduction in tumor size on MR/CT by bi-dimensional measurement, on a stable or decreasing dose of corticosteroids and accompanied by a stable or improving neurologic examination. Tumor assessments are done at baseline and the end of every second cycle (every 8 weeks) thereafter. (NCT01738646)
Timeframe: 3 Years

Interventionpercentage of participants (Number)
Vorinostat & Bevacizumab22.5

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Percentage of Participants Who Experience Grade 3 or Greater, Treatment Related, Non-hematologic Toxicities.

The percentage of participants who experience grade 3 or greater, treatment-related, non-hematologic toxicities will be calculated. (NCT01738646)
Timeframe: 2.7 Years

Interventionpercentage of participants (Number)
Vorinostat & Bevacizumab40

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Median Progression-free Survival (PFS)

Progression-free survival is defined as the time in months from the start of protocol treatment until the date of progression or death if death occurred before progression. If the participant is alive and progression-free, PFS will be censored at the date of last follow-up. Kaplan-Meier methods will be used to estimate progression-free survival. (NCT01738646)
Timeframe: 3 Years

Interventionmonths (Median)
Vorinostat & Bevacizumab3.7

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Median Overall Survival (OS)

Overall survival is defined as the time in months from the start of protocol treatment until the date of death, or the date of last follow-up if alive. Kaplan-Meier methods will be used to estimate overall survival. (NCT01738646)
Timeframe: 3 Years

Interventionmonths (Median)
Vorinostat & Bevacizumab10.4

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Response Rate

"All eligible patients will be treated with Azacitidine and oral vorinostat for 6 cycles of 28 days.~The response rate (CR, PR, HI or marrow CR) will be evaluated after six cycles, according to IWG 2006.~In patients still responding after six cycles, the drugs will continue to be supplied, and follow up until death or unacceptable tolerance will be continued in all patients.~Complete Response (CR): Bone marrow: less than 5% myeloblasts with Peripheral blood: HI responses).~Partial remission (RP): Bone marrow blasts decreased by at least 50% but still more than 5% with Peripheral blood: HI responses).~Marrow CR:Bone marrow: maximum of 5% myeloblasts and decrease by at least 50% over pretreatment~HI (hematologic improvement)~Erythroid response: Hgb increase at least by 1.5 g/dL~Platelet response: Increase from less than 20x109/L to more than 20x109/L and by at least 100%~Neutrophil response: At least 100% increase and an absolute increase of at least 0.5x109/L" (NCT01748240)
Timeframe: 6 month

Interventionpercentage of response (Number)
Azacitidine and Oral Vorinostat5

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The Percentage of Patients Alive at 1 Year

The percentage of patients alive at 1 year (NCT01789255)
Timeframe: Up to 1 year

Interventionpercentage of patients (Number)
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)76

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The Number of Participants That Experience Grade 2-4 Acute GVHD (Graft Versus Host Disease) by Day 100

"The incidence of grade 2-4 acute GVHD (Graft Versus Host Disease) by day 100~Grade 2 GVHD: Maculopapular rash covering 25-50% of BSA (Body Surface Area), bilirubin between 3.1-6 mg/dl, and/ or adult stool output between 1000-1500 ml/day (child between 20-30 ml/kg/day).~Grade 3 GVHD: Maculopapular rash covering >50% of BSA, bilirubin between 6.1-15 mg/dl, and/ or adult stool output >1500 ml/day (child >30 ml/kg/day).~Grade 4 GVHD: Generalized erythroderma plus bullous formation and desquamation >5% BSA, bilirubin >15 mg/dl, and/ or severe abdominal pain with or without ileus, or grossly bloody stool." (NCT01789255)
Timeframe: Day 100

Interventionparticipants (Number)
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)2

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Mean Percent of Planned Dose Administered

The addition of vorinostat to tacrolimus and methotrexate for GVHD prophylaxis will be considered feasible if 60% or more of the planned doses are administered. (NCT01789255)
Timeframe: Up to day 30

Interventionpercent of dose administered (Mean)
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)82.5

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Median Plasma Concentration of IL-6 in Patients Treated With Vorinostat and Patients Not Treated With Vorinostat

Median plasma concentration of IL-6 (Interleukin-6 cytokine) was compared in patients treated with Vorinostat to those not treated with Vorinostat. (NCT01789255)
Timeframe: Up to day 100

Interventionpg/mL (Median)
Treated with VorinostatNot Treated with Vorinostat
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)4.27.6

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Median Ac-H3 Levels in Patients Treated With Vorinostat and Patients Not Treated With Vorinostat

Median Ac-H3 levels ( depicted as a ratio of ac-H2 optical density (OD) and beta actin OD) were compared in patients treated with Vorinostat to patients not treated with Vorinostat. Optical Density is a dimensionless unit. (NCT01789255)
Timeframe: Up to day 100

InterventionRatio (Median)
Treated with VorinostatNot Treated with Vorinostat
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)0.9430.679

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The Percentage of Patients With Relapse at 1 Year

(NCT01789255)
Timeframe: Up to 1 year

Interventionpercentage of patients (Number)
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)19

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The Percentage of Patients Alive Without GVHD or Use of Steroids

The percentage of patients alive without GVHD or use of steroids at 1 year. (NCT01789255)
Timeframe: Up to 1 year

Interventionpercentage of patients (Number)
Supportive Care (Vorinostat, Tacrolimus, Methotrexate)47

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Non-Relapse Mortality Incidence

(NCT01790568)
Timeframe: 1 year

Interventionpercentage of patients (Number)
Vorinostat16

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Percentage of Patients Alive at 1 Year

Overall survival at 1 Year. (NCT01790568)
Timeframe: 1 Year

Interventionpercentage of patients (Number)
Vorinostat76

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Percentage of Patients That Experience Grade 2-4 GVHD Within 100 Days of Transplant

"GVHD Staging:~Grade 2: (Skin) Maculopapular rash 25-50% BSA, (Liver) bilirubin 3.1-6mg/dl, (Gut) 1000-1500 ml/day for adult and 20-30ml/kg/day for child.~Grade 3: (Skin) Maculopapular rash >50% BSA, (Liver) 6.1-15mg/dl, (Gut) >1500mg/day for adult and >30ml/kg/day for child.~Grade 4: (Skin) Generalized erythroderma plus bullous formation and desquamation >5% BSA, (Liver) >15mg/dl, (Gut) Severe abdominal pain with or without ileus, or grossly bloody stool." (NCT01790568)
Timeframe: 100 Days

Interventionpercentage of patients (Number)
Vorinostat22

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Frequency and Severity of Toxicities

Number of patients with Grade 3-5 adverse events that were possibly, probably or definitely related to study drug are reported by given type of adverse event. (NCT01802333)
Timeframe: Up to 5 years

,,
InterventionParticipants (Count of Participants)
Abdominal distensionAbdominal infectionAbdominal painAcidosisAcute kidney injuryAdult respiratory distress syndromeAlanine aminotransferase increasedAlkaline phosphatase increasedAlkalosisAllergic reactionAnal hemorrhageAnal painAnal ulcerAnemiaAnorectal infectionAnorexiaAspartate aminotransferase increasedAtelectasisAtrial fibrillationAtrial flutterAtrioventricular block completeBlood and lymphatic system disorders - OtherBlood bilirubin increasedBone infectionBone painBronchopulmonary hemorrhageBullous dermatitisCD4 lymphocytes decreasedCardiac arrestCardiac disorders - Other, specifyCardiac troponin I increasedCatheter related infectionChillsChronic kidney diseaseCognitive disturbanceColitisColonic hemorrhageColonic perforationConduction disorderConfusionConjunctivitisConstipationConstrictive pericarditisCreatinine increasedDeath NOSDehydrationDental cariesDevice related infectionDiarrheaDisseminated intravascular coagulationDry mouthDry skinDuodenal hemorrhageDyspepsiaDysphagiaDyspneaEdema cerebralEdema limbsEjection fraction decreasedElectrocardiogram QT corrected interval prolongedEncephalopathyEnterocolitisEnterocolitis infectiousEpistaxisErythema multiformeErythrodermaEsophageal hemorrhageEsophageal painEsophagitisEye infectionFatigueFebrile neutropeniaFeverGGT increasedGait disturbanceGastric hemorrhageGastritisGastroesophageal reflux diseaseGastrointestinal disorders - Other, specifyGeneral disorders and admin site conditions-OtherGeneralized muscle weaknessGenital edemaGlucose intoleranceGum infectionHeadacheHeart failureHematomaHematuriaHepatic failureHepatic infectionHepatobiliary disorders - Other, specifyHyperglycemiaHyperhidrosisHyperkalemiaHypermagnesemiaHypernatremiaHypertensionHyperuricemiaHypoalbuminemiaHypocalcemiaHypoglycemiaHypokalemiaHypomagnesemiaHyponatremiaHypophosphatemiaHypotensionHypoxiaIleusInfections and infestations - Other, specifyInfective myositisInjury, poison and procedural complications-OtherIntracranial hemorrhageInvestigations - Other, specifyIrregular menstruationJejunal obstructionKidney infectionLaryngeal edemaLaryngeal mucositisLeft ventricular systolic dysfunctionLeukocytosisLipase increasedLower gastrointestinal hemorrhageLung infectionLymphocyte count decreasedMenorrhagiaMetabolism and nutrition disorders-Other, specifyMiddle ear inflammationMucosal infectionMucositis oralMulti-organ failureMusculoskeletal and connective tiss disorder-OtherMyalgiaNauseaNeck edemaNervous system disorders - Other, specifyNeutrophil count decreasedNon-cardiac chest painOral painPainPain in extremityPalmar-plantar erythrodysesthesia syndromePapulopustular rashParesthesiaPericardial effusionPericardial tamponadePeriorbital edemaPeripheral sensory neuropathyPharyngeal mucositisPharyngitisPlatelet count decreasedPleural effusionPneumonitisPruritusPulmonary edemaPurpuraRash acneiformRash maculo-papularRectal hemorrhageRectal painRenal and urinary disorders - Other, specifyResp, thoracic and mediastinal disorders - OtherRespiratory failureRestrictive cardiomyopathySalivary duct inflammationScrotal infectionScrotal painSeizureSepsisSinus bradycardiaSinus tachycardiaSinusitisSkin and subcutaneous tissue disorders - OtherSkin infectionSkin ulcerationSmall intestinal obstructionSoft tissue infectionSore throatStomach painStrokeSupraventricular tachycardiaSyncopeTesticular disorderThromboembolic eventThrombotic thrombocytopenic purpuraTooth infectionTumor lysis syndromeTyphlitisUpper gastrointestinal hemorrhageUpper respiratory infectionUrinary incontinenceUrinary tract infectionUrine output decreasedVaginal hemorrhageVascular access complicationVasovagal reactionVentricular tachycardiaVomitingWeight lossWhite blood cell decreasedWound infection
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)114121122100001580580000191010111031003201010111111152001113002001121001301415243001110201123001115100070580180202132018110110010210021891111191007001411511000000011175110101111101311001160020501111002013148120500000321561
Arm II (High-dose Cytarabine, Idarubicin)016153172100101640161503111150112131170209000201061003201120017036216410001211816072020054100022120101211106181702012031124121000600100310122107010018310150112805002100010001680412112600138000002602021000201121000814010200211601500
Arm III (Vorinostat, High-dose Cytarabine, Idarubicin)119244201221011064121211100220030021040015110000040300381000008124205420110101311464130011210043000011601026182512429319921400130100101231477000111511510104100110111010012812150010010214001113412014100201130010923121612110421120

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Cytogenetic Risk Distribution of Patients on This Study

To estimate the cytogenetic risk distribution of patients on this study. (NCT01802333)
Timeframe: Baseline

Interventionpercentage of participants (Number)
High riskIntermediate riskLow risk
All Arms Combined22.364.213.5

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Prevalence of the Mutation NPM1 in Patients on This Study.

To estimate the prevalence of the mutation NPM1 in this patient population. (NCT01802333)
Timeframe: Baseline

Interventionpercentage of patients (Number)
All Arms Combined33

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Rate of Allogeneic HCT

The goal of the transplant objective is to determine whether it is possible to conduct allogeneic HCT on 60% or more of adults with high-risk AML in first complete remission (alternative). If 40% or fewer of high-risk patients in CR can be transplanted, the proposed transplant support system will not be considered feasible. A one-sided binomial test compared to the null transplant rate will be conducted. (NCT01802333)
Timeframe: Up to 5 years

Interventionpercentage of patients (Number)
High Risk Patients in First Complete Remission65

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Overall Survival (OS)

"To compare OS between patients who receive standard 7+3 therapy or IA to patients who receive IA + vorinostat.~OS is calculated for all patients from date of registration to date of death due to any cause. Patients last known to be alive are censored at date of last contact.~2-year OS by arm will be estimated using the Kaplan-Meier method." (NCT01802333)
Timeframe: OS assessed for up to 5 years, 2 year OS reported

InterventionProportion of participants (Number)
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)0.56
Arm II (High-dose Cytarabine, Idarubicin)0.59
Arm III (Vorinostat, High-dose Cytarabine, Idarubicin)0.58

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Complete Response (CR) Rate

"To compare the complete response rate between patients who receive standard 7+3 therapy or IA to patients who receive IA + vorinostat.~Complete response is defined as: ANC >= 1,000/mcl, platelet count >= 100,000/mcl, < 5% bone marrow blasts, no Auer rods, no evidence of extramedullary disease (no requirements for marrow cellularity or hemoglobin concentration)" (NCT01802333)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)75
Arm II (High-dose Cytarabine, Idarubicin)80
Arm III (Vorinostat, High-dose Cytarabine, Idarubicin)77

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Disease-free Survival (DFS)

"To compare the disease-free survival (DFS) between patients who receive standard 7+3 therapy or IA to patients who receive IA + vorinostat.~DFS is calculated for patients who have achieved a CR or CRi (complete response with incomplete blood count recovery) . DFS will be measured from the date of CR or CRi until relapse from CR or CRi for death from any cause. Observation is censored at the date of last follow-up for patients last known to be alive without report of relapse.~2-year DFS by arm will be estimated using the Kaplan-Meier method." (NCT01802333)
Timeframe: DFS assessed for up to 5 years, 2 year DFS reported

InterventionProportion of participants (Number)
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)0.48
Arm II (High-dose Cytarabine, Idarubicin)0.51
Arm III (Vorinostat, High-dose Cytarabine, Idarubicin)0.46

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Disease-free Survival (DFS) Among High Risk Patients

"DFS is calculated for patients who have achieved a CR or CRi (complete response with incomplete blood count recovery). DFS will be measured from the date of CR or CRi until relapse from CR or CRi for death from any cause. Observation is censored at the date of last follow-up for patients last known to be alive without report of relapse.~2-year DFS for high risk patients will be estimated using the Kaplan-Meier method." (NCT01802333)
Timeframe: DFS assessed for up to 5 years, 2 year DFS reported

InterventionProportion of participants (Number)
High Risk Patients0.30

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EFS of Arm I Compared to Arm II

"EFS is calculated for all patients from the date of initial registration on study until the first of the following: death from any cause, relapse from remission (CR or CRi) or completion of protocol Induction/Re-Induction therapy without documentation of CR or CRi.~A two-sided test of the hazard ratio (HR) of 7:3: IA (versus the null hypothesis of HR =1) will be done using a proportional hazards regression model with the stratification factors included as covariates.~2-year EFS by arm will be estimated using the Kaplan-Meier method." (NCT01802333)
Timeframe: EFS assessed for up to 5 years, 2 year EFS reported

InterventionProportion of participants (Number)
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)0.36
Arm II (High-dose Cytarabine, Idarubicin)0.41

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Event-free Survival (EFS)

"EFS is calculated for all patients from the date of initial registration on study until the first of the following: death from any cause, relapse from remission (CR or CRi) or completion of protocol Induction/Re-Induction therapy without documentation of CR or CRi.~2-year EFS by arm will be estimated using the Kaplan-Meier method. EFS will be compared between Arm I and Arm III and between Arm II and Arm III using Cox proportional hazards regression." (NCT01802333)
Timeframe: EFS assessed for up to 5 years, 2 year EFS reported

InterventionProportion of participants (Number)
Arm I (Standard Dose Cytarabine, Daunorubicin Hydrochloride)0.36
Arm II (High-dose Cytarabine, Idarubicin)0.41
Arm III (Vorinostat, High-dose Cytarabine, Idarubicin)0.37

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One-year Overall Survival (OS)

Proportion of participants alive at one year from the start of treatment. (NCT01879085)
Timeframe: Up to one year (per patient)

Interventionproportion of participants (Number)
Phase 20.477

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Objective Response Rate (ORR)

Number of patients with Complete response [CR] + partial response [PR], per RECIST v1.1 criteria . Per RECIST v1.1, CR: Disappearance of all target lesions. Any pathological lymph nodes(whether target or non-target) must have reduction in short axis to <10 mm. For non-target lesions: Disappearance of all non-target lesions and normalization of tumor marker level. All lymph nodes must be non-pathological in size (<10mm short axis);PR: At least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters (NCT01879085)
Timeframe: Up to 7 years and 7 months

InterventionParticipants (Count of Participants)
Phase 27

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Six-month Overall Survival (OS)

Proportion of participants alive at six months from the start of treatment. (NCT01879085)
Timeframe: Up to 6 months (per patient)

Interventionproportion of participants (Number)
Phase 20.742

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Progression-free Survival (PFS)

The median length of time from the beginning of study treatment that patients remain alive without progression of their disease (cancer). Per RECIST v1.1, progressive disease (PD) is defined as at least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5mm. For non-target lesions, PD: Unequivocal progression of existing non-target lesions. The appearance of one or more new lesions is also considered progression. (NCT01879085)
Timeframe: Up to 7 years and 7 months

Interventionmonths (Median)
Phase 25.552361

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Overall Survival (OS)

The median length of time from the start of treatment that diagnosed study participants remain alive. (NCT01879085)
Timeframe: Up to 7 years and 7 months

Interventionmonths (Median)
Phase 211.92608

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One-year Progression-free Survival (PFS)

Proportion of participants whose disease does not progress within one year of start of treatment (number of patients with progressive disease/total number of patients). Per RECIST v1.1, progressive disease (PD) is defined as at least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5mm. For non-target lesions, PD: Unequivocal progression of existing non-target lesions. The appearance of one or more new lesions is also considered progression. (NCT01879085)
Timeframe: Up to one year (per patient)

Interventionproportion of participants (Number)
Phase 20.304

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Six-month Progression-free Survival (PFS)

Proportion of participants whose disease does not progress within 6 months of start of treatment (number of patients without progressive disease/total number of patients). Per RECIST v1.1, progressive disease (PD) is defined as at least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5mm. For non-target lesions, PD: Unequivocal progression of existing non-target lesions. The appearance of one or more new lesions is also considered progression. (NCT01879085)
Timeframe: Up to 6 months (per patient)

Interventionproportion of participants (Number)
Phase 20.473

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Frequency of DLT

Maximum tolerated dose (MTD) of azacitidine based on DLT was defined as any Grade 4 nonhematologic and noninfectious toxicity or any grade 3 mucositis or skin toxicity lasting > 3 days at peak severity. For dose finding, the continunal reassessment method was used with a target DLT probability per cohort of 25%. Azacitidine doses were chosen adaptively for sucessive cohorts with a minimum size of 2 patients. Toxicity scoring followed the National Cancer Institute Common Toxicity Criteria, version 3. (NCT01983969)
Timeframe: Enrollment up to day 30 post transplant for each dosing cohort

InterventionDose-limiting toxicities (Number)
Azacitidine Dose Level 116
Azacitidine Dose Level 228
Azacitidine Dose Level 340

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Participants With Event-free Survival (EFS)

EFS is defined as the time from transplantation to either relapse, second tumors, or death, whichever occurred first, or last contact. EFS was analzyed by the individual disease groups rather than the cohort dose levels. (NCT01983969)
Timeframe: Enrollment up to 100 days post transplant.

InterventionParticipants (Count of Participants)
DLBCL17
Hodgkin Lymphoma16
T-cell NHL7
Other B-cell Lymphoma5

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Number of Participants With Grade 3 or Greater Non-hematologic Toxicities

Compare toxicity profiles for grade 3 or greater toxicities associated with each of 131I-MIBG treatment regimens; single-agent 131I-MIBG; Vincristine/Irinotecan/131I-MIBG; or Vorinostat/131I-MIBG (NCT02035137)
Timeframe: All toxicities from enrollment through 30 days following end of protocol therapy, an average of 6 months

InterventionParticipants (Count of Participants)
Single-Agent 131I-MIBG7
131I-MIBG With Vincristine/Irinotecan17
131I-MIBG With Vorinostat12

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Objective Tumor Response After One Course of Therapy

To identify the MIBG treatment regimen associated with the highest overall response rate after one course of treatment on the three arms. The response evaluation was based on central review (intent to treat analysis). Responders defined as meeting CR/MRD/PR criteria. Response was based on NANT response criteria v1.2 (https://doi.org/10.1002/pbc.26940). RECST 1.1 criteria was used for measurable tumors with PR criteria > 30% decrease in target tumor size. Curie score was used with PR criteria > 50% decrease in Curie score. Complete Response- disappearance of all target lesions, Curie score of 0 and no detectable bone marrow disease. Overall Response (OR)=CR+PR. (NCT02035137)
Timeframe: 43-50 days from study day 1

InterventionParticipants (Count of Participants)
Single-Agent 131I-MIBG5
131I-MIBG With Vincristine/Irinotecan5
131I-MIBG With Vorinostat11

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Biochemical Efficacy as Measured by Serum LGALS3

Serum concentration of LGALS3 (galectin-3). Galectin-3 is a carbohydrate-binding lectin whose expression is associated with inflammatory cells including macrophages, neutrophils, and mast cells. LGALS3 normal range = 1.4-5.3 ng/ml. (NCT02124083)
Timeframe: 6 months

Interventionng/mL (Mean)
Vorinostat6.565

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Biochemical Efficacy as Measured by Serum Cathepsin D

Serum concentration of Cathepsin D. Cathepsin D is an aspartyl protease involved in protein catabolism and tissue remodeling. Cathepsin D normal range = 220-515 ng/ml. (NCT02124083)
Timeframe: Baseline

Interventionng/mL (Mean)
Vorinostat648.2

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Biochemical Efficacy as Measured by Serum Cathepsin D

Serum concentration of Cathepsin D. Cathepsin D is an aspartyl protease involved in protein catabolism and tissue remodeling. Cathepsin D normal range = 220-515 ng/ml. (NCT02124083)
Timeframe: 6 months

Interventionng/mL (Mean)
Vorinostat625.3

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Biochemical Efficacy as Measured by Serum LGALS3

Serum concentration of LGALS3 (galectin-3). Galectin-3 is a carbohydrate-binding lectin whose expression is associated with inflammatory cells including macrophages, neutrophils, and mast cells. LGALS3 normal range = 1.4-5.3 ng/ml. (NCT02124083)
Timeframe: Baseline

Interventionng/mL (Mean)
Vorinostat6.667

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Number of Participants With Tolerabilty of 200 mg Vorinostat in Niemann-Pick Disease, Type C1

The number of Niemann-Pick Disease, type C1 patients completing 3 month 200 mg phase (NCT02124083)
Timeframe: 3 months

InterventionParticipants (Number)
Vorinostat12

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Number of Participants With Tolerabilty of 400 mg Vorinostat in Niemann-Pick Disease, Type C1

The number of Niemann-Pick Disease, type C1 patients completing 3 month 400 mg phase (NCT02124083)
Timeframe: 3 months

InterventionParticipants (Number)
Vorinostat11

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Viral Inhibition

"CD8+ T cell antiviral suppressive activity was expressed as percentage elimination and determined as follows: [(fraction of p24+ cells in CD4+ T cells cultured alone) - (fraction of p24 + in CD4+ T cells cultured with CD8+ cells)]/(fraction of p24+ cells in CD4+ T cells cultured alone) × 100.~Viral inhibition Assay" (NCT02336074)
Timeframe: 12 weeks

InterventionPercentage elimination (Mean)
Control (Arm A - ART Only)-18.25
Intervention (Arm B - ART + Vaccines + Vorinostat)1.50

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CD8+ T-cell Responses

Percentage of CD8+ CD107a+ IFNγ+ T cells , assessed using an optimized and qualified flow cytometry panel. (NCT02336074)
Timeframe: 12 weeks

,
Intervention% cells CD8+ CD107a+ IFNγ+ (Median)
Post randomisation week 9Post randomisation week 12
Control (Arm A - ART Only)0.0520.062
Intervention (Arm B - ART + Vaccines + Vorinostat)0.1940.263

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Percentage of CD4+ CD154+ IFNγ+ T Cells

Percentage of CD4+ CD154+ IFNγ+ T cells , assessed using an optimized and qualified flow cytometry panel. (NCT02336074)
Timeframe: 12 weeks

,
Intervention% cells CD4+ CD154+ IFNγ+ (Median)
Post randomisation week 9Post randomisation week 12
Control (Arm A - ART Only)0.0060.006
Intervention (Arm B - ART + Vaccines + Vorinostat)0.0970.109

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Total HIV DNA From CD4 T-cells

The average of two measures taken at post-randomisation week 16 and 18 (NCT02336074)
Timeframe: Averaged across post-randomisation week 16 and 18

InterventionHIV-DNA copies/mill CD4+ T cells (log10) (Mean)
Control (Arm A - ART Only)2.95
Intervention (Arm B - ART + Vaccines + Vorinostat)3.06

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Quantitative Viral Outgrowth

Number of Participants with undetectable quantitative viral outgrowth (NCT02336074)
Timeframe: At week 16

InterventionParticipants with undetectable outgrowth (Number)
Control (Arm A - ART Only)12
Intervention (Arm B - ART + Vaccines + Vorinostat)6

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Histone H4 Acetylation

Histone H4 acetylation using a H4K5/8/12/16 immunoassay with thawed PBMC derived cell lysates added to an ELISA using anti-H4 monoclonal antibody (NCT02336074)
Timeframe: 12 weeks

InterventionFold increase pre to post vorinostat (Mean)
Intervention (Arm B - ART + Vaccines + Vorinostat)3.19

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Duration of Response

The duration of overall response is measured from the time measurement criteria are met for CR or PR (whichever is first recorded) until the first date that recurrent or progressive disease is objectively documented (taking as reference for progressive disease the smallest measurements recorded since the treatment started). (NCT02395627)
Timeframe: Up to 24 months

Interventionmonths (Median)
Pembrolizumab Group A17.0
Pembrolizumab Group B8.8

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Objective Response Rate (ORR)

Objective response rate (ORR) will be defined as the proportion of participants whose status is stable disease (SD) or better (complete response (CR), partial response (PR)) at 24 weeks' follow-up as measured by Response Evaluation Criteria in Solid Tumors (RECIST). The best overall response is the best response recorded from the start of the treatment until disease progression/recurrence (taking as reference for progressive disease the smallest measurements recorded since the treatment started). The patient's best response assignment will depend on the achievement of both measurement and confirmation criteria. (NCT02395627)
Timeframe: Up to 24 weeks

Interventionpercentage of participants (Number)
Pembrolizumab Group A6.67
Pembrolizumab: Group B0

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Overall Survival (OS)

OS is defined as the length of time from the start of treatment for participants until death or the study has ended, whichever comes first. (NCT02395627)
Timeframe: Up to 36 months

Interventionmonths (Median)
Pembrolizumab Group A14.3
Pembrolizumab Group B15.0
Pembrolizumab Group C7.8

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Progression Free Survival

Progression-free survival (PFS) is defined as the length of time during and after the treatment that the participant has achieved an objective response, but does not progress as measured by RECIST v.1.1 (NCT02395627)
Timeframe: Up to 36 months

Interventionmonths (Median)
Pembrolizumab Group A2.57
Pembrolizumab Group B2.63

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Progression Free Survival

The Kaplan Meier methods will be used to estimate progression free survival. (NCT02538510)
Timeframe: Up to 2 years

InterventionMonths (Mean)
Head and Neck Squamous Cell Carcinoma12.6
Salivary Gland Carcinoma14.0

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Incidence of Toxicity Graded According to the National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.0

Toxicities will be summarized as the number and percentage of patients with each type of toxicity, per Criteria for Adverse Events version 4.0 (NCT02538510)
Timeframe: Up to 30 days after the completion of study treatment

,
InterventionParticipants (Count of Participants)
Adrenal insufficiencyALT increaseAnorexiaArthiritisAST increaseCoughIncreased CreatinineDermatitisDiarrheaFever with leukocytosisFatigueHyponatremiaHypothyroidismColitis and IleitisMalaiseNauseaNephritisPneumonitisNeuritisTracheitis/EpiglottitisVomiting
Head and Neck Squamous Cell Carcinoma100001210022111101011
Salivary Gland Carcinoma111110501140000310102

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Objective Response Rate

Radiologic assessments of measurable disease will be performed using radiographic imaging. RECIST 1.1 and immune response criteria will be used to assess response to therapy. Responses will be summarized as frequencies and percentages. (NCT02538510)
Timeframe: Up to 2 years

,
InterventionParticipants (Count of Participants)
partial responsestable diseaseprogressive disease
Head and Neck Squamous Cell885
Salivary Gland Carcinoma4136

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Total Number of Adverse Events

Collect and grade all of the adverse events to evaluate for safety. This data was collected for the first 2 cycles for each participant. (NCT03050450)
Timeframe: Two 28 day cycles

Interventiontotal adverse events (Number)
Grade 1 adverse eventsGrace 2 adverse eventsGrade 3 adverse eventsGrade 4 adverse eventsGrade 5 adverse events
Dose Level 168321221

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Number Participants With Hematologic and Non-hematologic Toxicities

Number participants with grades 3 to 5 hematologic and non-hematologic toxicities. All toxicities are for end of cycle 2. (NCT03050450)
Timeframe: Two 28 day cycles

InterventionParticipants (Count of Participants)
Grade 3 & 4 Blood/Bone MarrowGrade 3 & 4 GastrointestinalGrade 3 & 4 Metabolic/LaboratoryGrade 3 & 4 Musculoskelatal/Soft TissueGrade 3 & 4 NeurologyGrade 3 & 4 PainGrade 3 & 4 VascularGrade 3 & 4 & 5 Other
Dose Level 102511006

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Best Response of Children With Recurrent or Refractory Central Nervous System Tumors

Best response by MRIs per definitions in the protocol (complete response, partial response, stable disease, progressive disease). MRI's were obtained every 2 cycles and the best response was reported. (NCT03050450)
Timeframe: Every 2 cycles up to 24 cycles

InterventionParticipants (Count of Participants)
Complete ResponsePartial ResponseStable DiseaseProgressive Disease
Dose Level 10112

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Number of Participants Demonstrating an HIV-specific Immune Response to the Combination of Vorinostat (VOR) and HIV-specific T Cells (HXTC) Therapy as Well as a Change in the Frequency of Latent HIV Infection

The change in ex vivo HIV-specific immune response from baseline was measured by interferon-gamma (IFN-γ) ELISpot throughout the study. Change in the frequency of latent HIV infection from baseline to end of study was measured using a quantitative viral outgrowth assay (QVOA). Participants that exhibited any significant changes in both of these measures were considered to have experienced a positive result. (NCT03212989)
Timeframe: Up to end of study (weeks 16 through 45)

InterventionParticipants (Count of Participants)
VOR + HXTC Arm0

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Number of Participants With HIV-1 RNA Levels (Measured by Single Copy Assay) Greater or Equal to the Lower Limit of Quantification

Number of participants with HIV-1 RNA levels measured by single copy assay (SCA) greater or equal to the lower limit of quantification (LOQ). The lower limit of quantification for this study was 0.47 copies/mL. (NCT03382834)
Timeframe: Pre-entry, entry, Day 28, Day 35, Day 38 (5 hours post vorinostat), Day 45, Day 65

,
InterventionParticipants (Count of Participants)
Pre-entry SCA >= LOQEntry SCA >=LOQDay 28 SCA >=LOQDay 35 SCA >=LOQDay 38 SCA >=LOQDay 45 SCA >=LOQDay 65 SCA >=LOQ
Arm A: Tamoxifen + Vorinostat10911117910
Arm B: Vorinostat Alone6345545

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Proportion of Participants With New Grade 3 or Greater Adverse Events

Proportion of participants with new Grade 3 or greater adverse events that are considered definitely, probably, or possibly related to study treatment (as judged by the core protocol team). The DAIDS AE Grading Table (corrected Version 2.1, July 2017) was used. (NCT03382834)
Timeframe: Measured from study entry through Day 65

Interventionproportion of participants (Number)
Arm A: Tamoxifen + Vorinostat0
Arm B: Vorinostat Alone0

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Change From Baseline in Total HIV-1 DNA Levels in CD4+ T Cells

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value of Total HIV-1 DNA on Day 38 (5 hours post vorinostat) minus the value at baseline. (NCT03382834)
Timeframe: Pre-entry, entry, and Day 38

Interventionlog10 copies/million CD4 cells (Mean)
Arm A: Tamoxifen + Vorinostat0
Arm B: Vorinostat Alone-0.04

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Change From Baseline in Cell-associated HIV-1 RNA in CD4+ T Cells

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value of Cell-associated HIV-1 RNA on Day 38 (5 hours post vorinostat) minus the value at baseline. (NCT03382834)
Timeframe: Pre-entry, entry, and Day 38

Interventionlog10 copies/million CD4 cells (Mean)
Arm A: Tamoxifen + Vorinostat0.06
Arm B: Vorinostat Alone0.17

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Complete Response Rate

Percentage of subjects with a complete response in the skin based on mSWAT (NCT03713320)
Timeframe: Date of first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionPercentage of participants (Number)
Cobomarsen (Randomized)0
Vorinostat (Randomized)5.6

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Duration of Response in Skin

Duration of response in skin (no progression after achieving ≥ 50% improvement in mSWAT) (NCT03713320)
Timeframe: Monthly from first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionMonths (Median)
Cobomarsen (Randomized)NA
Vorinostat (Randomized)7.85

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Objective Response Rate in the Skin of at Least 28-days Duration (ORR1)

Percentage of participants achieving ≥ 50% improvement in mSWAT of at least 28-days duration (NCT03713320)
Timeframe: Monthly from first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

Interventionpercentage of participants (Number)
Cobomarsen (Randomized)31.6
Vorinostat (Randomized)33.3

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Percentage of Subjects Achieving ≥ 50% Improvement in mSWAT at 28 Days

Percentage of subjects achieving ≥ 50% improvement from baseline in mSWAT at 28 days after first dose (NCT03713320)
Timeframe: 28 days after first dose

Interventionpercentage of participants (Number)
Cobomarsen (Randomized)5.3
Vorinostat (Randomized)11.1

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Percentage of Subjects Achieving ≥ 50% Improvement in mSWAT at 4 Months

Percentage of subjects achieving ≥ 50% improvement from baseline in mSWAT at 4 months after first dose (NCT03713320)
Timeframe: 4 months after first dose

Interventionpercentage of participants (Number)
Cobomarsen (Randomized)21.1
Vorinostat (Randomized)22.2

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Progression-free Survival (PFS)

Time from date of randomization until the date of earliest documented progression or death from any cause. The duration of PFS was censored at the date of the last mSWAT assessment if the subject was alive and had no documented progression. Disease progression in the skin is defined as ≥ 25% increase in mSWAT score from baseline or, in participants with complete or partial response, increase in mSWAT score of greater than the sum of the nadir plus 50% baseline score. (NCT03713320)
Timeframe: Date of first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

Interventionmonths (Median)
Cobomarsen (Randomized)NA
Vorinostat (Randomized)6.01

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Pruritus Medication Utilization

Change from baseline in number of pruritus medications taken per subject (NCT03713320)
Timeframe: Date of first dose through end of treatment or interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionNumber of pruritus medications (Mean)
Cobomarsen (Randomized)-1
Vorinostat (Randomized)-0.9

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Time to ≥ 50% Improvement in mSWAT

Time from date of randomization until ≥ 50% improvement in mSWAT score (NCT03713320)
Timeframe: Monthly from first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionMonths (Mean)
Cobomarsen (Randomized)3.7
Vorinostat (Randomized)2.7

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Time to Maximal Effect in mSWAT

Time to greatest improvement in mSWAT score (NCT03713320)
Timeframe: Monthly from first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionMonths (Mean)
Cobomarsen (Randomized)4.5
Vorinostat (Randomized)3.0

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Peak Plasma Concentration (Cmax) of Cobomarsen - First Dose

Peak plasma concentration (Cmax) of cobomarsen after first dose (NCT03713320)
Timeframe: 1, 1.92, 6, 24 and 48 hours post-dose after the first dose

Interventionµg/mL (Mean)
Cobomarsen (Randomized)10.5

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Peak Plasma Concentration (Cmax) of Cobomarsen - Week 5

Peak plasma concentration (Cmax) of cobomarsen after fourth dose (Week 5) (NCT03713320)
Timeframe: 1, 1.92 and 6 hours post-dose after the Week 5 dose

Interventionµg/mL (Mean)
Cobomarsen (Randomized)9.34

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Percentage of Subjects Achieving an Objective Skin Response of at Least 4 Months Duration (ORR4)

ORR4 is the percentage of subjects with a complete response (CR) or partial response (PR) in the skin for 4 consecutive months confirmed by repeat assessments no less than 28 days (± 3 days) later. The modified Severity Weighted Assessment Tool (mSWAT) is used to measure skin disease severity based on the percentage of body surface area (BSA) with patches, plaques, or tumors. Total scores are calculated by multiplying the BSA percentage for each category of lesion (patch, plaque, or tumor) by a weighting factor and adding the three sub-scores. Lower scores indicate a lower degree of skin disease severity. CR corresponds to 100% clearance of skin lesions present at baseline (mSWAT score of 0). PR corresponds to 50-99% clearance of skin disease present at baseline (at least 50% reduction in mSWAT score), without new tumors. (NCT03713320)
Timeframe: Date of first dose through the earlier of last study visit or interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionPercentage of participants (Number)
Cobomarsen (Randomized)15.8
Vorinostat (Randomized)16.7

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Area Under the Plasma Concentration vs. Time Curve (AUC) of Cobomarsen - Week 5

Area under the curve (AUClast) for cobomarsen plasma concentration versus time curve after the fourth (Week 5) dose (NCT03713320)
Timeframe: 1, 1.92 and 6 hours post-dose after the Week 5 dose

Interventionµg*hr/mL (Mean)
Cobomarsen (Randomized)25.5

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Time to Progression

Time from date of randomization until the earliest date of confirmed progression (NCT03713320)
Timeframe: Date of first dose through interim analysis data cut-off date of 12-Oct-2020, up to 16 months

InterventionMonths (Mean)
Cobomarsen (Randomized)NA
Vorinostat (Randomized)6.01

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Percentage of Participants With Tumor Responses

Tumor responses will be classified using the Immune Related Response-Criteria (irRC)) through study completion. (NCT04190056)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Arm B (Pembrolizumab, Tamoxifen)0

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Duration of Response (DOR)

The duration of overall response is measured from the time measurement criteria are met for CR or PR (whichever is first recorded) until the first date that recurrent or progressive disease is objectively documented (taking as reference for progressive disease the smallest measurements recorded since the treatment started). The duration of overall CR is measured from the time measurement criteria are first met for CR until the first date that recurrent disease is objectively documented. Duration of stable disease is measured from the start of the treatment until the criteria for progression are met, taking as reference the smallest measurements recorded since the treatment started. Will use median DOR (computed by the Kaplan-Meier estimator) to summarize. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 24 weeks

Interventionweeks (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

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Median Overall Survival (OS)

Will use median OS (computed by the Kaplan-Meier estimator) to summarize from initiation of study treatment to the time of death from any cause on study. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 27 months

Interventionmonths (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

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Median Progression Free Survival (PFS)

Progression-free survival (PFS) is defined as the duration of time from start of treatment to time of progression or death from any cause on study, whichever occurs first. Will use median PFS (computed by the Kaplan-Meier estimator) to summarize. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 27 months

Interventionmonths (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

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Overall Response Rate (ORR)

ORR is defined as the proportion of participants randomized to that arm whose status is stable disease (SD) or better (complete response (CR), partial response (PR)). Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions: CR=Disappearance of all target lesions; PR = >=30% decrease in the sum of the longest diameter of target lesions, and SD=Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease,. (NCT04190056)
Timeframe: Up to 24 weeks

Interventionproportion of participants (Number)
Arm B (Pembrolizumab, Tamoxifen)0

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