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]
ID Source | ID |
---|---|
PubMed CID | 5311 |
CHEMBL ID | 98 |
CHEBI ID | 45716 |
SCHEMBL ID | 9018 |
MeSH ID | M0288128 |
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 |
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.
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
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.
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.
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.
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.
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.
Role | Description |
---|---|
EC 3.5.1.98 (histone deacetylase) inhibitor | An 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 inducer | Any substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms. |
antineoplastic agent | A 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] |
Class | Description |
---|---|
hydroxamic acid | A 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Nrf2 | Homo sapiens (human) | Potency | 3.3889 | 0.0920 | 8.2222 | 23.1093 | AID624171; AID651593 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 1.2909 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
PPM1D protein | Homo sapiens (human) | Potency | 1.4740 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
TDP1 protein | Homo sapiens (human) | Potency | 0.5087 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.1239 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 2.0669 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743040; AID743042; AID743053; AID743054; AID743063 |
Smad3 | Homo sapiens (human) | Potency | 3.1623 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 4.2163 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 5.6278 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 3.6190 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 0.9439 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 2.6525 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.9003 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 1.0576 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 1.0951 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 2.1130 | 0.3758 | 27.4851 | 61.6524 | AID743217 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 7.4978 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 4.7548 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079; AID743080; AID743091 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.8975 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
caspase-3 | Homo sapiens (human) | Potency | 4.2163 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 6.7267 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 14.9601 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 14.9601 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 2.3177 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 0.3261 | 0.0376 | 17.0823 | 61.1927 | AID1259364; AID1259388 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 5.2134 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 0.8913 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 0.0631 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
plasminogen precursor | Mus musculus (house mouse) | Potency | 0.0631 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 0.0631 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
geminin | Homo sapiens (human) | Potency | 6.5213 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 1.6276 | 0.0056 | 12.3677 | 36.1254 | AID624032; AID624044 |
DNA dC->dU-editing enzyme APOBEC-3F isoform a | Homo sapiens (human) | Potency | 7.0795 | 0.0259 | 11.2398 | 31.6228 | AID602313 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 3.3491 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 2.1534 | 0.0033 | 9.1582 | 39.8107 | AID1347407; AID1347411 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.7542 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 3.3491 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 1.9938 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 1.8959 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
PAX8 | Homo sapiens (human) | AC50 | 4.5800 | 0.0488 | 5.4354 | 69.1700 | AID687027 |
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7 | Homo sapiens (human) | AC50 | 0.9330 | 0.0398 | 15.0025 | 50.0000 | AID743267 |
Histone deacetylase 3 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 3 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 3 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Cytochrome P450 3A4 | Homo sapiens (human) | INH | 24.8000 | 1.7000 | 2.8500 | 4.0000 | AID663472 |
Histone deacetylase 4 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 4 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 4 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 1 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 1 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 1 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 7 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 7 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 7 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 2 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 2 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 2 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Polyamine deacetylase HDAC10 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Polyamine deacetylase HDAC10 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Polyamine deacetylase HDAC10 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 11 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 11 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 11 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 8 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 8 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 8 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 6 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 6 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 6 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 9 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 9 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 9 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
Histone deacetylase 5 | Homo sapiens (human) | AC50 | 3.1000 | 0.0100 | 2.7020 | 7.9000 | AID90344 |
Histone deacetylase 5 | Homo sapiens (human) | INH | 0.1885 | 0.0244 | 0.2434 | 0.5720 | AID1622899; AID603218 |
Histone deacetylase 5 | Homo sapiens (human) | Inhibition | 0.0800 | 0.0035 | 0.0417 | 0.0800 | AID243634 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2005 | Journal of molecular biology, Nov-18, Volume: 354, Issue:1 | Crystal structure of a bacterial class 2 histone deacetylase homologue. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2005 | Journal of molecular biology, Nov-18, Volume: 354, Issue:1 | Crystal structure of a bacterial class 2 histone deacetylase homologue. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1401372 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1702152 | Metabolic 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 analysis | 2018 | Journal 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. |
AID652754 | Inhibition of recombinant human HDAC10 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID723461 | Inhibition of human HDAC8 by fluorescence assay | 2013 | Journal 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. |
AID1482122 | Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1478598 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1622905 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1819530 | Antitumor 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 days | 2022 | Journal 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. |
AID1225984 | Inhibition 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 assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1312847 | Inhibition 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 a | 2016 | Journal 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. |
AID1630606 | Inhibition 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 assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID723431 | Potentiation 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 assay | 2013 | Journal 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. |
AID1200977 | Inhibition 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-275 | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1861334 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1164174 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1832683 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1664987 | Cytotoxicity against human 2C4 cells assessed as reduction in cell viability at 2000 nM incubated for 20 hrs | 2020 | ACS 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. |
AID760375 | Cytotoxicity against human BxPC3 cells after 72 hrs by MTS assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1548728 | Inhibition 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 fo | 2020 | Journal 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. |
AID1164182 | Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate at 5 uM after 1 hr by fluorescent activity assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1861253 | Antiproliferative activity against human ES2 cells assessed as reduction in cell viability measured after 7 days | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID476646 | Antiproliferative activity against human K562 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1859930 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID732144 | Inhibition of HDAC5 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1753840 | Inhibition of HDAC8 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1915584 | Inhibition of HDAC1 (unknown origin) at 0.1 microM relative to control | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID462789 | Inhibition of HDAC8 expressed in Escherichia coli assessed as Boc-Lys (acetyl)-AMC substrate hydrolysis by fluorimetric assay | 2010 | Bioorganic & 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. |
AID1861311 | Induction of apoptosis in human OCILY3 cells measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1449334 | Inhibition of HDAC1 in human CAL27 cells assessed as accumulation of histone 3 acetylation at 1 uM after 24 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1514611 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID1671980 | Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay | 2019 | Bioorganic & 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. |
AID1128544 | Inhibition of human HDAC-1 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID749703 | Inhibition of HDAC6 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1141816 | Oral bioavailability in ICR mouse at 10 mg/kg by LC-MS/MS analysis | 2014 | Journal 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. |
AID723421 | Potentiation 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 assay | 2013 | Journal 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. |
AID1849168 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1816188 | Inhibition of recombinant HDAC8 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | |||
AID1231812 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1614192 | Induction 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%) | |||
AID1469378 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID297488 | Cytotoxicity against human HCT116 cells | 2007 | Journal 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. |
AID1578905 | Induction of apoptosis in human Bel7402 cells assessed as increase in cleaved PARP level at 5 uM after 72 hrs by Western blot analysis | 2019 | Journal 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. |
AID1639366 | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1486302 | Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1578524 | Oral bioavailability in Balb/c nude mouse at 50 mg/kg measured upto 24 hrs by LC/MS/MS analysis | 2020 | ACS 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. |
AID1441706 | Anti-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 7 | 2017 | Journal 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. |
AID1170742 | Inhibition of human recombinant HDAC3 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1321731 | Inhibition 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 control | 2016 | Journal 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. |
AID1548287 | Induction 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%) | |||
AID1622907 | Inhibition of HDAC in human HeLa nuclear extract using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1730868 | Cytotoxicity against human FHC cells assessed as reduction of cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID748110 | Inhibition of HDAC5 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1855269 | Antitumor 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 days | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1469383 | Induction 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%) | 2018 | Journal 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 |
AID1605980 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1876341 | Inhibition of recombinant full length human HDAC3 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID586611 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID1547245 | Inhibition of GST-tagged BRD4 bromodomain (unknown origin) using biotinylated histone H4KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1441704 | Anti-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 eos | 2017 | Journal 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. |
AID1129789 | Induction 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1466400 | Antitumor 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 days | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. |
AID1441636 | Inhibition 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 analysis | 2017 | Journal 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. |
AID1436791 | Growth 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity. |
AID1547262 | Inhibition of human recombinant His-tagged BRD2 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1887683 | Cytotoxicity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID544091 | Antimalarial activity against drug-resistant Plasmodium falciparum W2 | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1206737 | Cytotoxicity against human HEL cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1478586 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID374818 | Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells | 2009 | Journal 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. |
AID1063056 | Inhibition of recombinant HDAC1 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1141763 | Cytotoxicity against human H460 cells by MTT assay | 2014 | Journal 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. |
AID1655804 | Cytotoxicity 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 control | 2020 | ACS 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. |
AID1762489 | Inhibition 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 f | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1550094 | Inhibition 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 assay | 2019 | Journal 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. |
AID1899586 | Inhibition of HDAC class 2b in human HT-29 cells using Boc-Lys-Ac as substrate incubated for 3 hrs by microplate reader assay | |||
AID748111 | Inhibition of HDAC4 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID760378 | Cytotoxicity against human HUT78 cells after 72 hrs by MTS assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1449317 | Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1282233 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 2016 | Journal 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. |
AID247931 | Concentration required to inhibit human PC-3 prostate carcinoma cells | 2005 | Journal 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. |
AID463865 | Inhibition of human HDAC in human HeLa cell nuclear extract after 15 mins by colorimetric assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors. |
AID1865305 | Antitumor 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 control | 2022 | Journal 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. |
AID1739585 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1365025 | Selectivity 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 cells | 2017 | Bioorganic & 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. |
AID1473740 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID1174700 | Induction 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%) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1762497 | Inhibition of HDAC3 (unknown origin) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1707465 | Synergistic antifungal activity against Candida albicans 0304103 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID1348917 | Inhibition 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 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1826592 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID623021 | Inhibition 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 assay | 2011 | European 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. |
AID1055717 | Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1273878 | Inhibition 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 analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1754767 | Downregulation of HDAC11 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1201642 | Inhibition of HDAC (unknown origin) using Fluor de Lys substrate after 2 hrs by microplate reader | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1239052 | Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID156319 | Inhibitory activity against PC-3 cell line | 2004 | Bioorganic & 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. |
AID476653 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID461258 | Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID717659 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1511152 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1550151 | Antitumor 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 caliper | 2019 | Journal 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. |
AID1355710 | Antifungal activity against FLC resistant Candida albicans 100 after 48 hrs in presence of fluconazol by checkerboard microdilution method | 2018 | Journal 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. |
AID1415639 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1742177 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID723146 | Potentiation 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 assay | 2013 | Journal 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. |
AID1177045 | Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1548250 | Inhibition 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 | |||
AID1742653 | Cytotoxicity against human SUM159PT cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID408888 | Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1177042 | Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1563940 | Inhibition of recombinant HDAC1 (unknown origin) measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. |
AID1737142 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID618023 | Antitumor 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 days | 2011 | Journal 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. |
AID1403154 | Inhibition of HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1633989 | Inhibition 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 analysis | 2019 | Bioorganic & 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). |
AID1203895 | Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1848630 | Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID414731 | Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal 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. |
AID1269327 | Cytotoxicity against human MCF7 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID382342 | Inhibition of human HDAC in HeLa cells by flour de lys assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group. |
AID663390 | Growth inhibition of human RXF393 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID80353 | Concentration required to inhibit the partially purified HDAC enzyme by 50% obtained from H1299 cell lysate | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4 | Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID729522 | Inhibition 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 analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN). |
AID1390015 | Selectivity 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 cells | 2018 | Bioorganic & 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. |
AID1808554 | Inhibition 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 assay | 2021 | Journal 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). |
AID1597931 | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1702059 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay | 2018 | Journal 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. |
AID1739596 | Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 1 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID480069 | Cytotoxicity against human HCT116 cells after 71 hrs by MTS assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. |
AID1433304 | Induction 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 control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID711159 | Inhibition of HDAC1 by fluorometric assay | 2012 | Journal 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. |
AID1415641 | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1127327 | Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1203893 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1404297 | Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1487005 | Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC2 (unknown origin) | 2017 | Bioorganic & 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. |
AID1605976 | Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1469325 | Induction 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%) | 2018 | Journal 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 |
AID274035 | Microsome stability: percent compound remaining | 2007 | Bioorganic & 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. |
AID1260652 | Cytotoxicity against human MV411 cells | |||
AID420640 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 24 hrs by Western blot | 2009 | European 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. |
AID1547263 | Inhibition of HDAC11 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1578477 | Inhibition 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 assay | 2020 | ACS 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. |
AID1274873 | Inhibition of HDAC3 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1275636 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1861264 | Selectivity index, ratio of IC50 for inhibition of HDAC3 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1293556 | Antiproliferative activity against human IGROV1 cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1690835 | Inhibition 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 aft | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID274033 | Inhibition of MDA-MB-231 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID670972 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1888417 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID1848558 | Inhibition of HDAC in human NCI-H522 cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1469323 | Induction 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%) | 2018 | Journal 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 |
AID456795 | Inhibition of HDAC in human HeLa cell nuclear extracts after 15 mins by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID297487 | Cytotoxicity against human HCT15 cells | 2007 | Journal 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. |
AID717791 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID243474 | Percentage inhibition against histone deacetylase of HeLa cells at 100 uM | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design. |
AID1548301 | Induction 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%) | |||
AID308049 | Inhibition of human HDAC 1 | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors. |
AID438220 | Selectivity ratio of IC50 for HDAC6 to IC50 for HDAC1/2 from human HeLa cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide. |
AID659643 | Inhibition of HDAC in human DU145 cells assessed as histone H3 hyperacetylation at 2.5 to 5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID744378 | Inhibition 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 analysis | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN). |
AID723434 | Potentiation 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 assay | 2013 | Journal 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. |
AID1170741 | Inhibition of human recombinant HDAC2 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID737907 | Selectivity index, ratio of IC50 for human HS68 cells to IC50 for human A549 cells | 2013 | Journal 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. |
AID1164189 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1348918 | Inhibition 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 fluores | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID541646 | Inhibition of human HDAC3 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1182315 | Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID616000 | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1547270 | Inhibition of HDAC1 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1821268 | Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID90342 | In vitro inhibitory activity against histone deacetylase (HDAC) isolated from HeLa nuclear extract | 2003 | Bioorganic & 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. |
AID1698864 | Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID1907400 | Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Dual-acting antitumor agents targeting the A |
AID408884 | Inhibition of HDAC10 | 2008 | Journal 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. |
AID1550326 | Synergistic antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs in presence of ruxolitinib by MTT assay | 2019 | Journal 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. |
AID613293 | Plasma concentration in human at 800 mg/kg, po administered as single dose | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1633995 | Therapeutic 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 i | 2019 | Bioorganic & 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). |
AID1321738 | Inhibition 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 control | 2016 | Journal 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. |
AID1246509 | Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1873387 | Inhibition of HDAC7 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1234889 | Inhibition 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 analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID527044 | Cytotoxicity against human NCI-H23 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID723448 | Potentiation 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 assay | 2013 | Journal 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. |
AID1550327 | Synergistic antiproliferative activity against human K562 cells assessed as combination index after 48 hrs in presence of ruxolitinib by MTT assay | 2019 | Journal 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. |
AID1873419 | Inhibition of HDAC3 (unknown origin) at 5 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1677508 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1572343 | Selectivity ratio of IC50 for recombinant C-terminal His/FLAG-tagged human HDAC1 to IC50 for N-terminal GST-tagged human HDAC6 | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID591327 | Inhibition of HDAC in human HeLa cells at 1 uM by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors. |
AID1406984 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1667068 | Inhibition 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 assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1886187 | Inhibition of HDAC8 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay | 2022 | Journal 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. |
AID288446 | Inhibition of HDAC in HeLa cells by fluorescent activity assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID420326 | Inhibition of HDAC from human HeLa cells by fluorogenic enzyme assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1487040 | Inhibition 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 addition | 2017 | Bioorganic & 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. |
AID446347 | Oral bioavailability in CD1 mouse at 15 mg/kg | 2010 | Journal 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. |
AID527038 | Cytotoxicity against human A549 cells by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1873389 | Inhibition of HDAC9 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1875510 | Selectivity index, ratio of IC50 for cytotoxicity against HMEC cells to GI50 for antiproliferative activity against human MDA-MB-231 cells | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID1203892 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID481559 | Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1821346 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1348912 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1486999 | Inhibition of HDAC1 (unknown origin) by ELISA-based assay | 2017 | Bioorganic & 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. |
AID496805 | Inhibition of human HDAC5 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1917530 | Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID1441663 | Anti-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 method | 2017 | Journal 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. |
AID659494 | Inhibition of HDAC6 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1890313 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1783069 | Antifungal activity against fluconazole-sensitive Candida albicans 10061 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID81711 | Concentration required to inhibit the HCT116 cell growth by 50%. | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4 | Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1676599 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1655898 | Inhibition 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) | 2020 | ACS 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. |
AID1061950 | Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID322418 | Cell cycle arrest in human LNCap cells assessed as accumulation at S phase relative to control at 1 uM | 2008 | Bioorganic & 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. |
AID1280270 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID348805 | Antiproliferative activity against human A549 cells after 72 hrs by celltiter-blue viability assay | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID352523 | Antiproliferative activity against human MIAPaCa2 cells by MTT assay | 2009 | Bioorganic & 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. |
AID1896934 | Cytotoxicity against human L02 cells assessed as reduction in cell viability by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-05, Volume: 75 | Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells. |
AID489913 | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13 | Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity. |
AID1753836 | Selectivity index, ratio of IC50 for inhibition of recombinant human HDAC1 to IC50 for inhibition of recombinant human HDAC6 | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1433271 | Inhibition of HDAC6 in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID353357 | Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G2/M phase at 3 uM after 16 hrs by flow cytometry | 2009 | Journal 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. |
AID463864 | Inhibition of human HDAC in human HeLa cell nuclear extract at 50 nM after 15 mins by colorimetric assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors. |
AID297499 | Cytotoxicity against human CCRF-CEM cells | 2007 | Journal 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. |
AID1312883 | Antitumor 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 control | 2016 | Journal 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. |
AID1466064 | Inhibition of recombinant human full length HDAC8 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1816225 | Induction 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%) | |||
AID526537 | Growth inhibition of human NCI-H23 cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1361627 | Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID297478 | Cytotoxicity against human NCI H69 cells | 2007 | Journal 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. |
AID1234897 | Antiproliferative activity against human H7402 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1418667 | Inhibition of recombinant human HDAC3 using fluorogenic HDAC substrate after 30 mins by fluorescence analysis | 2018 | Bioorganic & 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. |
AID1863424 | Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1658889 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors. |
AID1690836 | Inhibition 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 | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1127003 | Induction 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%) | 2014 | Journal 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. |
AID1754752 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1622964 | Inhibition of HDAC10 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID524988 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID734734 | Cytotoxicity against human LNCAP cells assessed as growth inhibition by MTS assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1541565 | Inhibition 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 | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID760494 | Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1164029 | Inhibition of human recombinant HDAC5 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1623525 | Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate-3 by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1848582 | Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1126964 | Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC3 (unknown origin) | 2014 | Journal 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. |
AID1469333 | Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID1622965 | Inhibition of HDAC6 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1816205 | Induction 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%) | |||
AID628446 | Induction of apoptosis in human HepG2 cells assessed as hyperacetylation of p53 after 24 hrs by Western blot analysis | 2011 | Journal 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. |
AID1578884 | Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay | 2019 | Journal 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. |
AID1848619 | Cytotoxicity against human COLO 205 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID619048 | Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1702091 | Induction 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 analysis | 2018 | Journal 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. |
AID461259 | Antiproliferative activity against human Capan1 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1361647 | Induction 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%) | 2018 | Journal 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. |
AID1401483 | Selectivity 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 lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1449684 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1550085 | Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | Journal 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. |
AID1653142 | Cytotoxicity against human MGC803 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1164923 | Induction 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 control | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1900937 | Toxicity 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) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID1476157 | Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1742720 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1689777 | Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1855259 | Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1266818 | Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | 2015 | Journal 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. |
AID1659650 | Inhibition of HDAC6 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID616005 | Inhibition of HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1702048 | Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1165114 | Cytotoxicity against human LNCAP cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1410011 | Reactivation of latent HIV1 infected in human U1 cells assessed as increase in p24 production after 48 hrs by ELISA | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor. |
AID1598137 | Activation 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 control | 2019 | Journal 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. |
AID1702066 | Inhibition 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 assay | 2018 | Journal 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. |
AID1422517 | Inhibition of HDAC in MEF assessed as increase in histone H4K8 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1515840 | Inhibition 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 hr | 2019 | Journal 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. |
AID1865252 | Synergistic antiproliferative activity against human MV4-11 cells assessed as combination index measured in presence of SHP099 by Chou-Talalay method | 2022 | Journal 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. |
AID90687 | Inhibitory concentration against maize Histone deacetylase 2 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID1885693 | Antitumor 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-Me | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy. |
AID1421612 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1060991 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors. |
AID1401902 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID723151 | Potentiation 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 assay | 2013 | Journal 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. |
AID1855260 | Antiproliferative activity against human MOLT-4 cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1730850 | Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1759728 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction. |
AID1848279 | Inhibition of HDAC6 (unknown origin) at 100 nM | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID274027 | Clearance after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1127001 | Induction 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%) | 2014 | Journal 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. |
AID1246517 | Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1566817 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1861329 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID775833 | Inhibition 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 control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1639368 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1426429 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID1855255 | Antiproliferative activity against human HeLa cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID274062 | Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) | 2007 | Bioorganic & 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. |
AID1702084 | Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1821339 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID328807 | Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID1401537 | Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID723139 | Potentiation 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 assay | 2013 | Journal 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. |
AID352762 | Toxicity against human HCT116 cells xenografted nude mouse assessed as body weight loss at 150 mg/kg, ip administered once daily for 18 days | 2009 | Bioorganic & 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. |
AID420515 | Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at G2/M phase at IC90 using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID1810050 | Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay | |||
AID1206744 | Cytotoxicity against human KG1 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1541444 | Inhibition 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 9 | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1639369 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID609490 | Antiproliferative activity against human HCT116 cells | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID615998 | Inhibition 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 assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1752944 | Inhibition 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 | |||
AID303348 | Inhibition of HDAC1 in presence of DTT | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. |
AID723474 | Cytotoxicity against cisplatin resistant human KYSE-510 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1266813 | Antiproliferative activity against human SW480 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1915595 | Inhibition of HDAC8 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID331957 | Increase in histone H3 acetylation in human HEK-TE cells at 5 uM after 6 hrs by Western blot analysis | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases. |
AID546548 | Inhibition of human recombinant HDAC6 expressed in HEK293 cells | 2010 | Journal 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. |
AID594124 | Inhibition of full length HDAC2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Discovery of histone deacetylase 8 selective inhibitors. |
AID1462230 | Inhibition of BRD4 (unknown origin) | 2017 | Bioorganic & 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. |
AID1659234 | Inhibition of human HDAC1 after 30 mins by microplate reader analysis | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6. |
AID274076 | Inhibition of PC3 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID591331 | Antiproliferative activity against human HCT116 cells after 5 days by Alamar blue assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors. |
AID1482102 | Inhibition of HDAC 5 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1233265 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay | 2015 | Journal 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. |
AID1260643 | Inhibition of human recombinant HDAC7 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID392406 | Inhibition of HDAC1 in human 293T cells after 16 hrs by fluorimetry | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Sulfamides as novel histone deacetylase inhibitors. |
AID1401341 | Inhibition of HDAC in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1401370 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1246510 | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1326521 | Inhibition of full length recombinant human HDAC6 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1431821 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1915596 | Inhibition of HDAC4 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1622906 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1250649 | Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1061954 | Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1127330 | Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1898917 | Inhibition of HDAC1/2 in human NCI-H460 cells at 7.4 uM assessed as increase in H4 acetylation measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1127320 | Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 72 hrs | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1141785 | Inhibition of HDAC6 in human HCT116 cells assessed as increase in HSP90 acetylation at 0.3 to 1 uM by coimmunoprecipitation analysis | 2014 | Journal 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. |
AID765378 | Inhibition of recombinant human HDAC4 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins | 2013 | Journal 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. |
AID1177051 | Antiprotozoan activity against Trypanosoma cruzi Tulahuen C4 amastigotes | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1861663 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1623526 | Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1482128 | Cytotoxicity against human FR2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1482133 | Induction 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%) | 2017 | Journal 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. |
AID1855262 | Induction 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%) | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1129007 | Inhibition of human HDAC-5 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1548267 | Induction 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 | |||
AID1816226 | Induction 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%) | |||
AID628437 | Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal 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. |
AID1478599 | Inhibition 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 analysis | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID274020 | Clearance after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1165116 | Cytotoxicity against human Jurkat gamma1 cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID316879 | Inhibition of human CEM cells assessed as viability | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1462222 | Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID593556 | Inhibition of human HDAC11 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1348920 | Inhibition of full length recombinant human HDAC5 preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1689778 | Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1129780 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1816222 | Induction 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%) | |||
AID1600659 | Inhibition 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 method | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID1848564 | Cytotoxicity against human WI-38 cells assessed as reduction in cell survival incubated for 30 mins by methylene blue staining based analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID344920 | Inhibition of HDAC1 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID1200971 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID420514 | Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at G2/M phase at IC80 using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID541652 | Inhibition of human HDAC6 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1246508 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1452274 | Inhibition of HDAC6 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. |
AID420643 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 48 hrs by Western blot | 2009 | European 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. |
AID1336950 | Induction 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%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1349716 | Inhibition of recombinant human full length C-terminal flag-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1742744 | Genotoxicity in Salmonella typhimurium TA1537 by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1742186 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1572358 | Induction of apoptosis in human T24 cells at 1 to 10 uM after 48 hrs by propidium iodide-staining based FACS analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1667099 | Cell 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 %) | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID525029 | Inhibition 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 control | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID288455 | Inhibition of tumor growth in MDA-MB-231 cells xenografted BALA/c nude mouse at 30 mg/kg, ip | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID1162484 | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents. |
AID420505 | Antiproliferative activity against human IGROV1 cells after 72 hrs | 2009 | European 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. |
AID1384235 | Effective permeability of the compound at 50 uM after 18 hrs by UV spectroscopy based PAMPA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1280281 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1349715 | Inhibition of human recombinant HDAC3/GST-tagged NCOR1 DAD (397 to 503 residues) expressed in baculovirus expression system after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID273167 | Inhibition of maize HD1A | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1128560 | Inhibition of human HDAC-7 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1541449 | Cytotoxicity against human A2780 cells assessed as reduction in cell survival measured after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1816236 | Antitumor 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 | |||
AID273177 | Induction of granulocytic differentiation of U937 cells measured as CD11c expression level after 48 hrs at 5 uM | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1816171 | Inhibition 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 | |||
AID1274879 | Inhibition of HDAC9 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1275632 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1742722 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1873410 | Inhibition of HDAC3 (unknown origin) preincubated for 30 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1235256 | Inhibition 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 assay | 2015 | Bioorganic & 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. |
AID1486998 | Inhibition 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 addition | 2017 | Bioorganic & 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. |
AID1548256 | Inhibition 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 | |||
AID1653099 | Antiproliferative activity against human HeLa cells by CCK8 assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1885673 | Synergistic antiproliferative activity against human L02 cells at 2.5 to 12.5 uM measured after 72 hrs in presence of CDDO-Me by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy. |
AID723159 | Potentiation 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 assay | 2013 | Journal 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. |
AID1548726 | Inhibition 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 analysis | 2020 | Journal 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. |
AID1769652 | Inhibition of ALK L1196M mutant (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1441677 | Anti-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 7 | 2017 | Journal 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. |
AID1821276 | Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID297493 | Cytotoxicity against human Hec-1-A cells | 2007 | Journal 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. |
AID1826642 | Induction 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%) | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID221993 | Compound was tested for anti-proliferative activity in human bone marrow cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1511150 | Antiproliferative activity against human HL60 cells incubated for 48 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1677520 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1177050 | Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1281847 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1901767 | Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID593553 | Inhibition of human HDAC8 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1690106 | Inhibition of HDAC in human HeLa cell nuclear extract using fluorescence substrate incubated for 30 mins by fluorescence based assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID1478589 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1864254 | Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability | 2022 | Journal 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. |
AID1898936 | Induction of DNA damage in human MM473 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1441696 | Protection 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 control | 2017 | Journal 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. |
AID1164179 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1651330 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID461269 | Antiproliferative activity against human CAL27 cells | 2010 | Journal 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. |
AID732444 | Inhibition of human MDA-MB-231 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID748100 | Inhibition of HDAC1 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1178594 | Inhibition 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 fluorometry | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1390024 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1720112 | Inhibition of EGFR (unknown origin) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID465159 | Growth inhibition of human SU-8686 cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID723449 | Potentiation 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 assay | 2013 | Journal 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. |
AID1348923 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1622978 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1587859 | Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1566040 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID1164797 | Half life in human hepatocytes at 5 uM by LCMS/MS analysis | 2014 | Journal 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. |
AID1174690 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1234890 | Inhibition 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 analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1441666 | Anti-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 ELISA | 2017 | Journal 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. |
AID481572 | Cytotoxicity against mouse S180 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID586609 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID1201644 | Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1206738 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1439780 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa. |
AID1312848 | Inhibition of full length recombinant human His-tagged p110 alpha/p85 alpha expressed in baculovirus expression system incubated for 1 hr by kinase-glo assay | 2016 | Journal 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. |
AID1390812 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
AID1421928 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1547266 | Inhibition of HDAC8 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1234901 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID737914 | Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis | 2013 | Journal 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. |
AID1775546 | Inhibition of HDAC2 (unknown origin) | 2021 | Journal 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 |
AID1337261 | Antiproliferative activity against human MDA-MB-231 cells up to 72 hrs by MTT assay | 2016 | Journal 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. |
AID308050 | Antiproliferative activity against mouse SC9 cells by MTS assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors. |
AID1566818 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1739588 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1848611 | Cytotoxicity against human SF-539 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1742760 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1753644 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1129006 | Inhibition of human HDAC-4 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID663403 | Half life in artificial gastric fluid | 2012 | Journal 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. |
AID1398823 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID717656 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1235258 | Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1751995 | Inhibition of HDAC6 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1753843 | Selectivity index, ratio of IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1141786 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal 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. |
AID1164042 | Antiproliferative activity against human MOLT4 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1614138 | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay | |||
AID461267 | Antiproliferative activity against human SCC15 cells | 2010 | Journal 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. |
AID1754757 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID616001 | Antiproliferative activity against human Hep3B cells after 48 hrs by SRB assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1655788 | Inhibition of human recombinant HDAC2 using AMC-K(Ac)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID499808 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1275644 | Growth inhibition of human A549 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1401532 | Antiproliferative activity against human A431 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1482115 | Cytotoxicity against human THP1 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1848622 | Cytotoxicity against human HCT-15 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID780573 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors. |
AID445124 | Inhibition of human recombinant HDAC1 expressed in baculovirus assessed as residual activity at 5 uM | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID1864225 | Inhibition of full length recombinant N-terminal GST-tagged human HDAC8 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay | 2022 | Journal 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. |
AID420324 | Inhibition of HDAC1 by fluorogenic enzyme assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1363798 | Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID1478594 | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1808549 | Inhibition 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 assay | 2021 | Journal 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). |
AID723129 | Potentiation 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 assay | 2013 | Journal 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. |
AID1349730 | Antitumor 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 days | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1227025 | Retention time of the compound in HEPES buffer treated with SAHA-TAP at pH 7.4 by LC-MS analysis in presence of GSH | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID347873 | Growth inhibition of human Melanoma cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1193536 | Inhibition 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 assay | 2015 | Bioorganic & 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. |
AID1890331 | Stability in human plasma incubated for 6 hrs in presence of NADPH and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1421918 | Gametocytocidal activity against synchronized Plasmodium falciparum NF54 mature stage 5 gametocytes after 48 hrs by ATP bioluminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID286790 | Inhibition of HDAC3 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Bispyridinium dienes: histone deacetylase inhibitors with selective activities. |
AID1497925 | Induction 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 analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | Development of the first small molecule histone deacetylase 6 (HDAC6) degraders. |
AID1541446 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID105415 | Antiproliferative activity against MDA-435 (human breast carcinoma) cell line. | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
AID1758461 | Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1671982 | Cell cycle arrest in human HCT-116 cells assessed as accumulation at G2/M phase measured after 24 hrs | 2019 | Bioorganic & 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. |
AID1861258 | Inhibition of HDAC2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1652193 | Inhibition 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 assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1769643 | Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID366640 | Inhibition of HDAC1 after 17 hrs | 2008 | Journal 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. |
AID1545987 | Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1614191 | Induction 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%) | |||
AID1861251 | Inhibition of HDAC derived from human HeLa cell nucleus | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1896935 | Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-05, Volume: 75 | Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells. |
AID1235257 | Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1493591 | Inhibition of human recombinant full-length HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID1901055 | Inhibition of HDAC2 (unknown origin) using trypsin and Ac-peptide as substrates | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID603544 | Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC in human HeLa cell nuclear extracts | 2011 | Journal 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. |
AID1655787 | Inhibition of human recombinant HDAC1 using AMC-K(Ac)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID593554 | Inhibition of human HDAC9 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1312849 | Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal 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. |
AID1326511 | Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1589336 | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors. |
AID1659651 | Inhibition of HDAC7 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID1886183 | Inhibition of HDAC1 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay | 2022 | Journal 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. |
AID1599724 | Cytotoxicity against human Meso163 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1266823 | Inhibition of HDAC in human HCT116 cells assessed as increase in acetyl-histone H3 expression at 5 uM after 48 hrs by immunoblotting analysis | 2015 | Journal 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. |
AID1321701 | Inhibition of HDAC2 (unknown origin) | 2016 | Journal 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. |
AID1598099 | Activation 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 re | 2019 | Journal 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. |
AID297498 | Cytotoxicity against human EOL1cells | 2007 | Journal 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. |
AID760372 | Inhibition of HDAC in human jurkat cells assessed as increase in H4K12 acetylation after 12 hrs by FACS analysis relative to control | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID723436 | Potentiation 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 assay | 2013 | Journal 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. |
AID90693 | Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi) | 2002 | Journal 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. |
AID352516 | Inhibition of human recombinant HDAC1 | 2009 | Bioorganic & 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. |
AID1126987 | Inhibition of HDAC2 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal 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. |
AID1263066 | Selectivity ratio of IC50 for human A549 cells to IC50 for African green monkey Vero cells | 2015 | Bioorganic & 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. |
AID1614233 | Induction 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%) | |||
AID1898896 | Resistance index, ratio of IC50 for human NCI-H460 cells to IC50 for H460-R9A cells | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1578497 | Induction 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 %) | 2020 | ACS 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. |
AID737916 | Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis | 2013 | Journal 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. |
AID760498 | Cytotoxicity against human U251 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID269669 | Antiproliferative activity against human PC3 cells by SRB assay | 2006 | Bioorganic & 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. |
AID1614197 | Induction 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%) | |||
AID1128558 | Inhibition of human HDAC-5 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID308651 | Increase in p27kip1 gene expression in PANC1 cells after 24 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID1597932 | Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID723466 | Inhibition of human HDAC1 by fluorescence assay | 2013 | Journal 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. |
AID1659655 | Antiproliferative activity against human PC3 cells incubated for 24 hrs by CCK8 assay | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID329919 | Induction of apoptosis in human U937 cells | 2008 | Bioorganic & 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. |
AID753164 | Cytotoxicity against human A549 cells | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID1898898 | Antiproliferative 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 assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1282292 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as death at 50 mg/kg, ip q2d for 9 days | 2016 | Journal 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. |
AID1816196 | Inhibition 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 | |||
AID1859929 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1547332 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1566039 | Inhibition 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 b | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID1702055 | Inhibition of HDAC1 in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate measured after 2 hrs by fluorescence based assay | 2018 | Journal 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. |
AID1234910 | Toxicity in human H7402 cells xenografted mouse assessed as change in toxic effect at 100 mg/kg/day, po for 16 days | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1566803 | Inhibition of recombinant full length human HDAC2 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1614196 | Induction 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%) | |||
AID1379287 | Inhibition 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 mi | 2017 | ACS 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. |
AID524996 | Inhibition of HDAC8 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1702237 | Oral bioavailability in Balb/c mouse at 50 mg/kg measured up to 24 hrs by LC/MS/MS analysis | 2018 | Journal 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. |
AID1848632 | Cytotoxicity against human TK-10 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1605972 | Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1449335 | Inhibition of HDAC1 in human Cal27CisR cells assessed as accumulation of histone 3 acetylation at 1 uM after 24 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1832671 | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1175813 | Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12 | Reniochalistatins A-E, cyclic peptides from the marine sponge Reniochalina stalagmitis. |
AID1349719 | Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID675298 | Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 1 uM by fluorescence assay | 2012 | Bioorganic & 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. |
AID1177052 | Antiprotozoan activity against Leishmania donovani MHOM- ET-67/L82 amastigotes | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1415638 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID420641 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 48 hrs by Western blot | 2009 | European 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. |
AID628209 | Antiproliferative activity against human SH-SY5Y cells after 24 hrs by XTT assay | 2011 | Journal 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. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID461255 | Antiproliferative activity against human H460 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID723423 | Potentiation 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 assay | 2013 | Journal 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. |
AID1173506 | Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1851613 | Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation | 2022 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 74 | Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives. |
AID1263147 | Antiproliferative activity against human MDA-MB-231 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID1709354 | Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human NAMALVA cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1764248 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1303691 | Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1765329 | Selectivity index, ratio of IC50 for human recombinant full length HDAC1 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1541554 | Inhibition of class 1 HDAC in human CAL27 cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID755615 | Cytotoxicity against SAHA-resistant human A549 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID1162487 | Growth inhibition of human HL60 cells after 72 hrs by CellTiter Glo assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents. |
AID1282260 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1361643 | Cell 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%) | 2018 | Journal 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. |
AID1449683 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID84276 | Inhibitory concentration against HT1080 cells proliferation | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID374831 | Antiproliferative activity against human U937 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID1065629 | Inhibition of human recombinant full length HDAC1 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1821314 | Antitumor activity against human HepG2 cells xenografted in mouse assessed as TGI at 12 mg/kg, ip administered every 2 days for 4 weeks | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID775829 | Inhibition 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 analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1339579 | Inhibition of HDAC1/HDAC2/HDAC3 in human U937 cells assessed as increase in histone H3 acetylation at 2 uM after 18 hrs by Western blot method | 2017 | ACS 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. |
AID1421613 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID618011 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1293557 | Antiproliferative activity against human H460 cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID748098 | Inhibition of HDAC3 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID310125 | Growth inhibition of human NB4 cells by SRB assay | 2007 | Bioorganic & 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. |
AID1055714 | Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID628452 | Inhibition of HDAC in human HepG2 cells assessed as increase in histone H4 acetylation at 1 to 10 uM after 6 hrs by Western blot analysis | 2011 | Journal 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. |
AID1355709 | Antifungal activity against FLC resistant Candida albicans 100 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID760388 | Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1422518 | Inhibition of HDAC in MEF assessed as increase in histone H4 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID366645 | Inhibition of HDAC10 after 17 hrs | 2008 | Journal 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. |
AID1785331 | Inhibition 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 | |||
AID1861307 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at G2/M phase in presence of pictilisib measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID343689 | Inhibition of nuclear HDAC isolated from human HeLa cells | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles. |
AID1410329 | Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID1730852 | Antiproliferation activity against human SK-BR-3 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1246527 | Resistance index, ratio of IC50 for imatinib resistant human IR-K562 cells to IC50 for human K562 cells | 2015 | Bioorganic & 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. |
AID1783107 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
AID527207 | Induction of autophagy in human A549 cells assessed as increase in LC3II after 3 hrs relative to control | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1578150 | Cytotoxicity against human SC9 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID462792 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2010 | Bioorganic & 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. |
AID1709350 | Cytotoxicity against human HS5 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID476828 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1166498 | Inhibition of human recombinant full length HDAC6 using (Boc-Lys (-acetyl)-AMC substrate after 30 mins | 2014 | Bioorganic & 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. |
AID760376 | Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1543944 | Inhibition of human recombinant HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1727729 | Inhibition of HDAC1 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1785008 | Antimigratory activity in human HepG2 cells assessed as reduction in wound closure at 6 uM measured after 48 hrs by scratch wound healing assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1459953 | Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1709351 | Selectivity index, ratio of IC50 for human HS5 cells to IC50 for human Jurkat cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1783067 | Antifungal activity against fluconazole-sensitive Candida albicans 7781 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1487088 | Growth inhibition of human Jurkat cells assessed as cell viability at 1 uM incubated for 44 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1826625 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1901153 | Inhibition 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 assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1901155 | Inhibition 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 assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1127017 | Antitumor 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 control | 2014 | Journal 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. |
AID1785329 | Inhibition 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 | |||
AID1848575 | Induction 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1863423 | Cytotoxicity against human HOP-62 cells assessed as cell viability after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1873403 | Inhibition of HDAC1 (unknown origin) preincubated for 120 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1900942 | Toxicity 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) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID1754799 | Downregulation of SIRT6 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1433259 | Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID316941 | Inhibition of HDAC9 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1487011 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC8 (unknown origin) | 2017 | Bioorganic & 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. |
AID1784193 | Inhibition of recombinant human HDAC6 using ZMAL as substrate incubated for 90 mins by fluorescence based micro plate assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis. |
AID1812442 | Inhibition of human recombinant HDAC1 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1861660 | Inhibition of colony formation in human HCT-116 cells at 2000 nM | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1865265 | Inhibition 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 analysis | 2022 | Journal 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. |
AID482939 | Inhibition of HDAC1 | 2010 | Bioorganic & 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. |
AID632972 | Cytotoxicity against human MCF7 cells | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1275651 | Antitumor 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 dosing | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1572380 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1398807 | Inhibition of HDAC3 in human MCF7 cells assessed as increase in acetylated histone H4 expression after 8 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1398822 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID90522 | Inhibitory concentration against rat liver Histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID1063055 | Inhibition of recombinant HDAC8 (unknown origin) using Fluor-de-Lys-HDAC8 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1677513 | Binding 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1525778 | Inhibition of HADC2 (unknown origin) | 2020 | Journal 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. |
AID1597941 | Antiproliferative activity against human BGC823 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID723430 | Potentiation 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 assay | 2013 | Journal 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. |
AID1469394 | Induction 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%) | 2018 | Journal 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 |
AID1245688 | Inhibition 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 assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1518827 | Antimalarial activity against ring stage Plasmodium falciparum 3D7 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID663356 | Growth inhibition of human NCI-H522 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1900929 | Toxicity in mouse bearing intracranial tumor assessed as median survival time at 50 mg/kg, ip for 10 days (Rvb= 13.8 days) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID1901148 | Inhibition of HDAC in human HeLa cell nuclear extracts using color de Lys as substrate measured after 30 mins by colorimetric assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1129005 | Inhibition of human HDAC-3/NCOR2 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID546545 | Inhibition of HDAC in human HeLa cell nuclear extracts | 2010 | Journal 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. |
AID1141804 | Antitumor 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 control | 2014 | Journal 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. |
AID1239051 | Cytotoxicity against human RPMI8226 cells assessed as cell viability after 72 hrs by CCK8 assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID1321733 | Inhibition 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 control | 2016 | Journal 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. |
AID1421603 | Inhibition of HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID765213 | Cytotoxicity against human A2780 cells | 2013 | Bioorganic & 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. |
AID476833 | Toxicity in FVB mouse assessed as effect on hematocrit at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1282251 | Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1597925 | Antiproliferative activity against human LoVo cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1303629 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1576455 | Cytotoxicity against human MCF10F cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID1855258 | Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1282252 | Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1541550 | Inhibition of HDAC6 in human CAL27 cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1737156 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1330926 | Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | 2017 | Bioorganic & 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. |
AID1515903 | Antiproliferative activity against human K562 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1518830 | Selectivity index, ratio of EC50 for human MDA-MB-231 cells to IC50 for ring stage Plasmodium falciparum K1 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID734732 | Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1865292 | Antitumor 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 | 2022 | Journal 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. |
AID1897390 | Induction 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 | |||
AID1876473 | Induction 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 %) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID710841 | Inhibition of HDAC by fluorescence assay | 2012 | Journal 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. |
AID1515915 | Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1897395 | Induction 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%) | |||
AID1234888 | Inhibition 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 analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1355687 | Inhibition 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 ATP | 2018 | Journal 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. |
AID476829 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID328826 | Antitumor 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 weeks | 2008 | Journal 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. |
AID1398799 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID723439 | Potentiation 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 assay | 2013 | Journal 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. |
AID1431819 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID723726 | Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID246080 | Effective Concentration of compound to inhibit the growth of human LOX-IMVI cells | 2005 | Journal 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. |
AID1688027 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1888591 | Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay | |||
AID1481747 | Antiproliferative activity against human RPMI8266 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
AID1732192 | Cytotoxicity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition. |
AID1422521 | Inhibition of human recombinant HDAC1 at 2 uM after 15 to 30 mins by fluorometric method | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID659495 | Inhibition of HDAC8 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1246525 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human THP1 cells | 2015 | Bioorganic & 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. |
AID1441657 | Anti-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 hrs | 2017 | Journal 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. |
AID1537556 | Selectivity 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 cel | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1451833 | Inhibition 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 fluore | 2017 | Journal 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. |
AID1915523 | Inhibition 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 method | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1164176 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1165104 | Antileishmanial activity against promastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1215086 | Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1502989 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1205625 | Inhibition 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 analysis | 2015 | Journal 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. |
AID1785339 | Inhibition of HDAC8 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | |||
AID723161 | Potentiation 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 assay | 2013 | Journal 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. |
AID1702068 | Inhibition 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 assay | 2018 | Journal 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. |
AID392398 | Inhibition of human recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus by fluorimetry | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Sulfamides as novel histone deacetylase inhibitors. |
AID1704068 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID420318 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1303621 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID723153 | Potentiation 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 assay | 2013 | Journal 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. |
AID1401506 | Inhibition of HDAC6 in human U937 cells assessed as increase in acetyl-alpha-tubulin levels at 5 uM after 18 hrs by Western blot method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1275592 | Inhibition of human recombinant HDAC3 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. |
AID1361642 | Cell 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%) | 2018 | Journal 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. |
AID1709356 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 24 hrs MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1623537 | Selectivity index, ratio of IC50 for HDAC10 (unknown origin) to IC50 for human recombinant HDAC6 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1686353 | Drug 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 spectrometry | 2016 | Journal 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. |
AID1832804 | Inhibition of human HDAC2 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm | 2021 | Journal 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. |
AID1858656 | Cytotoxicity against human SMMC-7721 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions. |
AID639798 | Oral bioavailability in mouse | 2011 | Journal 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. |
AID1848593 | Induction 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID316905 | Inhibition of human LOX-IMVI cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1293569 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1572352 | Inhibition 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 control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID519584 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1826651 | Antitumor 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 control | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1864226 | Inhibition 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 assay | 2022 | Journal 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. |
AID1390009 | Inhibition 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 assay | 2018 | Bioorganic & 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. |
AID1821270 | Inhibition of HDAC1 (unknown origin) incubated for 30 mins by microplate reader assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID461262 | Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1293570 | Inhibition of human HDAC9 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1487000 | Inhibition of HDAC2 (unknown origin) by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1511131 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1614232 | Induction 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%) | |||
AID1614227 | Induction 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%) | |||
AID1622901 | Cytotoxicity against human A549 cells after 72 hrs by CellTiter-Glo assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1897399 | Induction 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%) | |||
AID669760 | Growth inhibition of human A549 cells after 48 hrs by SRB assay | 2012 | Journal 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. |
AID759305 | Inhibition of human recombinant HDAC1 after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1449680 | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID384318 | Selectivity for IC50 of maize histone deacetylase 1B over IC50 of maize histone deacetylase 1A | 2008 | European 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. |
AID524995 | Inhibition of HDAC10 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID663399 | Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID546564 | Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay | 2010 | Journal 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. |
AID1550087 | Activation 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 analysis | 2019 | Journal 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. |
AID762186 | Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay | 2013 | Journal 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. |
AID1245680 | Inhibition 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 assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1742686 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1061948 | Cytotoxicity against human H460 cells | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1401369 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1545980 | Antiproliferative activity against human LoVo cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID420512 | Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at S phase at IC80 using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID1464872 | Inhibition of HDAC8 (unknown origin) | 2017 | Bioorganic & 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. |
AID1702088 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID605529 | Antiproliferative activity against human LoVo cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1454680 | Decrease in alcohol intake in rat assessed as operant alcohol self-administration at 50 mg/kg, ip administered once in a week relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
AID1578153 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1482130 | Antitumor 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 days | 2017 | Journal 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. |
AID723142 | Potentiation 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 assay | 2013 | Journal 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. |
AID1752936 | Inhibition 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 | |||
AID1753834 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1279129 | Inhibition of C-terminal His-tagged human recombinant HDAC8 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID1702083 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID226263 | Fold selectivity for classI HDAC | 2003 | Journal 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. |
AID350727 | Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID286789 | Inhibition of HDAC2 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Bispyridinium dienes: histone deacetylase inhibitors with selective activities. |
AID524823 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1384233 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1280308 | Inhibition of human KDAC6 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1469375 | Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID1876476 | Induction 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 analysis | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1141778 | Induction of apoptosis in human HCT116 cells assessed as accumulation at sub-G1 phase at 1 uM by propidium iodide staining-based flow cytometric analysis | 2014 | Journal 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. |
AID1915571 | Inhibition of HDAC (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID492806 | Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID723465 | Inhibition of human HDAC2 by fluorescence assay | 2013 | Journal 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. |
AID1390026 | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1821341 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1282241 | Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID461257 | Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1279124 | Inhibition 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 analysis | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID1653097 | Antiproliferative activity against human MCF7 cells by CCK8 assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1275634 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID71648 | Inhibitory concentration against friend cells proliferation | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID734731 | Cytotoxicity against human Jurkat gamma1 cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1282287 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as change in body weight at 100 mg/kg, po q2d for 8 days | 2016 | Journal 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. |
AID1605978 | Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1859932 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1754815 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID274100 | Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 90% of isolates after 48h. | 2007 | Bioorganic & 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. |
AID1326520 | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1887691 | Cytotoxicity against human WI-38 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID1808551 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 expressed in baculovirus infected Sf9 insect cells using fluorogenic substrate measured after 60 mins by FRET assay | 2021 | Journal 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). |
AID1246518 | Cytotoxicity against human K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & 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. |
AID1653138 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by SRB assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1478593 | Inhibition of HDAC8 (unknown origin) using substrate after 30 mins by fluorometric analysis | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1633670 | Neurotoxicity against rat CGN cells assessed as cell viability at 50 uM incubated for 24 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1200999 | Cmax in ICR mouse at 50 mg/kg, po | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1469313 | Induction 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%) | 2018 | Journal 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 |
AID1819514 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID1550109 | Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | Journal 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. |
AID1165109 | Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1487089 | Growth inhibition of human Jurkat cells assessed as cell viability at 10 uM incubated for 44 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID489911 | Inhibition of human HDAC8 | 2010 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13 | Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity. |
AID1282239 | Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID723141 | Potentiation 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 assay | 2013 | Journal 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. |
AID1380941 | Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1478596 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1303624 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1764803 | Selectivity 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-GA | 2021 | Journal 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. |
AID723457 | Potentiation of cisplatin-induced toxicity in cisplatin resistant human CAL27 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay | 2013 | Journal 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. |
AID1848586 | Inhibition of full length C-terminal his-tagged human recombinant HDAC8 expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1404296 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1482104 | Inhibition of HDAC 10 in human HeLa nuclear extract measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID440819 | Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. |
AID1193538 | Antiproliferative activity against human HCT116 cells after 5 days by Alamar Blue assay | 2015 | Bioorganic & 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. |
AID723476 | Cytotoxicity against cisplatin sensitive human CAL27 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1406985 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1720097 | Inhibition of BRD4 (unknown origin) at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID1886250 | Antitumor 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 days | 2022 | Journal 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. |
AID1548273 | Induction 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%) | |||
AID350715 | Inhibition of HDAC in human HeLa cell nuclear extracts by fluorimetry | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1633993 | Antiviral activity against HCV infected in human HuH7-luc/neo cells assessed as inhibition of DNA replication incubated for 3 days by luciferase reporter gene assay | 2019 | Bioorganic & 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). |
AID1865250 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID480068 | Inhibition of human recombinant HDAC2 preincubated for 24 hrs followed by 1 hr reaction with substrate by protease coupled end-point assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. |
AID1451823 | Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Journal 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. |
AID1702064 | Inhibition of HDAC5 (unknown origin) using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal 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. |
AID1688038 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID350716 | Inhibition of human recombinant HDAC1 by fluorimetry | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1164917 | Antiproliferative activity against human NCI-H929 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1164780 | Inhibition of HDAC1 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID580927 | Inhibition of HDAC activity in human HeLa cells at 0.1 uM after 24 hrs | 2010 | ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8 | Antiproliferative and differentiating activities of a novel series of histone deacetylase inhibitors. |
AID1441630 | Inhibition 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 mins | 2017 | Journal 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. |
AID710836 | Cytotoxicity against human NCI-H23 cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID732878 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID749390 | Inhibition of human recombinant HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
AID1200970 | Inhibition of HDAC6 in human A549 cells assessed as induction of tubulin acetylation after 17 to 18 hrs by ELISA | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1784970 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1764247 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1129783 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1622961 | Inhibition of HDAC2 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1549138 | Antifungal activity against azole-resistant Candida albicans 7781 after 48 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID765393 | Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID1234904 | Antiproliferative activity against human 3AO cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1174701 | Induction 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%) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1543943 | Inhibition of human recombinant HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1572351 | Inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 1 uM after 4 hrs by Western blot assay relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1737656 | Cytotoxicity against human KG -1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | |||
AID1785349 | Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1605973 | Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1897393 | Induction 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%) | |||
AID1303626 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID604139 | Inhibition of histone acetyltransferase in human U937 cells assessed as increase of pan-acetylated histone H4 level at 5 uM after 24 hrs by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). |
AID1742680 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1398814 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID481550 | Cytotoxicity against human HO8910 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1548244 | Inhibition 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 | |||
AID1650410 | Inhibition of recombinant human HDAC6 | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID1753842 | Selectivity index, ratio of IC50 for inhibition of HDAC3 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID663338 | Growth inhibition of human PC3 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1655792 | Inhibition of human recombinant HDAC6 using AMC-K(Ac)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID1698863 | Inhibition of c-MET (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID1888466 | Inhibition of purified human HDAC1 using Ac-Leu-Gly-(e-Ac)Lys-AMC by fluorometric HDAC assay | 2022 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 55 | Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat. |
AID1511971 | Inhibition 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 fluoresc | 2019 | ACS 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. |
AID1578498 | Induction 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 %) | 2020 | ACS 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. |
AID1659647 | Inhibition of HDAC1 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID90529 | Inhibitory concentration against histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID717660 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID619138 | Half life in rat liver microsomes | 2011 | Journal 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. |
AID663471 | Solubility in neutral water | 2012 | Journal 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. |
AID481555 | Cytotoxicity against human KB cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID632975 | Cytotoxicity against human NCI-H460 cells | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1469384 | Induction 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%) | 2018 | Journal 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 |
AID1742761 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1848304 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID274016 | Percent inhibition of CYP450 2C9 at 1 uM concentration | 2007 | Bioorganic & 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. |
AID348798 | Inhibition of HDAC3 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID440822 | Inhibition of human recombinant N-terminal FLAG-tagged HDAC5 (620-1122) expressed in baculovirus after 10 mins by fluorimetric analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. |
AID1201645 | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1518807 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1655801 | Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent cell viability assay | 2020 | ACS 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. |
AID1764292 | Inhibition 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) | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1901160 | Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1422512 | Inhibition of HDAC in mouse FL5.12 cells assessed as increase in histone H3 acetylation at 5 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1205626 | Induction of RUNX transcriptional activation in mouse C2C12-6xOSE2 cells at 1 uM after 24 hrs by luciferase reporter assay relative to FGF-2 | 2015 | Journal 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. |
AID1162217 | Cell 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%) | 2014 | Bioorganic & 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. |
AID1676592 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1396991 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors. |
AID1589335 | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate at 50 uM by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors. |
AID1861345 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID352760 | Antitumor 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 control | 2009 | Bioorganic & 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. |
AID1901159 | Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID723453 | Potentiation 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 assay | 2013 | Journal 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. |
AID1349720 | Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1888585 | Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay | |||
AID310185 | Growth inhibition of human ACHN cells by SRB assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID723127 | Potentiation 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 assay | 2013 | Journal 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. |
AID308649 | Increase in p21WAF1/CIP1 gene expression in PANC1 cells at 0.1 uM after 48 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID1383986 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID605299 | Antiproliferative activity against human HCT116 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1355690 | Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay | 2018 | Journal 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. |
AID1380942 | Antiproliferative activity against human AGS cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID669761 | Inhibition of human recombinant HDAC1 after 30 mins by fluorometric assay | 2012 | Journal 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. |
AID1129778 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID328800 | Inhibition of HDAC7 expressed in Escherichia coli | 2008 | Journal 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. |
AID1825921 | Inhibition 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 | |||
AID1784973 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1848321 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID723132 | Potentiation 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 assay | 2013 | Journal 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. |
AID1476147 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | Journal 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. |
AID723156 | Potentiation 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 assay | 2013 | Journal 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. |
AID609492 | Thermodynamic solubility of the compound at pH 6.8 | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1321726 | Lipophilicity, log D of the compound at pH 7.4 | 2016 | Journal 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. |
AID1783066 | Antifungal activity against fluconazole-sensitive Candida albicans 0304103 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1739597 | Antiproliferative activity against human HL60 assessed as reduction in cell growth at 1 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1901763 | Inhibition of full length human recombinant HDAC8 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1401387 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID481558 | Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1742649 | Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID273168 | Inhibition of maize HD1B | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1861260 | Inhibition of HDAC4 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1864241 | Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated H3 level at 1.25 to 5 uM by Western blot analysis | 2022 | Journal 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. |
AID1312851 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal 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. |
AID723422 | Potentiation 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 assay | 2013 | Journal 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. |
AID1164187 | Inhibition of human recombinant HDAC6 using Z-MAL as substrate after 1 hr by fluorescent activity assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID775843 | Inhibition of HDAC2 (unknown origin)-mediated deacetylation preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1754742 | Induction of apoptosis in human MCF7 cells assessed as downregulation of c-Myc gene expression at 1 uM measured after 24 hrs whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1464885 | Terminal half life in Sprague-Dawley rat 2 mg/kg, iv administered via bolus by LC-MS/MS analysis | 2017 | Bioorganic & 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. |
AID723148 | Potentiation 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 assay | 2013 | Journal 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. |
AID1493601 | Inhibition of HDAC6 in human A549 cells assessed as increase in acetylated alpha-tubulin levels at 500 nM after 3 hrs by Western blot analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID1239049 | Inhibition 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 hrs | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID243847 | Inhibitory activity against human histone deacetylase 4 (HDAC4) at 5 uM | 2005 | Journal 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. |
AID441872 | Inhibition of human recombinant HDAC8 using fluorescent acetylated substrate | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Binding ensemble profiling with photoaffinity labeling (BEProFL) approach: mapping the binding poses of HDAC8 inhibitors. |
AID1688030 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1897380 | Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID708273 | Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID421215 | Antitumor activity against human MCF10A cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID525000 | Inhibition of HDAC4 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1127321 | Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1633436 | Induction of neurogenesis in human SH-SY5Y cells assessed as stimulation of neurite outgrowth at 10 uM incubated for 72 hrs by phase contrast microscopic analysis | 2019 | ACS 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. |
AID1065945 | Inhibition of HDAC6 in human LNCAP cells assessed as increase in tubulin acetylation at 2.31 to 20 uM after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID639775 | Inhibition of KDM4E | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Lysine demethylases inhibitors. |
AID1361654 | Induction 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%) | 2018 | Journal 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. |
AID628438 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC3/NCoR2 | 2011 | Journal 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. |
AID1469376 | Induction 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%) | 2018 | Journal 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 |
AID373077 | Inhibition of human recombinant HDAC4 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1855245 | Inhibition 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 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID732154 | Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID652751 | Inhibition of recombinant human HDAC7 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1915562 | Inhibition of human HDAC1 incubated for 30 mins by SpectraMax M2 microplate reader analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1688023 | Inhibition 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 based | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1702154 | Metabolic stability in rat liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis | 2018 | Journal 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. |
AID1863169 | Inhibition of HDAC6 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID1129796 | Induction 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1897402 | Induction 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%) | |||
AID605537 | Antiproliferative activity against human COR-L23 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID481552 | Cytotoxicity against human HO8910 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID482959 | Octanol-water distribution coefficient, log D of the compound | 2010 | Bioorganic & 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. |
AID723450 | Potentiation 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 assay | 2013 | Journal 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. |
AID1487095 | Inhibition of HDAC8 (unknown origin) | 2017 | Bioorganic & 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. |
AID1418672 | GPx-like activity of the compound assessed as velocity for cumene hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & 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. |
AID689653 | Inhibition of HDAC8 after 45 mins by microplate fluorometric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Design, synthesis and evaluation of novel metalloproteinase inhibitors based on L-tyrosine scaffold. |
AID1189851 | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Hydroxamic acids block replication of hepatitis C virus. |
AID1434351 | Inhibition 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 FGF2 | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID456799 | Cytotoxicity against african green monkey Vero cells after 1 to 2 days by neutral red assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID473182 | Induction of HDAC-mediated H3/H4 histone acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA | 2010 | Journal 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. |
AID1303625 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1312929 | Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of acetylated alpha-tubulin level at 2 uM after 6 hrs by Western blot method | 2016 | Journal 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. |
AID723458 | Potentiation of cisplatin-induced toxicity in cisplatin resistant human A2780 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay | 2013 | Journal 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. |
AID1764284 | Inhibition 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 alo | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID274028 | AUC after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1742705 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID623097 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2011 | European 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. |
AID1389950 | Cytotoxic activity against human MCF7 cells after 24 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1487044 | Inhibition of HDAC1 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1260641 | Inhibition of human recombinant HDAC5 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1282255 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1541562 | Inhibition of class 1 HDAC in human Cal27CisR cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1266837 | Induction 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 analysis | 2015 | Journal 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. |
AID626566 | Growth inhibition of human HCT116 cells after 5 days by alamar blue assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22 | 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors. |
AID310184 | Growth inhibition of human HCT15 cells by SRB assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID1873390 | Inhibition of HDAC10 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID297489 | Cytotoxicity against human PC3 cells | 2007 | Journal 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. |
AID764215 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1819522 | Downregulation 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 analysis | 2022 | Journal 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. |
AID723452 | Potentiation 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 assay | 2013 | Journal 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. |
AID1543932 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1821275 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1816710 | Inhibition of HDAC2 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID274071 | Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID723144 | Potentiation 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 assay | 2013 | Journal 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. |
AID1206747 | Induction of nitric oxide release in human HEL cells at 100 uM after 3 to 5 hrs by Griess assay | 2015 | Journal 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. |
AID1873388 | Inhibition of HDAC8 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1742655 | Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1895827 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020). |
AID723454 | Potentiation 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 assay | 2013 | Journal 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. |
AID1174695 | Inhibition of HDAC6 (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1614139 | Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay | |||
AID1658891 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors. |
AID1063037 | Inhibition of recombinant HDAC6 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1476121 | Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHKKAc as substrate in presence of ATP | 2017 | Journal 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. |
AID1389952 | Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 16 uM after 24 hrs by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1126993 | Induction 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%) | 2014 | Journal 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. |
AID1861337 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1141771 | Cytotoxicity against human MKN45 cells by MTT assay | 2014 | Journal 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. |
AID1396985 | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors. |
AID1541563 | Inhibition 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) | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1730861 | Antiproliferative activity against human NCI-H820 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1848617 | Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID605398 | Inhibition of HDAC6 in human HCT116 cells assessed as induction of alpha-tubulin acetylation after 30 hrs by Western blot analysis | 2010 | Journal 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. |
AID1543938 | Antiproliferative activity against human Bel7402/5-FU cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1165115 | Cytotoxicity against human Jurkat cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1739568 | Antiproliferative activity against human HL60 assessed as reduction in cell growth at 100 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1754814 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1873406 | Inhibition of HDAC2 (unknown origin) preincubated for 60 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1759720 | Inhibition 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 b | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction. |
AID461253 | Antiproliferative activity against human HCC827 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID619049 | Competitive inhibition of HDAC4 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID723135 | Potentiation 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 assay | 2013 | Journal 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. |
AID1898902 | Antiproliferative activity against human MM487 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1439351 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous Non-Radioactive assay | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID1690837 | Inhibition 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 fluores | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1784987 | Inhibition of HDAC3 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID663375 | Growth inhibition of human SNB19 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1164026 | Inhibition of human recombinant HDAC3 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1633439 | Immunomodulatory 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 analysis | 2019 | ACS 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. |
AID80076 | Inhibitory activity against H1299 human lung carcinoma cell growth | 2003 | Journal 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). |
AID1336936 | Inhibition of class 1 HDAC in human LNCAP cells assessed as acetylated histone H4 accumulation at 10 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1542181 | Inhibition of HDAC3 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID324956 | Inhibition of HDAC6 in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID1273866 | Inhibition of HDAC in human HeLa cells nuclear extract using Fluor de lys as substrate after 15 mins by fluorometric analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1401530 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1605966 | Antiproliferative activity against human SR cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID725670 | Inhibition 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 additio | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
AID1848277 | Inhibition of PI3Kalpha (unknown origin) by mobility shift assay | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID476836 | Toxicity in FVB mouse assessed as effect on body weight at 50 mg/kg, po administered 5 times per week for 2 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1739571 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1361641 | Cell 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%) | 2018 | Journal 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. |
AID1865272 | Inhibition of SHP2 in human MV4-11 cells assessed as downregulation of ERK phosphorylation incubated for 24 hrs by Western blot analysis | 2022 | Journal 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. |
AID1462215 | Inhibition of recombinant human HDAC1 at 0.1 uM after 30 mins by fluorescence assay relative to control | 2017 | Bioorganic & 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. |
AID1890309 | Inhibition of HDAC2 (unknown origin) using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1173505 | Inhibition of full length C-terminal 6x-His tagged human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1547271 | Inhibition of HDAC7 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1688026 | Inhibition 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 base | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1826595 | Inhibition 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 microtite | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1348922 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1234887 | Inhibition 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 analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1421924 | Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1873405 | Inhibition of HDAC2 (unknown origin) preincubated for 30 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1898937 | Induction of DNA damage in human MM487 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID669757 | Growth inhibition of human Hep3B cells after 48 hrs by SRB assay | 2012 | Journal 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. |
AID1348919 | Inhibition 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 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1826597 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1164025 | Inhibition of human recombinant HDAC2 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1816235 | Antitumor 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 | |||
AID603532 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID723140 | Potentiation 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 assay | 2013 | Journal 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. |
AID1361639 | Inhibition of HDAC in human A549 cells assessed as increase in histone H4 acetylation after 24 hrs by Western blot analysis | 2018 | Journal 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. |
AID619052 | Competitive inhibition of HDAC7 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1882977 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer. |
AID1832686 | Inhibition of full length human HDAC2 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1671984 | Cell cycle arrest in human MCF7/ADR cells assessed as accumulation at G2/M phase measured after 24 hrs | 2019 | Bioorganic & 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. |
AID1856989 | Inhibition of HDAC6 (unknown origin) preincubated for 5 mins followed by substrate addition and measured after 30 mins by multimode microplate reader analysis | 2022 | Journal 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. |
AID711157 | Inhibition of HDAC8 by fluorometric assay | 2012 | Journal 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. |
AID446341 | Inhibition of histone acetylation in human K562 cells at 0.5 uM by flow cytofluorometry relative to control | 2010 | Journal 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. |
AID1164193 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1578493 | Induction 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 %) | 2020 | ACS 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. |
AID1541452 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID545854 | Inhibition of human HDAC in HeLa cells by fluorescent activity assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1765326 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1819521 | Downregulation 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 analysis | 2022 | Journal 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. |
AID723478 | Cytotoxicity against cisplatin sensitive human MDA-MB-231 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1293558 | Antiproliferative activity against human LoVo cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1543937 | Antiproliferative activity against human Bel7402 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1633424 | Inhibition 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 ELISA | 2019 | ACS 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. |
AID723441 | Potentiation 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 assay | 2013 | Journal 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. |
AID1415647 | Inhibition of HDAC2 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1260642 | Inhibition of human recombinant HDAC6 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1633994 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay | 2019 | Bioorganic & 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). |
AID269672 | Antiproliferative activity against human ACHN cells by SRB assay | 2006 | Bioorganic & 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. |
AID1548266 | Induction of apoptosis in human RPMI8226 cells assessed as induction of caspase-3/7 activation incubated for 24 hrs by fluorometric assay | |||
AID1833062 | Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID1129773 | Increase in p21 mRNA level in human Jurkat cells at 10 uM after 24 hrs by quantitative RT-PCR analysis | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1915570 | Cytotoxicity against human MDA-MB-231 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1279127 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID1897491 | Toxicity 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 | |||
AID300839 | Growth inhibition of human hepatocytes after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID327547 | Increase in acetylated alpha tubulin level in human HCT116 cells at 10 uM after 24 hrs relative to control | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID1390962 | Inhibition of HDAC1 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis | 2018 | Bioorganic & 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). |
AID1380948 | Antiproliferative activity against human HEL cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID350728 | Growth inhibition of human DMS114 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1282262 | Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID476651 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID347869 | Growth inhibition of human Breast cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1281856 | Antiproliferative activity against human JeKo1 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID631666 | Inhibition of human recombinant full-length HDAC1 using fluorophore conjugated substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). |
AID723157 | Potentiation 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 assay | 2013 | Journal 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. |
AID1548914 | Induction 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 analysis | 2020 | Journal 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. |
AID1164027 | Inhibition of human recombinant HDAC8 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID538409 | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Inhibitors selective for HDAC6 in enzymes and cells. |
AID1250654 | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay | 2015 | Journal 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. |
AID1900913 | Cytotoxicity against human TMZ-resistant U251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID1633672 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1722283 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17 | The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells. |
AID1758464 | Dark toxicity in human HCT-116 cells assessed as reduction in cell viability incubated under dark for 48 hrs measured after 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1605979 | Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID482970 | Toxicity in human PC3 cells xenografted nude mouse | 2010 | Bioorganic & 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. |
AID1201650 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1293568 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1352480 | Inhibition of HDAC1 in human HeLa cells after 72 hrs by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID274024 | Bioavailability after i.p. dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1201649 | Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID488237 | Inhibition of HDAC2 after 10 mins by fluorometric assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID1266826 | Cytotoxicity against rat IEC-18 cells assessed as survival after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1819505 | Inhibition of HDAC6 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2022 | Journal 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. |
AID603538 | Antitumor 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 days | 2011 | Journal 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. |
AID1864220 | Binding 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 assay | 2022 | Journal 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. |
AID1677500 | Induction of apoptosis in human HeLA cells at 3 uM after 48 hr by annexin V FITC and propidium iodide staining based flow cytometric analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1240554 | Induction 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%) | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID328809 | Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID723124 | Potentiation 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 assay | 2013 | Journal 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. |
AID1248352 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID663359 | Growth inhibition of human HCT15 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID525015 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1810053 | Displacement of [3H]SCH58261 from adenosine A2A receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis | |||
AID1737141 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID255817 | Inhibitory concentration against Histone deacetylase 1A in maize | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates. |
AID545860 | Antimalarial activity against sPlasmodium falciparum VS/1 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1441634 | Inhibition 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 analysis | 2017 | Journal 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. |
AID1548302 | Induction 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%) | |||
AID609508 | Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors. |
AID748099 | Inhibition of HDAC2 in human HeLa cells assessed as increase in histone H3 acetylation at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1384225 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1861328 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1873385 | Inhibition of HDAC5 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1777023 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase. |
AID1384219 | Inhibition 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 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID545861 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCB1 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID456801 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID1737137 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1454051 | Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID348391 | Inhibition of HDAC in human NB4 cells assessed as induction of histone H4 acetylation after 6 hrs by Western blot analysis | 2008 | Bioorganic & 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. |
AID1832691 | Inhibition 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 method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID366644 | Inhibition of HDAC6 after 17 hrs | 2008 | Journal 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. |
AID1848587 | Inhibition of full length N-terminal GST/C-terminal his-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID445134 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID1449333 | Inhibition of HDAC6 in human Cal27CisR cells assessed accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1890315 | Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1127012 | Induction 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 analysis | 2014 | Journal 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. |
AID618331 | Antitumor 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 15 | 2011 | Journal 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. |
AID723119 | Potentiation 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 assay | 2013 | Journal 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. |
AID1771468 | Inhibition of tubulin polymerization (unknown origin) measured after 1 min by fluorescence assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID482954 | Solubility at pH 7 | 2010 | Bioorganic & 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. |
AID1476120 | Inhibition 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 control | 2017 | Journal 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. |
AID655471 | Restoration 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 control | 2011 | ACS 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. |
AID1875503 | Inhibition 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 analysis | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID1614129 | Inhibition 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 | |||
AID1826623 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1898527 | Acute toxicity in po dosed ICR mouse assessed as maximum tolerated dose measured after 7 days | 2021 | Journal 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. |
AID1449323 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1709366 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID723435 | Potentiation 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 assay | 2013 | Journal 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. |
AID1537560 | Antiproliferative activity against human NB-1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1578479 | Inhibition 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 assay | 2020 | ACS 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. |
AID1065637 | Inhibition of human recombinant HDAC5 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1390022 | Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1740130 | Inhibition 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 substrate | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1816712 | Inhibition of HDAC11 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1864268 | Antitumor 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 days | 2022 | Journal 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. |
AID1548263 | Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay | |||
AID1650440 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID1702195 | Antitumor 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 14 | 2018 | Journal 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. |
AID1127322 | Antiproliferative activity against p53 defective cis-platinum-resistant human IGROV1/Pt1 cells assessed as growth inhibition after 72 hrs | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1482174 | Cytotoxicity against human MCF7 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1282300 | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal 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. |
AID1848585 | Inhibition of full length C-terminal his6/FLAG-tagged human recombinant HDAC3 (1 to 2383 residues) expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID350723 | Ratio of GI50 for human MKN45 cells to IC50 for human recombinant HDAC1 | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1541457 | Inhibition 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 by | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1890339 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1390020 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1441659 | Anti-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 met | 2017 | Journal 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. |
AID374829 | Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID1650437 | Inhibition of HDAC6 in human Cal27CisR cells assessed as increase in acetylated alpha-tubulin at 3 uM incubated for 24 hrs by immunoblot analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID274102 | Inhibition of maize HD1-B (mean) | 2007 | Bioorganic & 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. |
AID411262 | Cytotoxicity against HMEC after 72 hrs by trypan blue exclusion assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1282231 | Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID350729 | Growth inhibition of human LOXIMVI cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1861343 | Inhibition of HDAC in human OCILY3 cells assessed as effect on pS6 levels at 2.5 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1698862 | Inhibition of HDAC1 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID1578886 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2019 | Journal 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. |
AID1245682 | Cytotoxicity against human HEL cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1548257 | Inhibition 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 | |||
AID1775568 | Inhibition of human DNMT1 enzyme using polydeoxy-inosine polydeoxy-cytosine DNA as substrate incubated for 15 mins in presence of SAM by TR-FRET assay | 2021 | Journal 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 |
AID1650416 | Cytotoxicity against human CAL27 cells assessed as reduction in cell viability by MTT assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID1537554 | Inhibition 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 a | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID443633 | Inhibition of mouse recombinant serine racemase expressed in Escherichia coli MC1061 assessed as formation of D-serine at 5 mM after 30 mins by HPLC analysis | 2009 | Journal 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. |
AID1563941 | Inhibition of recombinant HDAC2 (unknown origin) measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. |
AID1848596 | Cytotoxicity against human CCRF-CEM cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1855249 | Binding affinity to pBR322 DNA (unknown origin) at 50 uM after 30 mins by Agarose gel electrophoresis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID316892 | Inhibition of HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID274029 | Oral bioavailability after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1688021 | Cytotoxicity against human PC-3 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID525020 | Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 1 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1201651 | Antiproliferative activity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1451821 | Inhibition 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 assay | 2017 | Journal 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. |
AID1231808 | Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | 2015 | Bioorganic & 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. |
AID1263067 | Selectivity ratio of IC50 for human MCF7 cells to IC50 for African green monkey Vero cells | 2015 | Bioorganic & 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. |
AID1389954 | Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 70 uM after 24 hrs by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1686356 | Competitive 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 anal | 2016 | Journal 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. |
AID663353 | Growth inhibition of human NCI-H23 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1174685 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1401535 | Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1897405 | Induction 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%) | |||
AID1293561 | Antiproliferative activity against mitoxantrone resistant human HT-29 cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID723451 | Potentiation 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 assay | 2013 | Journal 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. |
AID723160 | Potentiation 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 assay | 2013 | Journal 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. |
AID1888407 | Synergistic 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 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID1166499 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by WST8 assay | 2014 | Bioorganic & 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. |
AID1511153 | Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1275590 | Inhibition of human recombinant HDAC1 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. |
AID1464870 | Inhibition of HDAC1 (unknown origin) | 2017 | Bioorganic & 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. |
AID622258 | Inhibition of HDAC1 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1386704 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1848628 | Cytotoxicity against human ACHN cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID329926 | Induction of granulocytic differentiation in human U937 cells assessed as CD11c expression at 5 uM after 30 hrs | 2008 | Bioorganic & 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. |
AID286792 | Effect on alpha tubulin acetylation in U937 cells at 1 uM after 24 hrs by Western blot analysis | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Bispyridinium dienes: histone deacetylase inhibitors with selective activities. |
AID613328 | Antitumor 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 control | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID723444 | Potentiation 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 assay | 2013 | Journal 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. |
AID1890514 | Inhibition of HDAC8 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID328796 | Inhibition of HDAC4 expressed in Escherichia coli | 2008 | Journal 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. |
AID760502 | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1511127 | Induction 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 analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID297477 | Cytotoxicity against human A549 cells | 2007 | Journal 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. |
AID1421611 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1742628 | Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated Histone H3 incubated for 8 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID765376 | Inhibition of recombinant human HDAC7 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins | 2013 | Journal 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. |
AID609497 | Half life in rat liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1441637 | Inhibition 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 assay | 2017 | Journal 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. |
AID421197 | Antitumor activity against human MCF7 cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID605393 | Inhibition of human recombinant HDAC2 using fluor de Lys as substrate by fluorometric analysis | 2010 | Journal 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. |
AID1164198 | Antiproliferative activity against human MCF7 cells assessed as reduction in doubling time at 5 uM after 10 to 18 hrs by real-time mode analysis | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1861648 | Antiproliferative activity against human HCT-116 cells measured after 72 hrs | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID316878 | Inhibition of HDAC in human CEM cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID421217 | Inhibition of HDAC3 from human HeLa cells at 5 uM | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID1061952 | Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1847778 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID1855244 | Inhibition 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 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1639364 | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1812434 | Antiplasmodial activity against asynchronous asexual culture of Plasmodium falciparum NF54 assessed as parasite growth inhibition | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1403152 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID481565 | Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1129012 | Inhibition of human HDAC-10 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1337256 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1439771 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa. |
AID1542187 | Inhibition of HDAC9 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1655894 | Inhibition 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) | 2020 | ACS 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. |
AID1865262 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1201646 | Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1235116 | Cytotoxicity against human ES2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1597936 | Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1281867 | Induction 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%) | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1515916 | Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1777021 | Inhibition of HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase. |
AID408882 | Inhibition of HDAC3 | 2008 | Journal 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. |
AID1234896 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID744873 | Cytotoxicity against human U251 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Discovery of adamantane based highly potent HDAC inhibitors. |
AID1676601 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1515909 | Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1664992 | Inhibition 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 hrs | 2020 | ACS 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. |
AID1861326 | Inhibition of HDAC in human DOHH-2 cells assessed as effect on total Stat3 levels at 2.5 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1550127 | Induction 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%) | 2019 | Journal 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. |
AID255813 | Inhibitory concentration against Histone deacetylase 2 in maize | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates. |
AID1890311 | Inhibition of HDAC8 (unknown origin) using Boc-Lys-(triflouroacetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1200972 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1614120 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | |||
AID1164916 | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1722285 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17 | The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells. |
AID1248356 | Inhibition 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 assay | 2015 | Bioorganic & 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. |
AID723133 | Potentiation 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 assay | 2013 | Journal 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. |
AID1915524 | Inhibition 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 method | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1173500 | Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1326515 | Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID717792 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID476835 | Toxicity in FVB mouse assessed as effect on body weight at 50 mg/kg, po administered 5 times per week for 2 weeks measured during test | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1597934 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1614245 | Inhibition 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 | |||
AID1063035 | Inhibition of recombinant HDAC11 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1614259 | Toxicity against NOD/SCID mouse xenografted with human MM1S cells assessed as mouse survival at 50 mg/kg, po qd administered for 10 days | |||
AID1754753 | Inhibition 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 r | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1808552 | Inhibition 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 assay | 2021 | Journal 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). |
AID1274877 | Inhibition of HDAC7 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1511136 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID734736 | Inhibition of HDAC1 (unknown origin) at 10 uM after 60 mins by SAMDI spectrophotometric analysis relative to control | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1915564 | Inhibition of human HDAC6 incubated for 30 mins by SpectraMax M2 microplate reader analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID675299 | Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate by fluorescence assay | 2012 | Bioorganic & 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. |
AID603533 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1751994 | Selectivity ratio of IC50 for HDAC11 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID663395 | Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1765327 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID723447 | Potentiation 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 assay | 2013 | Journal 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. |
AID1511130 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1704065 | Inhibition 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 method | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID1622963 | Inhibition of HDAC8 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID538408 | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Inhibitors selective for HDAC6 in enzymes and cells. |
AID1890510 | Inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1324233 | Inhibition 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 control | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID1441698 | Anti-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 7 | 2017 | Journal 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. |
AID1274871 | Inhibition of HDAC1 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID488238 | Inhibition of HDAC3 after 10 mins by fluorometric assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID546549 | Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain | 2010 | Journal 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. |
AID1863422 | Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1127002 | Induction 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%) | 2014 | Journal 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. |
AID1127333 | Induction of apoptosis in human IGROV1 cells at IC80 after 72 hrs by TUNEL and flow cytometry analysis (Rvb = 4%) | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1760297 | Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1578475 | Inhibition 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 assay | 2020 | ACS 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. |
AID1599783 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID420503 | Antiproliferative activity against human H460 cells after 72 hrs | 2009 | European 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. |
AID373081 | Inhibition of human recombinant HDAC8 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID663334 | Growth inhibition of human K562 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1127329 | Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1441700 | Inhibition 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 analysis | 2017 | Journal 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. |
AID1702090 | Antiproliferative activity against human SNU-398 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1742752 | Antitumor 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 34 | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1647328 | Anti-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 recognition | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID765222 | Cytotoxicity against human SKOV3 cells | 2013 | Bioorganic & 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. |
AID1816192 | Inhibition 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 | |||
AID1622980 | Cytotoxicity against human MDA-MB-231 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1164039 | Antiproliferative activity against human HT1080 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1651331 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID1690842 | Inhibition 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 assa | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID456796 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID1293563 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1336925 | Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1380966 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1547267 | Inhibition of HDAC5 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1887064 | Cytotoxicity against human NCI-H522 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis. |
AID1890314 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1449325 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1578148 | Antiproliferative activity against human HT1080 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1235114 | Cytotoxicity against HEL cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID723475 | Cytotoxicity against cisplatin resistant human CAL27 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1174682 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID329918 | Induction of p21 expression in human U937 cells | 2008 | Bioorganic & 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. |
AID663389 | Growth inhibition of human ACHN cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID414719 | Inhibition of HDAC in human HeLa cells assessed as induction of cellular histone H3 hyperacetylation | 2009 | Journal 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. |
AID1915594 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1751997 | Inhibition of HDAC11 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1599726 | Cytotoxicity against human ADCA72 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1605937 | Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID511063 | Inhibition of HDAC1 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1865258 | Inhibition 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 analysis | 2022 | Journal 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. |
AID420513 | Cell cycle arrest in cisplatin-resistant human IGROV1 cells assessed as partial accumulation at S phase at IC90 using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID1469289 | Induction 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%) | 2018 | Journal 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 |
AID411257 | Selectivity for ratio of IC50 for human HDAC6 to IC50 for human HDAC1/2 by fluorimetric assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID90352 | In vitro inhibitory activity against human histone deacetylase (HDAC) using HeLa nuclear extract | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Thiol-based SAHA analogues as potent histone deacetylase inhibitors. |
AID1915526 | Antiproliferative activity against human DU-145 cells incubated for 48 hrs by Sulforhodamine B staining method | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1614229 | Induction 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%) | |||
AID1821956 | Inhibition 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 | |||
AID1865308 | Antitumor 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%) | 2022 | Journal 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. |
AID353356 | Inhibition of HDAC in human SHSY5Y cells by fluorimetric cellular activity assay | 2009 | Journal 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. |
AID527041 | Cytotoxicity against human NCI-H226 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1591852 | Inhibition 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 cont | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID411256 | Inhibition of HDAC6 from human HeLa cells nuclear extract by cell free fluorimetric assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1127009 | Induction 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%) | 2014 | Journal 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. |
AID1164925 | Induction of HDAC6 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID331898 | Displacement 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 p | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID750108 | Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate at 10 uM by fluorescence assay | 2013 | Bioorganic & 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. |
AID1240553 | Induction 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%) | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID663368 | Growth inhibition of human NCI-ADR-RES cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID708270 | Growth inhibition of human HGC27 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID1514594 | Inhibition of HDAC1 (unknown origin) at 20 nM using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA relative to control | 2019 | Bioorganic & 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. |
AID243846 | Inhibitory activity against human histone deacetylase 1 (HDAC1) at 5 uM | 2005 | Journal 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. |
AID274019 | Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID723158 | Potentiation 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 assay | 2013 | Journal 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. |
AID1622937 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID358682 | Increase in E2F1 mRNA expression in rat ST14A cells after 72 hrs by RT-PCR relative to control | 2007 | The 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. |
AID1545830 | Antiproliferative activity against human HCT116 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1723743 | Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2020 | Journal 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. |
AID473031 | Ex vivo inhibition of human HDAC5 in human Caco-2 cells by fluorometric cellular activity assay | 2010 | Journal 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. |
AID604038 | Inhibition of histone acetyltransferase in human U937 cells assessed as increase of histone H3 acetylation level at 5 uM after 15 mins by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). |
AID1454055 | Growth inhibition of human T47D cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1861655 | Inhibition of HDAC3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID421218 | Inhibition of HDAC8 from human HeLa cells at 5 uM | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID1812441 | Inhibition of Plasmodium falciparum NF54 HDAC using extract measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1614121 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | |||
AID631667 | Inhibition of human recombinant full-length HDAC2 using fluorophore conjugated substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). |
AID1164032 | Inhibition of human recombinant HDAC6 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1808553 | Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 cells using fluorogenic substrate measured after 60 mins by FRET assay | 2021 | Journal 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). |
AID274096 | Inhibition of maize HD1-A (mean) | 2007 | Bioorganic & 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. |
AID1421923 | Antimalarial 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 | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID749702 | Inhibition of HDAC8 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1699973 | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2020 | Bioorganic & 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. |
AID1890515 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1518829 | Selectivity index, ratio of EC50 for human MDA-MB-231 cells to IC50 for ring stage Plasmodium falciparum 3D7 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1742660 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID445122 | Inhibition of HDAC | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID1401507 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1848600 | Cytotoxicity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1897406 | Induction 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%) | |||
AID723162 | Potentiation 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 assay | 2013 | Journal 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. |
AID1129785 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1754781 | Upregulation of NFkB2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1401531 | Antiproliferative activity against human Capan1 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1730855 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1816213 | Induction 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%) | |||
AID1203889 | Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID723145 | Potentiation 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 assay | 2013 | Journal 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. |
AID1698861 | Inhibition of c-MET (unknown origin) at 100 nM relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID723117 | Potentiation 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 assay | 2013 | Journal 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. |
AID1614231 | Induction 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%) | |||
AID1189854 | Therapeutic index, ratio of CC50 for human HuH7 cells to EC50 for HCV genotype 1b infected in human Huh7 cells | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Hydroxamic acids block replication of hepatitis C virus. |
AID1764802 | Selectivity 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( | 2021 | Journal 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. |
AID1784990 | Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID781052 | Inhibition of HDAC in human HeLa cell nuclear extracts using Fluor de Lys as substrate at 1 uM by fluorescence assay | 2013 | Bioorganic & 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. |
AID1246519 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & 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. |
AID90195 | Concentration required to inhibit Histone Deacetylase (HDAC) from K562 erythroleukemia cells | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC). |
AID488236 | Inhibition of HDAC in human SCC4 cells assessed as increase in histone acetylation at 1 uM after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID1312850 | Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal 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. |
AID1421911 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1178598 | Inhibition of human HDAC8 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1233266 | Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay | 2015 | Journal 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. |
AID1200984 | Half life in ICR mouse at 10 mg/kg, iv | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1410328 | Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID760492 | Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1380945 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID603541 | Antitumor 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 days | 2011 | Journal 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. |
AID81123 | Percent of HL-60 cells (from human acute promyelocytic leukemia) to develop the ability to reduce nitroblue tetrazolium after administration (1 uM) | 1995 | Journal 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. |
AID1330948 | Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1873418 | Inhibition of HDAC2 (unknown origin) at 5 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID723477 | Cytotoxicity against cisplatin resistant human MDA-MB-231 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1361635 | Inhibition of HDAC8 (unknown origin) after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID1737152 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1441667 | Plasma concentration in human | 2017 | Journal 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. |
AID710834 | Cytotoxicity against human NUGC3 cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID1476156 | Antiproliferative activity against human XG6 cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1667093 | Cell 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 %) | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID316906 | Inhibition of human SKOV3 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID348390 | Inhibition of HDAC in human NB4 cells assessed as induction of histone H3 acetylation after 6 hrs by Western blot analysis | 2008 | Bioorganic & 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. |
AID663331 | Inhibition of HDAC in human HeLa cell nuclear extracts using Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorimetry | 2012 | Journal 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. |
AID1469489 | Antitumor 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 control | 2018 | Journal 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 |
AID655470 | Inhibition of HDAC1 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1178597 | Inhibition of human HDAC3 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1469436 | Inhibition of HDAC1 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot method | 2018 | Journal 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 |
AID1141787 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal 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. |
AID1141788 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal 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. |
AID723121 | Potentiation 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 assay | 2013 | Journal 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. |
AID1239048 | Inhibition 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 hrs | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID1576448 | Inhibition of HDAC (unknown origin) nuclear extract at 0.5 uM relative to control | |||
AID1861664 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID481557 | Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID473030 | Ex vivo inhibition of human HDAC3 in human Caco-2 cells by fluorometric cellular activity assay | 2010 | Journal 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. |
AID1547268 | Inhibition of HDAC4 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1155320 | Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1742756 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1178596 | Inhibition of human HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1763822 | Inhibition of human recombinant HDAC6 incubated for 15 mins by fluorogenic assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID1819516 | Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID274117 | Inhibition of HeLa cell proliferation | 2006 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23 | A series of novel, potent, and selective histone deacetylase inhibitors. |
AID723134 | Potentiation 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 assay | 2013 | Journal 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. |
AID1421929 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1274875 | Inhibition of HDAC5 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID623022 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2011 | European 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. |
AID1274835 | Toxicity 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 control | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1572347 | Inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 10 uM after 4 hrs by Western blot assay relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID348799 | Inhibition of HDAC6 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID1403157 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID274170 | Antiproliferative activity against H1299 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID286793 | Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Bispyridinium dienes: histone deacetylase inhibitors with selective activities. |
AID316910 | Inhibition of human HDAC8 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID723728 | Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1251316 | Inhibition of HDAC1 (unknown origin) | 2015 | Bioorganic & 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. |
AID723125 | Potentiation 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 assay | 2013 | Journal 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. |
AID765385 | Inhibition of recombinant human HDAC6 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID1486303 | Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1181307 | Inhibition of HDAC6 in human U937 cells assessed as increase in acetyl-alpha-tubulin level at 5 uM by Western blotting method | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID105419 | Antiproliferative activity against human MDA-435 breast carcinoma cell line | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. |
AID313729 | Inhibition of HDAC1 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID708274 | Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID748109 | Inhibition of HDAC6 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1225988 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1865302 | Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on lung at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID316877 | Inhibition of human liver HDAC | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID734738 | Inhibition of HDAC8 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1630598 | Inhibition of recombinant full length C-terminal His-tagged human HDAC2 expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID760496 | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID310182 | Growth inhibition of human MDA-MB-231 cells by SRB assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID1437245 | Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID465157 | Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1764816 | Inhibition of Nanoluc-fused HDAC6 CD2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay | 2021 | Journal 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. |
AID1723742 | Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2020 | Journal 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. |
AID373079 | Inhibition of human recombinant HDAC6 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1597974 | Inhibition of HDAC in human HeLA cell nuclear extracts | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1141241 | Inhibition of MMP2 (unknown origin) using succinylated gelatin as substrate preincubated for 10 mins before substrate addition measured after 30 mins by spectrophotometry | 2014 | Bioorganic & 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. |
AID1709357 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 48 hrs MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1275655 | Toxicity 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 dosing | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1401905 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID1482173 | Cytotoxicity against human A549 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1482121 | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID420499 | Toxicity 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 weeks | 2009 | European 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. |
AID1348934 | Upregulation of CDH1 gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1754766 | Downregulation of HDAC10 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID759311 | Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1166500 | Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay | 2014 | Bioorganic & 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. |
AID1688029 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1600735 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1622927 | Inhibition of maize HD2 using [3H]acetate-labelled histone as substrate by liquid scintillation counting method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1542184 | Inhibition of HDAC6 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID288454 | Growth inhibition of NCI-H23 cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID374817 | Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells | 2009 | Journal 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. |
AID1514602 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID1887065 | Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human NCI-H522 cells by methylene blue staining based analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis. |
AID675297 | Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 0.1 uM by fluorescence assay | 2012 | Bioorganic & 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. |
AID1266092 | Inhibition of HDAC1 (unknown origin) by fluorimetric assay | 2016 | Bioorganic & 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. |
AID1702070 | Inhibition of human full length HDAC11 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal 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. |
AID1410323 | Inhibition of recombinant human full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID723128 | Potentiation 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 assay | 2013 | Journal 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. |
AID1469283 | Induction 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%) | 2018 | Journal 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 |
AID1667080 | Inhibition of STAT3 in human MDA-MB-231 cells assessed as downregulation of Bcl-xL expression after 24 hrs by western blot analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1863434 | Inhibition of HDAC2 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1421626 | Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1727745 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase after 24 hrs by flow cytometry | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID344916 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess 2-oxoglutarate and 10 uM Fe2 by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID1859931 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID672028 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID1321724 | Cytotoxicity against mouse primary glial cells assessed as reduction in cell viability after 72 hrs by luminescence based ATPlite assay | 2016 | Journal 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. |
AID711145 | Inhibition of HDAC8 at 0.3 uM in presence of 10 mol% Cu(I) by fluorometric assay | 2012 | Journal 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. |
AID1851615 | Cytotoxicity against HUVEC cells assessed as inhibition of cell growth | 2022 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 74 | Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives. |
AID1702087 | Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID526532 | Growth inhibition of human PC3 cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1622974 | Inhibition of HDAC8 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1754763 | Downregulation of HDAC5 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1901761 | Inhibition of full length human recombinant HDAC3 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID723473 | Cytotoxicity against cisplatin sensitive human KYSE-510 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID420501 | Antiproliferative activity against human NB4 cells after 72 hrs | 2009 | European 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. |
AID695300 | Induction of Oct3/4 gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes. |
AID1379282 | Inhibition 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 analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors. |
AID1401505 | Cytotoxicity against human Jurkat cells assessed as cell viability at 10 uM after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1466379 | Toxicity 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) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. |
AID1812435 | Cytotoxicity against human Hep-G2 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1399552 | Antiproliferative activity against human A549 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID1572354 | Antiproliferative activity against human HuH7 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1730862 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID723131 | Potentiation 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 assay | 2013 | Journal 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. |
AID1597971 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID269670 | Antiproliferative activity against human HCT15 cells by SRB assay | 2006 | Bioorganic & 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. |
AID1182314 | Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID609505 | Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors. |
AID1459947 | Antiproliferative activity against human HCT116 cells measured after 48 hrs by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID344917 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess H3K9me3 peptide and 10 uM Fe2 by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID373074 | Inhibition of human recombinant HDAC1 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID90702 | Inhibition of Histone deacetylase 6 (HDAC6) of HeLa nuclear extracts | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1415649 | Inhibition of HDAC6 in human HepG2 cells assessed as increase in acetylated-alpha tubulin level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1398806 | Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID723443 | Potentiation 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 assay | 2013 | Journal 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. |
AID1275633 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1371070 | Antiparasitic activity against tachyzoite stage of Toxoplasma gondii | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1622983 | Cytotoxicity against human PC3 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1875511 | Selectivity index, ratio of IC50 for cytotoxicity against HMEC cells to GI50 for antiproliferative activity against human NCI-H526 cells | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID1493590 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID1622899 | Inhibition of HDAC in human HeLa nuclear extract at 100 uM using Fluor-de-lys as substrate measured after 15 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1861649 | Antiproliferative activity against human MCF7 cells measured after 72 hrs | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1126959 | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2014 | Journal 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. |
AID1129009 | Inhibition of human HDAC-7 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID487874 | Antiproliferative activity against human A549 cells after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | New aryldithiolethione derivatives as potent histone deacetylase inhibitors. |
AID1240556 | Induction 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 cytometry | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID1578896 | Inhibition of HDAC in human Bel7402 cells assessed as increase in acetylated alpha-tubulin expression at 5 uM incubated for 72 hrs by Western blot analysis | 2019 | Journal 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. |
AID1742182 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1861255 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1652195 | Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1785337 | Inhibition of recombiant human HDAC6 using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence microplate reader assay | |||
AID1433298 | Induction 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 control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1633990 | Inhibition 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 analysis | 2019 | Bioorganic & 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). |
AID765374 | Inhibition of recombinant human HDAC9 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins | 2013 | Journal 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. |
AID1126960 | Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2014 | Journal 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. |
AID772639 | Inhibition 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 analysis | 2013 | Journal 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. |
AID1898895 | Antiproliferative activity against human H460-R9A cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1576449 | Inhibition 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 | |||
AID1876344 | Inhibition of recombinant full length HDAC11 (unknown origin) expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID708279 | Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID445136 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID1873401 | Inhibition of HDAC1 (unknown origin) preincubated for 60 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1542183 | Inhibition of HDAC5 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID541650 | Inhibition of human HDAC7 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1785350 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1380987 | Antitumor 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 control | 2018 | Journal 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. |
AID628439 | Inhibition of human recombinant HDAC8 using Fluor de Lys as substrate | 2011 | Journal 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. |
AID1202584 | Inhibition of His-tagged HDAC6 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID760493 | Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1126978 | Antiproliferative activity against HEL cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID628208 | Antiproliferative activity against human SH-SY5Y cells after 48 hrs by XTT assay | 2011 | Journal 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. |
AID723471 | Inhibition of HDAC in cisplatin resistant human MDA-MB-231 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1783064 | Antifungal activity against Cryptococcus neoformans H99 assessed as inhibition of fungal growth incubated for 72 hrs by two-fold serial microdilution method | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1486323 | Genotoxicity in Salmonella typhimurium TA102 at 50 times antiproliferative IC50 by Ames test | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID749697 | Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1063058 | Inhibition of recombinant HDAC3 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID737910 | Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID420508 | Induction of apoptosis in human IGROV1 cells at IC80 after 72 hrs by TUNEL assay | 2009 | European 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. |
AID1547315 | Increase 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1591721 | Inhibition 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 analysis | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1280280 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1451824 | Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Journal 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. |
AID1888410 | Cytotoxicity against human HaCaT cells assessed as inhibition of cell growth | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID723442 | Potentiation 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 assay | 2013 | Journal 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. |
AID1201643 | Inhibition of human recombinant FLT3 after 1 hr by LanthaScreen assay platform | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID445137 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID663339 | Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay | 2012 | Journal 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. |
AID1173504 | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1127326 | Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1739589 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID482973 | Antitumor 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 22 | 2010 | Bioorganic & 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. |
AID603534 | Cytotoxicity against human NB4 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID663367 | Growth inhibition of human OVCAR8 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1282285 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as change in body weight at 50 mg/kg, ip q2d for 9 days | 2016 | Journal 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. |
AID1541443 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1650408 | Inhibition of HDAC6 in human CAL27 cells assessed as increase in acetylated alpha-tubulin at 3 uM incubated for 24 hrs by immunoblot analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID208380 | Concentration required to inhibit complete cell proliferation of T/5 cells | 1995 | Journal 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. |
AID673991 | Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1282259 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1864253 | Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability | 2022 | Journal 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. |
AID1888420 | Inhibition of human HDAC | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID759308 | Therapeutic index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells expressing ERalpha and ERbeta | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1449319 | Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1684873 | Toxicity 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) | |||
AID1549162 | Inhibition 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 fluorimetry | 2020 | Journal 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. |
AID1614228 | Induction 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%) | |||
AID1235260 | Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1742721 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID723427 | Potentiation 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 assay | 2013 | Journal 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. |
AID1396959 | Antiproliferative activity against human HCT116 cells | 2018 | Bioorganic & 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). |
AID1330946 | Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1398802 | Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID525024 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 1 uM by RT-PCR | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1898901 | Antiproliferative activity against human MM473 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1127004 | Induction 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%) | 2014 | Journal 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. |
AID605622 | Cell 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 analysis | 2010 | Journal 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. |
AID1758470 | Inhibition of human recombinant HDAC10 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1227024 | Half life in patient serum at 400 mg single dose | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID732871 | Inhibition of HDAC2 in human MDA-MB-231 cells assessed as decrease in acetylation levels of histone H4 at 1 uM by Western blot analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID411260 | Cytotoxicity against human DU145 cells after 72 hrs by trypan blue exclusion assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1165117 | Inhibition of HDAC6 in human LNCAP cells assessed as tubulin acetylation by Western blot analysis | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1901156 | Inhibition 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 assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1280275 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID246069 | Effective Concentration of compound to inhibit the growth of human SNB-78 cells | 2005 | Journal 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. |
AID1576454 | Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID269917 | Selectivity index, EC50 for histone H4 acetylation/EC50 for alpha-tubulin acetylation in HCT116 cells | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16 | Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID1126980 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1917528 | Inhibition of PI3Kdelta (unknown origin) measured by ADP-Glo assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID1633435 | Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of N-myc mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis | 2019 | ACS 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. |
AID616004 | Inhibition of HDAC4 using Boc-Lys(TFA)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID440820 | Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. |
AID1466061 | Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1765324 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1129004 | Inhibition of human HDAC-2 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1863438 | Inhibition of HDAC6 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1126958 | Inhibition of HDAC in human HeLa nuclear extracts using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2014 | Journal 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. |
AID1469380 | Inhibition of HDAC1 (unknown origin) | 2018 | Journal 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 |
AID1234895 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1614123 | Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay | |||
AID488235 | Inhibition of HDAC in human SCC4 cells assessed as increase in tubulin acetylation at 1 uM after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID1751993 | Selectivity ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1421916 | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID748982 | Inhibition of HDAC4 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID350724 | Ratio of GI50 for human MKN45 cells to IC50 for human recombinant HDAC2 | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1486307 | Antiproliferative activity against human HCC1937 cells after 3 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1275643 | Growth inhibition of human MDA-MB-231 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID732877 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1548269 | Inhibition 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 | |||
AID1514608 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID511066 | Inhibition of HDAC6 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID732145 | Inhibition of HDAC3 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1164775 | Stability of the compound in aqueous solution at pH 1.2 after 24 hrs | 2014 | Journal 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. |
AID1466056 | Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1623536 | Selectivity index, ratio of IC50 for human recombinant HDAC7 to IC50 for human recombinant HDAC6 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1127000 | Induction 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%) | 2014 | Journal 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. |
AID1486674 | Inhibition 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 analysis | 2017 | Bioorganic & 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. |
AID663337 | Growth inhibition of human OVCAR3 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID748984 | Inhibition of HDAC2 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1543967 | Induction 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 assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1742661 | Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1898919 | Inhibition of POLA1 in human NCI-H460 cells at 7.4 uM assessed as upregulation of p21 expression and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1273876 | Inhibition of human CYP1A2 using 3-cyano-7-ethoxycoumarin as substrate at 10 uM after 15 mins by fluorimetric analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID473032 | Ex vivo inhibition of human HDAC7 in human Caco-2 cells by fluorometric cellular activity assay | 2010 | Journal 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. |
AID420654 | Toxicity 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 weeks | 2009 | European 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. |
AID717818 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1518810 | Effect 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 analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID443647 | Binding affinity to pyridoxal-5'-phosphate assessed as formation of syn- and anti-PLP-aldoxime by NMR spectroscopy | 2009 | Journal 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. |
AID1141777 | Induction of apoptosis in human HCT116 cells assessed as accumulation at sub-G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal 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. |
AID489914 | Cytotoxicity against human U251 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13 | Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity. |
AID1280272 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1742179 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID616003 | Inhibition 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 assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID760377 | Cytotoxicity against human Jurkat cells after 72 hrs by MTS assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1478585 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID526534 | Growth inhibition of human ACHN cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1263142 | Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID1371076 | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID411258 | Cytotoxicity against human SKMES1 cells after 72 hrs by trypan blue exclusion assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1361633 | Inhibition of HDAC3 (unknown origin) after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID1742178 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1737155 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1330925 | Inhibition of HER2 (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis | 2017 | Bioorganic & 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. |
AID1383999 | Inhibition 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 analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1667082 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1742656 | Cytotoxicity against human Bcap37 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID440821 | Inhibition of human recombinant N-terminal FLAG-tagged HDAC4 (612-1034) expressed in baculovirus after 10 mins by fluorimetric analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. |
AID1246522 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability | 2015 | Bioorganic & 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. |
AID1469374 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID1548262 | Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay | |||
AID1650412 | Inhibition of recombinant human HDAC2 | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID347867 | Growth inhibition of human lung cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1811394 | Antitumor 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 days | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID1826627 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1873413 | Inhibition of HDAC3 (unknown origin) preincubated for 120 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID482946 | Inhibition of HDAC6 | 2010 | Bioorganic & 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. |
AID1622902 | Cytotoxicity against human K562 cells after 72 hrs by CellTiter-Glo assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1550120 | Induction 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%) | 2019 | Journal 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. |
AID1279128 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID1266839 | Activation of p53 in human HCT116 cell at 0.1 to 5 uM after 12 hrs by western blot analysis | 2015 | Journal 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. |
AID1861250 | Inhibition of PARP-1 derived from human HeLa cell nucleus | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1164172 | Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by trypan blue dye exclusion method | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1231813 | Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1401480 | Selectivity ratio of IC50 for HDAC6 in human HeLa-S3 cell lysates to IC50 for HDAC3 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID481573 | Cytotoxicity against mouse S180 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1055716 | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1515905 | Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1821272 | Inhibition of HDAC3 (unknown origin) incubated for 30 mins by microplate reader assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1647331 | Anti-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 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1709347 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1865299 | Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on heart at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID297476 | Cytotoxicity against human NCI H460 cells | 2007 | Journal 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. |
AID1129786 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1231807 | Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | 2015 | Bioorganic & 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. |
AID1355731 | Protection against spleen enlargement in SCID mouse xenografted with human HEL cells at 10 mg/kg, ip qd | 2018 | Journal 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. |
AID1667096 | Cell 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 %) | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1548284 | Induction 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%) | |||
AID313732 | Inhibition of HDAC4 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID1441631 | Inhibition 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 analysis | 2017 | Journal 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. |
AID672022 | Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis | 2012 | Bioorganic & 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. |
AID1486295 | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID723425 | Potentiation 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 assay | 2013 | Journal 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. |
AID1164024 | Inhibition of human recombinant HDAC1 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1421627 | Antiproliferative activity against human KMS-12-BM cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1422516 | Inhibition of HDAC in MEF assessed as increase in histone H4K5 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1437240 | Inhibition of HDAC1 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID1129770 | Inhibition 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 control | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1572349 | Inhibition 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 control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1888581 | Inhibition 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 | |||
AID1274878 | Inhibition of HDAC8 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID655477 | Inhibition of recombinant human HDAC2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1537557 | Antiproliferative activity against human CHP134 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1266093 | Inhibition of HDAC2 (unknown origin) by fluorimetric assay | 2016 | Bioorganic & 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. |
AID775832 | Inhibition 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 control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1206768 | Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect S9 cells after 30 mins by fluorescence assay | 2015 | Journal 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. |
AID1514609 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID90359 | Concentration required for inhibition of histone deacetylase HD2 in vitro. | 2004 | Journal 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. |
AID316876 | Inhibition of human SQ20B cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1821964 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | |||
AID1769648 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1398800 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1421903 | Antiplasmodial activity against multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1832687 | Inhibition 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 | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1811370 | Inhibition 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID1890335 | Stability in human liver microsomes assessed as clearance and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1246516 | Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID525027 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID663380 | Growth inhibition of human M14 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1352483 | Inhibition of HDAC6 in human HeLa cells after 72 hrs by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID1832801 | Inhibition of human recombinant HDAC1 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader | 2021 | Journal 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. |
AID631669 | Inhibition of human recombinant full-length HDAC6 using fluorophore conjugated substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). |
AID434538 | Cytotoxicity against human H460 cells after 24 hrs by sulforhodamine B assay | 2009 | Bioorganic & 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. |
AID663382 | Growth inhibition of human SK-MEL-2 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1205627 | Growth inhibition of human PC3 cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID482975 | Antitumor activity against human HCT116 cells xenografted in BALB/c mouse at 200 mg/kg, po after 21 days | 2010 | Bioorganic & 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. |
AID711158 | Inhibition of HDAC2 by fluorometric assay | 2012 | Journal 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. |
AID1227047 | Cytotoxicity against human HH cells assessed as cell proliferation after 70 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1861327 | Inhibition of HDAC in human OCILY3 cells assessed as effect on total Stat3 levels at 2.5 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID316885 | Antiproliferative activity against human A549 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1690104 | Growth inhibition of human NCI-H1975 cells incubated for 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID288451 | Growth inhibition of PC3 cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID316880 | Inhibition of mouse liver HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID274073 | AUC after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1720096 | Inhibition of HDAC (unknown origin) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID619041 | Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay | 2011 | Journal 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. |
AID1548291 | Induction 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%) | |||
AID473185 | Induction of P21WAF1 gene expression in human Caco-2 cells at 5 uM after 24 hrs by Western blotting | 2010 | Journal 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. |
AID540211 | Fraction unbound in human after iv administration | 2008 | Drug 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. |
AID1478591 | Inhibition of HDAC1 (unknown origin) using substrate after 30 mins by fluorometric analysis | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1164781 | Inhibition of HDAC2 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1688025 | Inhibition 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 | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1826600 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1129011 | Inhibition of human HDAC-9 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1205633 | Induction 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 TSA | 2015 | Journal 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. |
AID1537567 | Cell 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 %) | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1876339 | Cytotoxicity against human MRC9 cells assessed as cell viability incubated for 72 hrs by Cell titer- blue assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID1898497 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2021 | Journal 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. |
AID1515881 | Induction 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%) | 2019 | Journal 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. |
AID343687 | Inhibition of recombinant HDAC1 expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles. |
AID1599774 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1535345 | Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay | 2019 | Bioorganic & 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. |
AID1127323 | Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID420502 | Inhibition of HDAC2 in human HeLa cells | 2009 | European 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. |
AID1614195 | Induction 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%) | |||
AID1164786 | Inhibition of HDAC11 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1812439 | Inhibition of human HDAC using human HeLa cell nuclear extract measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID84275 | Antiproliferative activity against human HT1080 fibrosarcoma cell line | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. |
AID481547 | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1742185 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID449261 | Antiproliferative activity against human HCT116 cells after 2 days by MTT assay | 2009 | European 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. |
AID765384 | Inhibition of recombinant human HDAC10 enzyme using tetrapeptide Ac-ArgThr-Lys(Ac)Lys(Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID1250656 | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay | 2015 | Journal 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. |
AID1164180 | Induction of apoptosis in human U937 cells using annexin-V/PI staining after 48 hrs by flow cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1431820 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1897372 | Inhibition of FGFR4 (unknown origin) | |||
AID382344 | Viability of human DU145 cells after 72 hrs by MTS assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group. |
AID274074 | Oral bioavailability after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1390017 | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay | 2018 | Bioorganic & 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. |
AID1441640 | Anti-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 based | 2017 | Journal 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. |
AID725667 | Inhibition 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 afte | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
AID652765 | Induction of CFTR deltaF508 mutant mRNA expression in cystic fibrosis patient lung cells relative to control | 2011 | ACS 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. |
AID1727730 | Inhibition of HDAC6 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1873392 | Antiproliferative activity against human MV4-11 cells | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1518784 | Antiproliferative activity against human KMS-12-BM cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1655790 | Inhibition of human recombinant HDAC4 using AMC-K(TFA)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID328832 | Toxicity in ip dosed BALB/c mouse assessed as maximum tolerated dose | 2008 | Journal 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. |
AID1518785 | Antiproliferative activity against human NCI-H929 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1848322 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID1897398 | Induction 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%) | |||
AID1274881 | Inhibition of HDAC11 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID329915 | Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay | 2008 | Bioorganic & 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. |
AID1821267 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID747266 | Growth inhibition of human HeLa cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1384229 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID297497 | Cytotoxicity against human K562 cells | 2007 | Journal 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. |
AID1752940 | Antiplasmodial 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 | |||
AID1633422 | Inhibition 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 analysis | 2019 | ACS 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. |
AID1227032 | Inhibition of human recombinant HDAC6 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1915563 | Inhibition of human HDAC2 incubated for 30 mins by SpectraMax M2 microplate reader analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID603543 | Inhibition of HDAC6 in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader | 2011 | Journal 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. |
AID90671 | Inhibitory activity afgainst maize Histone deacetylase 1-A | 2003 | Journal 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. |
AID1545817 | Antiproliferative activity against human MCF7 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1633437 | Immunomodulatory 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 analysis | 2019 | ACS 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. |
AID1754777 | Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl3 gene expression at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1742668 | Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID732873 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID723118 | Potentiation 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 assay | 2013 | Journal 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. |
AID417069 | Activation 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 assay | 2009 | Bioorganic & 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. |
AID1518781 | Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1742667 | Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1623529 | Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1742759 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1281852 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1139707 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives. |
AID1231809 | Inhibition of recombinant HDAC8 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | 2015 | Bioorganic & 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. |
AID723428 | Potentiation 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 assay | 2013 | Journal 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. |
AID1819515 | Antiproliferative activity against HEL cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID1129793 | Induction 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1449214 | Inhibition 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 assay | 2017 | Journal 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. |
AID1548245 | Inhibition 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 | |||
AID1578155 | Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1547344 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1339586 | Growth inhibition of human MOLM13 cells after 44 hrs by MTT assay | 2017 | ACS 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. |
AID1754773 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID723446 | Potentiation 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 assay | 2013 | Journal 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. |
AID1348933 | Upregulation of TIMP3 gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1355715 | Synergistic antifungal activity against FLC resistant Candida albicans 100 assessed as FIC index after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID717806 | Inhibition of HDAC1 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1296349 | Inhibition 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 assay | 2016 | Journal 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. |
AID1537561 | Antiproliferative activity against human G55T2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID759301 | Cytotoxicity against human MCF7 cells expressing ERalpha and ERbeta assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID670099 | Antitumor activity against human A549 cells xenografted in nude mouse assessed as time to end point at 200 mg/kg, po administered QD till end point | 2012 | Journal 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. |
AID1200975 | Intrinsic clearance in human liver microsomes at 1 uM preincubated for 10 mins followed by NADPH addition measured over 30 mins by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1888406 | Synergistic antifungal activity against azole-resistant Candida albicans 0304103 assessed as fractional inhibitory concentration incubated for 48 hrs by CLSI based checkerboard microdilution assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID1348915 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1578917 | Inhibition 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 analysis | 2019 | Journal 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. |
AID302099 | Antiproliferative activity against H661 cells after 48 hrs | 2007 | Bioorganic & 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. |
AID603536 | Cytotoxicity against human ES2 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1126998 | Induction 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%) | 2014 | Journal 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. |
AID1563943 | Inhibition of recombinant HDAC6 (unknown origin) measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. |
AID1864240 | Inhibition of HDAC in human MDA-MB-231 cells incubated for 45 mins by luminescence assay | 2022 | Journal 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. |
AID1422513 | Inhibition of HDAC in MEF assessed as increase in histone H3K9 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1170746 | Inhibition of human recombinant HDAC11 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1282254 | Cytotoxicity against human Ramos cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1548729 | Inhibition 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 analysis | 2020 | Journal 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. |
AID1697202 | Inhibition of HDAC6 (unknown origin) | 2020 | Bioorganic & 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. |
AID289928 | Antiproliferative activity against human H661 cells after 48 hrs | 2007 | Bioorganic & 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. |
AID343688 | Inhibition of recombinant HDAC6 expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles. |
AID300836 | Growth inhibition of human MDA-MB-231 cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID1511133 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1821273 | Inhibition of HDAC6 (unknown origin) incubated for 30 mins by microplate reader assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1622960 | Inhibition of HDAC1 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1731760 | Metabolic 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 analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates. |
AID1401476 | Selectivity ratio of IC50 for HDAC3 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1599730 | Cytotoxicity against human ADCA72 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1865267 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1326516 | Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated alpha-tubulin after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID747268 | Inhibition of human recombinant HDAC7 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1409640 | Inhibition of HDAC in human HeLa cells using Boc-K(Ac)-AMC as substrate by fluorescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy. |
AID1785346 | Inhibition 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 | |||
AID1250655 | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay | 2015 | Journal 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. |
AID1266810 | Antiproliferative activity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1591856 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID1869146 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | |||
AID674000 | Growth inhibition of human HeLa cells after 72 hrs by XTT assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1451832 | Inhibition 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 assay | 2017 | Journal 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. |
AID1576466 | Induction 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%) | |||
AID274015 | Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) | 2007 | Bioorganic & 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. |
AID1401534 | Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID499800 | Inhibition of HDAC8 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1462217 | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1887682 | Cytotoxicity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID329920 | Induction of granulocytic differentiation in human U937 cells | 2008 | Bioorganic & 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. |
AID546547 | Inhibition of human recombinant HDAC1 expressed in HEK293 cells | 2010 | Journal 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. |
AID90685 | Inhibition of Histone deacetylase 2 (HDAC2) activity of HeLa nuclear extracts | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1449324 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1890328 | Induction of apoptosis in mouse CT26 cells assessed as apoptotic cells at 6 uM measured by Annexin V-FITC/PI staining based flow cytometry method | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID373073 | Inhibition of HDAC from human HeLa cells | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID465152 | Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1482118 | Cytotoxicity against human COLO205 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1129800 | Induction 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1162486 | Growth inhibition of human PC3 cells after 72 hrs by CellTiter Glo assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents. |
AID1566037 | Inhibition 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 b | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID316931 | Inhibition of HDAC3 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1441670 | Anti-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 7 | 2017 | Journal 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. |
AID496806 | Inhibition of human HDAC6 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID723126 | Potentiation 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 assay | 2013 | Journal 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. |
AID1164184 | Inhibition of human recombinant HDAC6 using Z-MAL as substrate at 5 uM after 1 hr by fluorescent activity assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1380946 | Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1164038 | Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1225986 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID316896 | Inhibition of human HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1898925 | Antiproliferative activity against human NCI-H460 cells at 7.4 uM assessed as reduction in PIN1 level and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1339584 | Growth inhibition of human Jurkat cells at 1 to 10 uM after 44 hrs by MTT assay | 2017 | ACS 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. |
AID310181 | Growth inhibition of human PC3 cells by SRB assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID1502979 | Antiproliferative activity against human SW620 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID316908 | Inhibition of human St4 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID344919 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of 50 uM Fe by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID482950 | Inhibition of HDAC11 | 2010 | Bioorganic & 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. |
AID1177056 | Antiprotozoan activity against Leishmania donovani MHOM- ET-67/L82 amastigotes at 1 uM | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1614133 | Inhibition 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 | |||
AID663371 | Growth inhibition of human DU145 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1164784 | Inhibition of HDAC8 (unknown origin) using fluorogenic tetrapeptide RHK(Ac)K(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1901228 | Half life in dog liver microsomes by LC-MS/MS analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID90681 | Inhibition of mouse HDAC1 | 2004 | Journal 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. |
AID1742662 | Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID604039 | Inhibition of histone acetyltransferase in human MCF7 cells assessed as increase of alpha-tubulin acetylation level at 5 uM after 15 mins by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). |
AID732146 | Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID228859 | Activity in histone hyperacetylation assay in cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1250657 | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay | 2015 | Journal 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. |
AID1464877 | Anti-proliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1763817 | Antiproliferative activity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID1819545 | Antitumor 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 control | 2022 | Journal 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. |
AID605298 | Inhibition of HDAC in human HeLa cells nuclear extract using fluor de Lys as substrate preincubated for 5 mins by fluorometric analysis | 2010 | Journal 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. |
AID1676591 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID723445 | Potentiation 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 assay | 2013 | Journal 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. |
AID1403159 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1296347 | Inhibition 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 assay | 2016 | Journal 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. |
AID1482119 | Cytotoxicity against human Caco2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1225978 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1260656 | Binding affinity to human recombinant HDAC8 by fluorescence assay | |||
AID1737149 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1848320 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID1614230 | Induction 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%) | |||
AID1737134 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID353355 | Inhibition of HDAC in human SHSY5Y cells at 10 uM by fluorimetric cellular activity assay | 2009 | Journal 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. |
AID1401536 | Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1622935 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1361626 | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1275645 | Growth inhibition of human PC3 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID373078 | Inhibition of human recombinant HDAC5 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1174687 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1473738 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID525018 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in mutant Fdelta508 CFTR protein level at 5 uM after 4 hrs by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1821323 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1164195 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1348921 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID465149 | Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1547345 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1129013 | Inhibition of human HDAC-11 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID663404 | Half life in artificial intestinal fluid | 2012 | Journal 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. |
AID1441650 | Anti-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 ELISA | 2017 | Journal 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. |
AID1859933 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1067347 | Inhibition of HDAC1/2 in human HeLa cell extracts using acetylated histone peptide as substrate after 30 mins | 2014 | Bioorganic & 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. |
AID1864676 | Inhibition 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 | |||
AID1578883 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2019 | Journal 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. |
AID488277 | Inhibition of HDAC8 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | On the inhibition of histone deacetylase 8. |
AID1126976 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1754772 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1174681 | Antiproliferative activity against human U266 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1294804 | Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate at 0.5 uM by fluorometric assay | 2016 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10 | A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors. |
AID604081 | Inhibition of JMJD2E pre-incubated for 30 mins | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Inhibitors of histone demethylases. |
AID1415648 | Inhibition of HDAC3 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1542182 | Inhibition of HDAC4 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1785352 | Synergistic antiproliferative activity against human A549 cells assessed as combination index in presence of palbociclib by Chou-Talalay method | |||
AID1865243 | Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID544093 | Antimalarial activity against drug-resistant Plasmodium falciparum TM90C2A | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID652753 | Inhibition of recombinant human HDAC9 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1155322 | Selectivity index, ratio of IC50 for erythrocytes (unknown origin) to IC50 for Plasmodium falciparum | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1250647 | Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1434362 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1882466 | Inhibition of HDAC3 (unknown origin) | 2022 | Journal 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. |
AID1336933 | Inhibition of HDAC6 in human LNCAP cells assessed as acetylated tubulin accumulation in cytosol at 10 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID663392 | Growth inhibition of human TK10 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID525025 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 0.1 uM by RT-PCR | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID476834 | Toxicity in FVB mouse assessed as effect on hematocrit at 50 mg/kg, po administered 5 times per week for 2 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1739582 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID274036 | Hepatocyte stability | 2007 | Bioorganic & 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. |
AID476642 | Antiproliferative activity against human HT-29 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1469334 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID622255 | Inhibition of HDAC1 after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1676597 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1251317 | Inhibition of HDAC6 (unknown origin) | 2015 | Bioorganic & 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. |
AID1566805 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1164185 | Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate after 1 hr by fluorescent activity assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1887684 | Cytotoxicity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID329917 | Induction of alpha tubulin hyperacetylation in human U937 cells | 2008 | Bioorganic & 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. |
AID1578887 | Inhibition of human HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2019 | Journal 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. |
AID1751985 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID445135 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID1352479 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID1832796 | Cytotoxicity against human HL-60 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay | 2021 | Journal 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. |
AID1890350 | Selectivity ratio of IC50 for recombinant human HDAC1 over IC50 for recombinant human HDAC6 | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID672030 | Selectivity ratio of IC50 for human HDAC2 preincubated with compound for 3 hrs to IC50 for human HDAC1 preincubated with compound for 3 hrs | 2012 | Bioorganic & 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. |
AID1633434 | Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of MAP-2 mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis | 2019 | ACS 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. |
AID748983 | Inhibition of HDAC1 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1441703 | Anti-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 microsc | 2017 | Journal 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. |
AID1742222 | Tmax in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1821338 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID622254 | Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1355096 | Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay | |||
AID1886184 | Inhibition of HDAC2 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay | 2022 | Journal 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. |
AID1742669 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID274068 | Oral bioavailability after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1421913 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1566822 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1487006 | Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC3 (unknown origin) | 2017 | Bioorganic & 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. |
AID1754775 | Induction of apoptosis in human MCF7 cells assessed as increase in caspase 3/7 activity at 1 to 3 uM measured after 48 hrs by ELISA | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1816189 | Inhibition of recombinant HDAC4 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | |||
AID1263060 | Inhibition of NTHi-induced NF-kappaB activation in human BEAS-2B cells treated 1 hr before NTHi stimulation measured after 5 hrs by luciferase assay | 2015 | Bioorganic & 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. |
AID1702141 | Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin at Lys40 residue incubated for 3 hrs by ELISA | 2018 | Journal 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. |
AID1404300 | Antiproliferative activity against human SK-MEL-28 cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1396989 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors. |
AID1231814 | Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID755622 | Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID1754769 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1164035 | Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1742650 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID717826 | Inhibition of HDAC1 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1754762 | Downregulation of HDAC4 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1263146 | Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID481549 | Cytotoxicity against human HO8910 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1352482 | Inhibition of HDAC4 in human HeLa cells after 72 hrs by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID1652192 | Inhibition 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 assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1861652 | Cytotoxicity against human L02 cells measured after 72 hrs | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1826612 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1164033 | Inhibition of human recombinant HDAC10 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1563944 | Inhibition of recombinant HDAC8 (unknown origin) measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. |
AID618083 | Toxicity 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 19 | 2011 | Journal 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. |
AID1326526 | Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as tumor growth inhibition at 200 mg/kg, po qd | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1398815 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1821266 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1380952 | Inhibition of HDAC1 (unknown origin) using fluorogenic substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | 2018 | Journal 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. |
AID1464878 | Anti-proliferative activity against human MRC5 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID652748 | Inhibition of recombinant human HDAC4 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1702092 | Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis | 2018 | Journal 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. |
AID765383 | Inhibition of recombinant human HDAC11 enzyme using Ac-LeuGlyLys(Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID609496 | Cardiac safety index, Ratio of IC50 for human ERG to IC50 for human HCT116 cells | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1454054 | Growth inhibition of human MDA-MB-231 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID322414 | Antiproliferative activity against human LNCap by MTT assay | 2008 | Bioorganic & 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. |
AID1246512 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1401906 | Selectivity ratio of IC50 for human recombinant HDAC2 to IC50 for human recombinant HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID316903 | Inhibition of human HCT116 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1699972 | Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2020 | Bioorganic & 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. |
AID1126994 | Induction 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%) | 2014 | Journal 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. |
AID1864270 | Antitumor 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 days | 2022 | Journal 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. |
AID732449 | Inhibition of human U937 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID737915 | Inhibition of recombinant HDAC6 (unknown origin) after 10 mins by fluorimetric analysis | 2013 | Journal 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. |
AID1751987 | Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1542180 | Inhibition of HDAC2 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1269323 | Cytotoxicity against human U251MG cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID711146 | Inhibition of HDAC8 at 0.3 uM in absence of Cu(I) by fluorometric assay | 2012 | Journal 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. |
AID759300 | Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1752946 | Antiplasmodial 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 | |||
AID760512 | Inhibition of HDAC1 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID411254 | Inhibition of HDAC8 from human HeLa cells nuclear extract by cell free fluorimetric assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1816223 | Induction 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%) | |||
AID350721 | Growth inhibition of human MKN45 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID663361 | Growth inhibition of human KM12 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1459946 | Antiproliferative activity against human A549 cells measured after 48 hrs by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1548265 | Induction of apoptosis in human RPMI8226 cells incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry | |||
AID1550121 | Induction 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%) | 2019 | Journal 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. |
AID748107 | Inhibition of HDAC9 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1754754 | Inhibition 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 anal | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID628451 | Inhibition of HDAC in human HepG2 cells assessed as increase in histone H4 acetylation at 1 to 10 uM after 24 hrs by Western blot analysis | 2011 | Journal 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. |
AID1246520 | Cytotoxicity against human THP1 cells assessed as reduction in cell viability | 2015 | Bioorganic & 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. |
AID1550104 | Inhibition 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 analysis | 2019 | Journal 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. |
AID1441688 | Anti-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 ELISA | 2017 | Journal 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. |
AID1246511 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1764251 | Inhibition 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 fluorimetry | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID461266 | Antiproliferative activity against human LNCAP cells | 2010 | Journal 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. |
AID1178595 | Inhibition of human HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID503663 | Effect on FXN mRNA expression in human GM15850 cells at 5 uM after 12 hrs by qRT-PCR analysis | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1469395 | Induction 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%) | 2018 | Journal 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 |
AID1566038 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID1233268 | Therapeutic index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells | 2015 | Journal 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. |
AID1293566 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1775548 | Inhibition of HDAC6 (unknown origin) | 2021 | Journal 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 |
AID628449 | Induction of apoptosis in human HepG2 cells assessed as hyperacetylation of p53 at 1 to 10 uM by Western blot analysis | 2011 | Journal 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. |
AID775830 | Inhibition 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 analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1129776 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1578882 | Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay | 2019 | Journal 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. |
AID663372 | Growth inhibition of human SF268 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1355744 | In 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) | 2018 | Journal 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. |
AID541645 | Inhibition of human HDAC2 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID373075 | Inhibition of human recombinant HDAC2 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1273879 | Inhibition of human CYP3A4 using 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate at 10 uM after 30 mins by fluorimetric analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID613327 | Antitumor activity against human HCT116 cells xenografted in athymic nude mouse model assessed as tumor growth inhibition at 5 mg/kg, iv | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1614136 | Inhibition 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 | |||
AID1865295 | Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID652759 | Increase of HDAC7-meidated histone H3 acetylation in human CFBE41o cells at 0.2 to 5 uM by Western blot analysis | 2011 | ACS 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. |
AID1174688 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID420504 | Antiproliferative activity against human HCT116 cells after 72 hrs | 2009 | European 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. |
AID1633674 | Immunomodulatory 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 analysis | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1321621 | Antiproliferative activity against human A549 cells measured after 72 hrs by WST1 assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy. |
AID1433255 | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1141766 | Cytotoxicity against human HSC3 cells by MTT assay | 2014 | Journal 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. |
AID1406993 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1476160 | Antiproliferative activity against human NKYS cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1469300 | Induction 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%) | 2018 | Journal 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 |
AID1688033 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1826621 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID524997 | Inhibition of HDAC7 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1486298 | Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1126982 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1547354 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1462227 | Inhibition of BRD4/HDAC1 in human OCI-AML2 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & 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. |
AID525034 | In vivo inhibition of HDAC | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1206742 | Cytotoxicity against human MDA cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1280259 | Inhibition of human HDAC1 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID723437 | Potentiation 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 assay | 2013 | Journal 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. |
AID404445 | Cytotoxicity against human SU 86.86 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID90340 | Inhibition of Histone deacetylase (HDAC)of HeLa nuclear extracts | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1398804 | Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1441668 | Plasma concentration in mouse by liquid chromatography mass spectrometry | 2017 | Journal 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. |
AID1885700 | Toxicity in ICR mouse assessed as effect on ALT level at 12 umol/kg, ip measured after 12 hrs in presence of CDDO-Me | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy. |
AID1888421 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID374819 | Inhibition of wild type His-tagged HDAC5 catalytic domain T678-L1122 expressed in Escherichia coli | 2009 | Journal 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. |
AID1390810 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
AID527320 | Growth inhibition of human U937 cells after 72 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases. |
AID750110 | Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate at 1 uM by fluorescence assay | 2013 | Bioorganic & 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. |
AID1482142 | Induction 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%) | 2017 | Journal 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. |
AID1727742 | Inhibition of HDAC8 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1464886 | Oral bioavailability in Sprague-Dawley rat 20 mg/kg administered via gavage by LC-MS/MS analysis | 2017 | Bioorganic & 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. |
AID1578919 | Inhibition 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 analysis | 2019 | Journal 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. |
AID476645 | Antiproliferative activity against human HL60 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1164766 | Efflux ratio of permeability from apical to basolateral side to basolateral to apical side of human Caco2 cells in presence of digoxin | 2014 | Journal 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. |
AID1578494 | Induction 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 %) | 2020 | ACS 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. |
AID1422519 | Inhibition of human recombinant HDAC1 at 2 uM after 15 to 30 mins by COLOR DE LYS-based colorimetric method | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1572341 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID619139 | Half life in dog liver microsomes | 2011 | Journal 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. |
AID352517 | Inhibition of human recombinant HDAC3 | 2009 | Bioorganic & 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. |
AID1511967 | Inhibition 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 assay | 2019 | ACS 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. |
AID1566813 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID313731 | Inhibition of HDAC3 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID1164774 | Toxicity 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 weeks | 2014 | Journal 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. |
AID1864679 | Inhibition 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 | |||
AID764218 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1433253 | Antiproliferative activity against human CMY cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1434356 | Growth inhibition of human HCT15 cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1566806 | Inhibition of recombinant full length human HDAC4 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1502986 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1737136 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1434352 | Inhibition of HDAC in human HeLa cell nuclear extract using acetylated lysine side chain of histone as substrate measured after 30 mins by fluorometric assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1141242 | Inhibition of pig kidney microsomal APN using L-Leu-p-nitroanilide as substrate preincubated for 5 mins before substrate addition measured after 30 mins by spectrophotometry | 2014 | Bioorganic & 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. |
AID1783063 | Antifungal activity against fluconazole-resistant Candida tropicalis 3890 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1754759 | Downregulation of HDAC2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID593551 | Inhibition of human HDAC6 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID541654 | Inhibition of human HDAC11 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1234898 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1260637 | Inhibition of human recombinant HDAC1 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1401545 | Antiproliferative activity against human KM-H2 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1600657 | Inhibition 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 m | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID1784989 | Inhibition of HDAC6 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1848278 | Inhibition of PI3Kalpha (unknown origin) at 1 uM by mobility shift assay | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID755620 | Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID1518806 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1587865 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1449332 | Inhibition of HDAC6 in human CAL27 cells assessed as accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1861257 | Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1473739 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID1511140 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID461260 | Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1758462 | Dark toxicity in human A549 cells assessed as reduction in cell viability incubated under dark for 48 hrs measured after 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1394887 | Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) after 3 hrs by fluorescence polarization assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1599729 | Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1667069 | Antiproliferative activity in human A549 cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID487873 | Inhibition of HDAC in human HeLa cells extracts after 60 mins by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | New aryldithiolethione derivatives as potent histone deacetylase inhibitors. |
AID1421927 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1849159 | Selectivity 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 | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1754770 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1548276 | Antiproliferative 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 | |||
AID1281866 | Induction 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%) | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1469437 | Inhibition of HDAC1 in human Hep3B cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot method | 2018 | Journal 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 |
AID1821344 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1543960 | Induction 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%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1676588 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1785338 | Inhibition of HDAC7 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | |||
AID1225983 | Inhibition 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 assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1361650 | Induction 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%) | 2018 | Journal 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. |
AID663374 | Growth inhibition of human SF539 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID292436 | Inhibition of HDAC in HeLa cells | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Trithiocarbonates: exploration of a new head group for HDAC inhibitors. |
AID1356280 | Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay | |||
AID1263145 | Inhibition of human recombinant HDAC6 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID1441680 | Anti-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) | 2017 | Journal 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. |
AID1355707 | Antifungal activity against FLC resistant Candida albicans 0304103 after 48 hrs in presence of fluconazol by checkerboard microdilution method | 2018 | Journal 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. |
AID663393 | Growth inhibition of human UO31 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1514601 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID652763 | Inhibition of HDAC6 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID350732 | Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1201653 | Antiproliferative activity against human OVCAR5 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1816195 | Inhibition 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 | |||
AID1819549 | Antitumor 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 control | 2022 | Journal 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. |
AID1915578 | Inhibition of VEGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID71776 | Tested in vivo for the inhibition of proliferation of friend leukemic cells | 2002 | Journal 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. |
AID482967 | Volume of distribution at steady state in mouse at 10 mg/kg, iv | 2010 | Bioorganic & 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. |
AID527042 | Cytotoxicity against human NCI-H460 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1897506 | Antiangiogenic 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 | |||
AID593552 | Inhibition of human HDAC7 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1754778 | Downregulation of NFkB1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1890438 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay | 2022 | Bioorganic & medicinal chemistry, 04-15, Volume: 60 | Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones. |
AID1273872 | Inhibition of HDAC6 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1487016 | Inhibition of HDAC2 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method | 2017 | Bioorganic & 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. |
AID1482141 | Induction 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%) | 2017 | Journal 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. |
AID541655 | Growth inhibition of human H460 cells after 48 hrs by SRB assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID273179 | Induction of apoptosis in U937 cells at 5 uM by AnnexinV/PI double staining | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1901173 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1917531 | Selectivity index, ratio IC50 for inhibition of HDAC6 (unknown origin) to IC50 for inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID780576 | Growth inhibition of human MCF7 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors. |
AID411255 | Selectivity for ratio of IC50 for human HDAC8 to IC50 for human HDAC1/2 by fluorimetric assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID663345 | Growth inhibition of human HL-60(TB) cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1361652 | Induction 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%) | 2018 | Journal 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. |
AID1572357 | Induction of apoptosis in human MDA-MB-231 cells at 1 to 10 uM after 48 hrs by propidium iodide-staining based FACS analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1898526 | Cytotoxicity against human L02 cells assessed as reduction in cell viability at 32 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Journal 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. |
AID1363818 | Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID1630597 | Inhibition of recombinant full length C-terminal FLAG-tagged/C-terminal His-tagged human HDAC1 using fluorogenic substrate at 10 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID310123 | Inhibition of HDAC2 in HeLa cell lysates | 2007 | Bioorganic & 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. |
AID1415671 | Half life in rat liver microsomes at 5 uM in presence of NADPH by LC-MS analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1863440 | Inhibition of HDAC8 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID241474 | Inhibitory concentration against maize histone deacetylase 2 | 2005 | Journal 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. |
AID723426 | Potentiation 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 assay | 2013 | Journal 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. |
AID1177054 | Antiprotozoan activity against Giardia lamblia G1 | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1886185 | Inhibition of HDAC3 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay | 2022 | Journal 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. |
AID1487014 | Inhibition of HDAC6 in human U937 cells assessed as increase in acetylated-alpha-tubulin level at 5 uM incubated for 18 hrs by Western blot method | 2017 | Bioorganic & 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. |
AID1759727 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction. |
AID1403156 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID723123 | Potentiation 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 assay | 2013 | Journal 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. |
AID240810 | Inhibitory concentration against human histone deacetylase | 2005 | Journal 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. |
AID1421909 | Selectivity index, ratio of IC50 for human HepG2A16 cells to IC50 for drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID708770 | Inhibition of HDAC in human HeLa cells nuclear extracts by fluorometric assay | 2012 | Journal 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. |
AID1126986 | Inhibition of HDAC1 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal 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. |
AID525010 | Inhibition of HDAC7 in human CFBE41o- cell line assessed as increase in Fdelta508 CFTR protein trafficking at 1 uM every 24 hrs by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1415652 | Inhibition of HDAC4 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1653139 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability by SRB assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1280279 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1433250 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID371222 | Cytotoxicity against human HCT116 cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-mercaptoketone based histone deacetylase inhibitors. |
AID473175 | Induction of HDAC-mediated histone acetylation in human Caco-2 cells at 5 uM after 6 hrs by indirect ELISA | 2010 | Journal 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. |
AID1233250 | Inhibition of human recombinant HDAC1 after 15 mins by fluorogenic assay | 2015 | Journal 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. |
AID1783070 | Antifungal activity against fluconazole-sensitive Candida albicans 9770 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1897404 | Induction 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%) | |||
AID320398 | Induction of tubulin hyperacetylation in human MCF7 cells at 10 uM by Western blot | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode. |
AID1667088 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1543972 | Induction 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 assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID310183 | Growth inhibition of human NUGC3 cells by SRB assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID717805 | Inhibition of HDAC3 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1855254 | Antiproliferative activity against human HCT-116 cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID759303 | Inhibition of human recombinant HDAC8 after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID725669 | Inhibition 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 by | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
AID482952 | Antiproliferative activity against human A2780 cells | 2010 | Bioorganic & 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. |
AID1404301 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1754756 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID446348 | Hepatic blood flow in mouse | 2010 | Journal 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. |
AID1816214 | Induction 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%) | |||
AID1173507 | Inhibition of full length N-terminal GST-tagged human HDAC11 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1371051 | Antilieshmanial activity against promastigote stage of Leishmania donovani by fluorimetric assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1473741 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID1709368 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1785334 | Inhibition 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 | |||
AID327541 | Inhibition of human HDAC in HeLa cells at 1 uM | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID90839 | Inhibition of Histone deacetylase 8 (HDAC8) of HeLa nuclear extracts | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID499799 | Inhibition of HDAC in human HeLa cell nuclear extracts | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1897494 | Toxicity 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 | |||
AID1141784 | Inhibition of HDAC in human HCT116 cells assessed as increase in alpha-tubulin acetylation after 3 hrs by Western blotting analysis | 2014 | Journal 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. |
AID1215096 | Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis relative to rifampicin | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1401903 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID1631200 | Inhibition of HDAC8 (unknown origin) using fluorophore-conjugated substrate by fluorescence assay | 2016 | ACS medicinal chemistry letters, Oct-13, Volume: 7, Issue:10 | Development of a Potent and Selective HDAC8 Inhibitor. |
AID1164907 | Inhibition of HDAC2 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID663365 | Growth inhibition of human OVCAR4 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID663366 | Growth inhibition of human OVCAR5 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1811379 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth measured after 2 days by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID723440 | Potentiation 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 assay | 2013 | Journal 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. |
AID1128562 | Inhibition of human HDAC-10 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1633438 | Immunomodulatory 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 analysis | 2019 | ACS 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. |
AID308647 | Antiproliferative activity against human drug-resistant PT45 cells | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID90345 | Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1); Potent inhibitor | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | (2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors. |
AID1454031 | Inhibition 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 additio | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1410362 | Antitumor 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 control | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID374830 | Antiproliferative activity against human MCF7 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID1164921 | Induction of cell differentiation in human BE(2)-C cells assessed as neurite outgrowth at 2 uM by CCK-8 assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1168913 | Inhibition of HDAC1/HDAC2 in human HeLa cell extract incubated for 5 mins prior to substrate addition measured after 30 mins by microtitre plate reader analysis | 2014 | Bioorganic & 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. |
AID1547264 | Inhibition of HDAC10 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID591330 | Inhibition of HDAC in human HeLa cells by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors. |
AID761581 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID258011 | Inhibition of HDAC in human leukemic CEM cells | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. |
AID1322159 | Inhibition 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 assay | 2016 | Bioorganic & 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. |
AID1433270 | Inhibition of HDAC in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1476151 | Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay | 2017 | Journal 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. |
AID1275585 | Inhibition of HDAC in mouse forebrain assessed as acetylation of histone H3K9 at 10 uM after 24 hrs by immunofluorescence-based detection analysis | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. |
AID1655800 | Cytotoxicity 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 control | 2020 | ACS 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. |
AID723470 | Inhibition of HDAC in cisplatin sensitive human CAL27 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1200976 | Intrinsic clearance in mouse liver microsomes at 1 uM preincubated for 10 mins followed by NADPH addition measured over 30 mins by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID618093 | Toxicity 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 19 | 2011 | Journal 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. |
AID456797 | Antimalarial 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 method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID761577 | Induction of apoptosis in human NB4 cells after 48 hrs by Annexin V test | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID1426425 | Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID1742224 | AUC (0 to t) in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID105420 | Concentration required for the antiproliferation of Human MDA-435 breast carcinoma cells | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC). |
AID672033 | Ratio of IC50 for human HDAC2 preincubated for 3 hrs to IC50 for human HDAC2 preincubated for 5 mins | 2012 | Bioorganic & 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. |
AID1600733 | Antiproliferative activity against human CAL27 cells after 72 hrs by microplate reader based MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1462024 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. |
AID1863175 | Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID1410326 | Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID1865300 | Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on liver at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID1330924 | Inhibition of wild-type EGFR (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis | 2017 | Bioorganic & 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. |
AID1467045 | Effect 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 assay | 2017 | Journal 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. |
AID1324232 | Antagonist 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 control | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID1410324 | Inhibition of recombinant human GST-tagged IDO1 (1 to 404 residues) using D-Tryptophan as substrate | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID316902 | Inhibition of human SNB78 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1409642 | Inhibition of HDAC in human K562 cells using Boc-K(Ac)-AMC as substrate by fluorescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy. |
AID1758467 | Inhibition of human recombinant HDAC3 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID414718 | Inhibition of human recombinant HDAC6 expressed in HEK293 cells | 2009 | Journal 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. |
AID1168916 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1466057 | Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID246082 | Effective Concentration of compound to inhibit the growth of human RXF-631L cells | 2005 | Journal 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. |
AID1464879 | Inhibition of recombinant human ERG expressed in HEK293 cells at -80 mV holding potential measured for 9 mins by Qpatch clamp method | 2017 | Bioorganic & 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. |
AID1769649 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID613114 | Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Epigenetic profiling of the antitumor natural product psammaplin A and its analogues. |
AID1897401 | Induction 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%) | |||
AID1260647 | Inhibition of human recombinant HDAC11 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1784974 | Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1816697 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID669763 | Inhibition of human recombinant HDAC6 after 30 mins by fluorometric assay | 2012 | Journal 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. |
AID1361640 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1399810 | Solubility in PG/EtOH (96%) at 30 mg/mL after 24 hrs by UV-spectrometric method | 2018 | Bioorganic & 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. |
AID723456 | Potentiation of cisplatin-induced toxicity in cisplatin resistant human KYSE-510 cells at 1 uM pretreated for 48 hrs followed by cisplatin treatment by MTT assay | 2013 | Journal 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. |
AID1861306 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at G2/M phase measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1279125 | Inhibition of C-terminal GST-tagged human recombinant HDAC2 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID476652 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1600732 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1355729 | Toxicity in BALB/C nude mouse xenografted with human HEL cells at 10 mg/kg, ip bid treated for 21 consecutive days | 2018 | Journal 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. |
AID1193537 | Inhibition 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 assay | 2015 | Bioorganic & 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. |
AID737918 | Inhibition of recombinant HMG-CoA reductase (unknown origin) after 10 mins by spectrophotometric analysis | 2013 | Journal 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. |
AID1235259 | Cytotoxicity against human K562 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1730857 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1865241 | Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID1633654 | Inhibition of human recombinant HDAC6 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID672021 | Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis | 2012 | Bioorganic & 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. |
AID331899 | Displacement 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 assay | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID1225976 | Cytotoxicity against HLF assessed as growth inhibition after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1401377 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1449216 | Inhibition 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 assay | 2017 | Journal 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. |
AID613122 | Inhibition of HDAC1 in human U937 cells assessed as up-regulation of p21 / WAF1 at 5 uM after 24 hrs by Western blot analysis | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Epigenetic profiling of the antitumor natural product psammaplin A and its analogues. |
AID1493593 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID622257 | Inhibition of HDAC6 after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1451848 | Antitumor 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 control | 2017 | Journal 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. |
AID1783110 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
AID1486306 | Antiproliferative activity against human Raji cells after 3 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1511157 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1811367 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 6 days by WST8 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID1061949 | Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1622973 | Inhibition of HDAC4 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1897382 | Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID1614122 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | |||
AID1832685 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1415640 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1326509 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1459954 | Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1888405 | Synergistic 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 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID1764250 | Antiproliferative activity against human CAL-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1275646 | Growth inhibition of human Aspc-1 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug 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. |
AID1441684 | Anti-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 method | 2017 | Journal 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. |
AID1487043 | Inhibition 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 addition | 2017 | Bioorganic & 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. |
AID1650413 | Inhibition of HDAC in human A2780 cells | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID1821966 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
AID1250640 | Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID669758 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay | 2012 | Journal 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. |
AID1720109 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID1808542 | Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 cells measured after 60 mins by FRET assay | 2021 | Journal 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). |
AID723155 | Potentiation 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 assay | 2013 | Journal 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. |
AID1181305 | Inhibition of human recombinant HDAC6 pre-incubated at room temperature for 15 min before substrate addition by fluorimetric assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID544094 | Cytotoxicity against mouse RAW264.7 cells by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1478588 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1677511 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID618020 | Antitumor 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 control | 2011 | Journal 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. |
AID1855242 | Inhibition of HDAC1/HDAC2 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate and measured by fluorometric method | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID489912 | Cytotoxicity against human NCI-H460 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13 | Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity. |
AID663396 | Growth inhibition of human Hs 578T cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1361648 | Induction 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%) | 2018 | Journal 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. |
AID1389949 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1855247 | Binding affinity to calf thymus DNA at 50 uM incubated for 30 mins and measured by fluorescence spectroscopy | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID421213 | Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation at 5 uM | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID316898 | Inhibition of HDAC2 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1865264 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1410012 | Reactivation of latent HIV1 infected in human U1 cells assessed as increase in p24 production after 48 hrs by ELISA relative to vorinostat | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor. |
AID1336937 | Inhibition of HDAC in human LNCAP cells assessed as down regulation of androgen receptor expression at 10 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1578147 | Inhibition of HDAC in human K562 nuclear extract | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1065960 | Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID732152 | Inhibition of HDAC6 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1848629 | Cytotoxicity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID404446 | Cytotoxicity against nontransformed human microvascular epithelial cells | 2008 | Journal 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. |
AID619045 | Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay | 2011 | Journal 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. |
AID1652190 | Inhibition 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 assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1550108 | Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | Journal 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. |
AID420500 | Toxicity in athymic nude Swiss mouse bearing human H460 cells assessed as death administered QD 5 days a week for 2 weeks | 2009 | European 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. |
AID1202591 | Cytotoxicity against human KB cells after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID1127325 | Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID449260 | Inhibition of HDAC1/HDAC2 from human Hela nuclear extracts using [3H]acetylated histone peptide by colorimetry | 2009 | European 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. |
AID672031 | Selectivity ratio of IC50 for human HDAC2 preincubated with compound for 24 hrs to IC50 for human HDAC1 preincubated with compound for 3 hrs | 2012 | Bioorganic & 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. |
AID1753838 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID672029 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID1293553 | Inhibition of HDAC in human HeLa nuclear extract using BOC-Ac-Lys-AMC as substrate incubated for 90 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1367346 | Antiproliferative activity against human HCT116 cells by MTT assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Synthesis and biological evaluation of Santacruzamate-A based analogues. |
AID1598104 | Activation 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 cytometry | 2019 | Journal 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. |
AID503689 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID605542 | Antiproliferative activity against human MCR5-SV2 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID717797 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID723143 | Potentiation 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 assay | 2013 | Journal 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. |
AID1273869 | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1689779 | Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1292165 | Induction 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 analysis | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Novel spiropyrazolone antitumor scaffold with potent activity: Design, synthesis and structure-activity relationship. |
AID1403158 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID628440 | Inhibition of human recombinant HDAC3/NCoR2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC | 2011 | Journal 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. |
AID1389958 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1337290 | Antiproliferative activity against human KHYG cells after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID274098 | Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 90% of isolates after 24h. | 2007 | Bioorganic & 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. |
AID1248353 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID1321620 | Antiproliferative activity against human HCT116 cells measured after 72 hrs by WST1 assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy. |
AID1439781 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa. |
AID246068 | Effective Concentration of compound to inhibit the growth of human HCT116 cells | 2005 | Journal 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. |
AID1065968 | Inhibition of HDAC6 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacYGC as substrate after 60 mins by SAMDI mass spectrometric analysis | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID313735 | Inhibition of HDAC7 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID1321702 | Inhibition of HDAC3 (unknown origin) | 2016 | Journal 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. |
AID1900912 | Cytotoxicity against human TMZ-sensitive U251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID1482169 | Cytotoxicity against human COLO205 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID408886 | Selectivity for HDAC6 over HDAC1 | 2008 | Journal 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. |
AID1449328 | Inhibition of human HDAC8 using Z-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate measured after 90 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1572381 | Antiproliferative activity against human THP1 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID488274 | Inhibition of HDAC2 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | On the inhibition of histone deacetylase 8. |
AID655475 | Restoration of CFTR deltaF508 mutant trafficking to cell surface as glycoforms in human CFBE41o cells at 5 uM after 24 hrs by Western blotting | 2011 | ACS 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. |
AID274072 | Clearance after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1401478 | Selectivity 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 cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1622982 | Cytotoxicity against human RWPE1 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1441702 | Inhibition 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)- | 2017 | Journal 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. |
AID586614 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine incorporation | 2011 | Antimicrobial 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. |
AID352748 | Inhibition of C-terminal FLAG tagged HDAC3 | 2009 | Bioorganic & 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. |
AID1487047 | Inhibition of HDAC6 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1819534 | Toxicity 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 analysis | 2022 | Journal 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. |
AID1785351 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1384208 | Inhibition of HDAC3 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID723136 | Potentiation 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 assay | 2013 | Journal 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. |
AID1623531 | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate-3 by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID352753 | Antiproliferative activity against human A549 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Bioorganic & 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. |
AID1572360 | Inhibition 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 control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1702142 | Inhibition 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 ELISA | 2018 | Journal 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. |
AID1566819 | Antiproliferative activity against human ARD cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1848565 | Ratio of IC50 for cytotoxicity against human WI-38 cells to IC50 for cytotoxicity against human NCI-H522 | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1689812 | Antiproliferative activity against human H460 cells assessed as inhibition of cell growth at 2 uM measured after 72 hrs by CCK-8 assay relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1174692 | Inhibition of HDAC1 (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID297485 | Cytotoxicity against human non-proliferating RKOp21 cells | 2007 | Journal 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. |
AID1233267 | Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay | 2015 | Journal 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. |
AID353353 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control | 2009 | Journal 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. |
AID1826629 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID328805 | Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID1337195 | Inhibition 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 assay | 2016 | Journal 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. |
AID1758469 | Inhibition of human recombinant HDAC8 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1441686 | Anti-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 ELISA | 2017 | Journal 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. |
AID1578889 | Inhibition of human HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2019 | Journal 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. |
AID527045 | Cytotoxicity against human H441 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1578503 | Induction 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 %) | 2020 | ACS 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. |
AID1649505 | Antileishmanial activity against Leishmania infantum MON-1 intracellular amastigotes infected in Swiss mouse BMDM measured after 48 hrs by Giemsa staining based optical microscopic analysis | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | |
AID1753635 | Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1886237 | Antivascular activity against HUVEC cells assessed as inhibition of capillary-like tubule formation at 1 uM measured after 6 hrs by inverted microscopy | 2022 | Journal 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. |
AID1677494 | Antiproliferative activity against siRNA-induced BAX knock down human HeLa cells after 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID324948 | Inhibition of HDAC1 in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID1227049 | Cytotoxicity against human Jurkat cells assessed as cell proliferation after 70 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1754782 | Induction 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1783093 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID252895 | Concentration required to inhibit growth of human LNCaP prostate cancer cells | 2005 | Journal 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. |
AID1126996 | Induction 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%) | 2014 | Journal 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. |
AID1882456 | Inhibition of HDAC1 (unknown origin) | 2022 | Journal 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. |
AID1065638 | Inhibition of human recombinant HDAC4 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1410325 | Inhibition of recombinant human GST-tagged IDO1 (1 to 404 residues) at 1 uM using D-Tryptophan as substrate relative to control | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID1336923 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1545988 | Antiproliferative activity against human Aspc-1 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1614135 | Inhibition 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 | |||
AID1383987 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID772655 | Inhibition 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 analysis | 2013 | Journal 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. |
AID723730 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1349725 | Inhibition of recombinant human N-terminal GST-tagged HDAC4 (612 to end residues) expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1434358 | Growth inhibition of human NUGC3 cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1482129 | Cytotoxicity against human MCF10A cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1686352 | Drug 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 spectrometry | 2016 | Journal 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. |
AID1690834 | Inhibition 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 fluoresc | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1386691 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1225981 | Inhibition 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 assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1558003 | Inhibition 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 assay | 2019 | Journal 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. |
AID496803 | Inhibition of human HDAC3 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1812443 | Inhibition of human recombinant HDAC2 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID781050 | Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID1548891 | Induction 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 analysis | 2020 | Journal 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. |
AID481556 | Cytotoxicity against human KB cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID420635 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 4 hrs by Western blot | 2009 | European 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. |
AID546562 | Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay | 2010 | Journal 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. |
AID1576467 | Induction 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%) | |||
AID1614194 | Induction 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%) | |||
AID525003 | Inhibition of HDAC1 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1832798 | Cytotoxicity against human MOLT-4 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay | 2021 | Journal 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. |
AID1543933 | Antiproliferative activity against human H1299 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1543969 | Induction 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 microscopy | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID723137 | Potentiation 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 assay | 2013 | Journal 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. |
AID1730851 | Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1174693 | Inhibition of HDAC2 (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1737657 | Cytotoxicity against human THP-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | |||
AID1863176 | Selectivity index, ratio of IC50 for HDAC7 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID1451820 | Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence assay | 2017 | Journal 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. |
AID1441709 | Protection 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 method | 2017 | Journal 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. |
AID1764254 | Inhibition 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 | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID473189 | Growth inhibition of human BJ cells at 0.05 to 100 uM after 48 hrs by MTT assay | 2010 | Journal 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. |
AID1487003 | Inhibition of HDAC8 (unknown origin) by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1227031 | Inhibition of human recombinant HDAC3 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1401540 | Antiproliferative activity against human Maver2 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1434354 | Growth inhibition of human MDA-MB-231 cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID352747 | Inhibition of C-terminal FLAG tagged HDAC2 | 2009 | Bioorganic & 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. |
AID1441685 | Anti-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 method | 2017 | Journal 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. |
AID1469385 | Induction 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%) | 2018 | Journal 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 |
AID316886 | Antiproliferative activity against human SKBR3 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID482944 | Inhibition of HDAC4 | 2010 | Bioorganic & 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. |
AID1281851 | Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1898525 | Cytotoxicity against human MCF-10 A cells assessed as reduction in cell viability at 32 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Journal 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. |
AID465153 | Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID723429 | Potentiation 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 assay | 2013 | Journal 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. |
AID1785336 | Inhibition of HDAC5 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | |||
AID1227022 | Binding affinity to human HDAC8 C153A mutant assessed as loss of activity at 2 to 8 uM by Fluor-de-Lys activity assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1882467 | Inhibition of HDAC8 (unknown origin) | 2022 | Journal 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. |
AID580940 | Antitumor 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 measurement | 2010 | ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8 | Antiproliferative and differentiating activities of a novel series of histone deacetylase inhibitors. |
AID1720098 | Growth inhibition of human THP-1 cells | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID1373249 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold. |
AID760008 | Downregulation of Gli1 mRNA expression in human DaOY cells at 2.5 uM relative to DMSO-treated control | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere. |
AID1406978 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1774969 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12 | Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. |
AID258010 | Inhibition of HDAC in rat liver homogenate | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. |
AID1821962 | Selectivity 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 | |||
AID1280266 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1303627 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1469397 | Induction 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%) | 2018 | Journal 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 |
AID1155321 | Cytotoxicity against erythrocytes (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1203890 | Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1677514 | Binding 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID760499 | Cytotoxicity against human KM12 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1339585 | Growth inhibition of human Jurkat cells after 44 hrs by MTT assay | 2017 | ACS 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. |
AID525016 | Inhibition of HDAC in human CFBE41o- cell line assessed as hyperacetylation of histone H3 at 5 uM after 8 hrs by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1282299 | Inhibition 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 analysis | 2016 | Journal 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. |
AID618097 | Toxicity 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 22 | 2011 | Journal 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. |
AID1379286 | Inhibition 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 analysis | 2017 | ACS 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. |
AID1383994 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1754810 | Upregulation of SIRT4 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID594125 | Inhibition of full length HDAC8 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Discovery of histone deacetylase 8 selective inhibitors. |
AID1206750 | Induction 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 analysis | 2015 | Journal 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. |
AID1688028 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID525031 | Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1066162 | Antimigratory activity against human HCT116 cells at 50 uM after 72 hrs | 2014 | Journal 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. |
AID1178600 | Inhibition of human HDAC9 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1348913 | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1404299 | Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID348392 | Antiproliferative activity against human NB4 cells after 48 hrs | 2008 | Bioorganic & 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. |
AID619044 | Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay | 2011 | Journal 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. |
AID1652194 | Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1511128 | Induction 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 analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID670517 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
AID723122 | Potentiation 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 assay | 2013 | Journal 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. |
AID1275245 | Inhibition of VEGFR2 (unknown origin) preincubated for 5 mins followed by addition of ATP/gastrin precursor(Tyr87) biotinylated peptide cocktail incubated for 30 mins by ELISA | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC. |
AID1742757 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1155331 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for asexual blood stage of Plasmodium falciparum 3D7 | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID90353 | Inhibitory concentration against human histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID747264 | Growth inhibition of human BGC823 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID732142 | Inhibition of HDAC9 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID762187 | Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay | 2013 | Journal 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. |
AID1784971 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID760507 | Inhibition of HDAC6 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1273871 | Inhibition of HDAC3 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1742630 | Inhibition 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 analysis | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1399544 | Inhibition of recombinant human HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID1572356 | Antiproliferative activity against human T24 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1650419 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID1433256 | Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID723149 | Potentiation 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 assay | 2013 | Journal 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. |
AID1449215 | Inhibition 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 assay | 2017 | Journal 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. |
AID1653140 | Cytotoxicity against human U251 cells assessed as reduction in cell viability by SRB assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1855243 | Inhibition 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 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1467237 | Inhibition 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 fluorometr | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID1293564 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1650414 | Cytotoxicity against human A2780 cells assessed as reduction in cell viability by MTT assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID619043 | Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay | 2011 | Journal 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. |
AID663362 | Growth inhibition of human SW620 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1280261 | Inhibition of human HDAC8 using Z-L-Lys(eta-trifluoroacetyl)-AMC as substrate after 90 mins by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1722282 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17 | The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells. |
AID1890308 | Inhibition of recombinant human HDAC6 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1321712 | Inhibition 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 control | 2016 | Journal 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. |
AID527318 | Growth inhibition of human HCT116 cells after 72 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases. |
AID748106 | Inhibition of HDAC8 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1873420 | Inhibition of HDAC1 (unknown origin) at 1 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured immediately | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID652752 | Inhibition of recombinant human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID717794 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1462218 | Inhibition of human BRD4 bromo domain 2 at 5 uM | 2017 | Bioorganic & 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. |
AID603545 | Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC6 in human HeLa cell nuclear extracts | 2011 | Journal 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. |
AID717796 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1688045 | Upregulation of acetylated alpha-tubulin level in human HL-60 cells at 2 uM measured after 12 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1915567 | Cytotoxicity against human RWPE-1 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID525013 | Inhibition of HDAC7 expressed in hamster BHK cell line assessed as increase in plasma membrane Fdelta508 CFTR protein at 5 uM by immunofluorescence method | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID628288 | Antiproliferative activity against human HepG2 cells after 24 hrs by XTT assay | 2011 | Journal 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. |
AID748113 | Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1597940 | Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID414750 | Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal 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. |
AID1754765 | Downregulation of HDAC6 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1469301 | Induction 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%) | 2018 | Journal 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 |
AID1597933 | Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID670516 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
AID1384206 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1688040 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID525033 | Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1337254 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1129782 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1174686 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1848302 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID663387 | Growth inhibition of human 786-0 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1689772 | Antiproliferative activity against human H460 cells assessed as inhibition of cell growth at 8 uM measured after 72 hrs by CCK-8 assay relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1742225 | AUC (0 to infinity) in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1476183 | Inhibition 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 ATP | 2017 | Journal 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. |
AID1784185 | Inhibition of Schistosoma mansoni HDAC8 using Fluor de Lys as substrate incubated for 90 mins by fluorescence method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis. |
AID1915601 | Cytotoxicity against human SMMC-7721 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID760510 | Inhibition of HDAC3 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID737911 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1399811 | Solubility in pH 7.4 phosphate buffer solution at 100 uM after 24 hrs by HPLC method | 2018 | Bioorganic & 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. |
AID1482097 | Inhibition of HDAC 1 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1676596 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1547346 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID619047 | Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID256473 | Selectivity for class I (HD1B) against class II (HD1A) histone deacetylases | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates. |
AID274101 | Inhibition of maize HD2 (mean) | 2007 | Bioorganic & 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. |
AID328808 | Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID1403170 | Antimigratory activity in human HepG2 cells at 1 uM after 24 hrs by wound-healing assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1753839 | Inhibition of HDAC3 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1398821 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1816202 | Antiproliferative activity against human CAL-51 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | |||
AID1655888 | Inhibition 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) | 2020 | ACS 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. |
AID1127005 | Induction 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%) | 2014 | Journal 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. |
AID764216 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID385230 | Inhibition of HDAC6 | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Structural origin of selectivity in class II-selective histone deacetylase inhibitors. |
AID374828 | Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID626564 | Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 10 uM by fluorescence spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22 | 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors. |
AID747259 | Growth inhibition of human A431 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1547272 | Inhibition of HDAC6 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1467239 | Inhibition 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 fluoromet | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID1622929 | Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1235111 | Cytotoxicity against mouse B16 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1361632 | Inhibition of HDAC2 (unknown origin) after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID1486297 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1873424 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID764647 | Inhibition 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 analysis | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Novel β-dicarbonyl derivatives as inhibitors of aminopeptidase N (APN). |
AID1886186 | Inhibition of HDAC6 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay | 2022 | Journal 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. |
AID95277 | Compound was tested for anti-proliferative activity in Jurkat human leukemia cell line | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1282257 | Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1422495 | Cytotoxicity against mouse FL5.12 cells assessed as vacuole formation at 10 uM after 3 hrs by fluorescence microscopic analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1441699 | Inhibition 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 mins | 2017 | Journal 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. |
AID1775545 | Inhibition of HDAC1 (unknown origin) | 2021 | Journal 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 |
AID1633653 | Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1655793 | Inhibition of human recombinant HDAC8 using AMC-K(Ac)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID473179 | Induction of HDAC-mediated histone acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA | 2010 | Journal 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. |
AID1256442 | Inhibition VEGFR2 (unknown origin) for 30 mins by ELISA | 2015 | Bioorganic & 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. |
AID1441648 | Anti-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 method | 2017 | Journal 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. |
AID1821347 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1308510 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay | 2016 | Bioorganic & 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. |
AID1737148 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID350718 | Inhibition of human recombinant HDAC8 by fluorimetry | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1275642 | Growth inhibition of human HT-29 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1280271 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID765211 | Cytotoxicity against human A2780C/P cells | 2013 | Bioorganic & 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. |
AID1164776 | Stability of the compound in aqueous solution at pH 7.4 after 24 hrs | 2014 | Journal 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. |
AID1280282 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1566820 | Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1281848 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID663333 | Growth inhibition of human HepG2 cells after 72 hrs by MTT assay | 2012 | Journal 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. |
AID1548286 | Induction 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%) | |||
AID1863168 | Inhibition of HDAC7 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID663475 | Efflux ratio, ratio of apparent permeability from basolateral to apical side over apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM | 2012 | Journal 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. |
AID352520 | Inhibition of human recombinant HDAC10 | 2009 | Bioorganic & 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. |
AID1482166 | Cytotoxicity against human THP1 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID420320 | Binding affinity to Bordetella / Alcaligenes strain FB188 HDAC by FRET assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1785344 | Inhibition 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 | |||
AID239792 | Selectivity for class I HDACs as ratio of IC50 for maize histone deacetylase 1-A and 1-B | 2005 | Journal 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. |
AID1897397 | Induction 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%) | |||
AID1127324 | Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1164191 | Inhibition of HDAC6 in human U937 cells assessed as hyperacetylation of tubulin at 5 uM after 24 hrs by Western blot analysis relative to control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1164909 | Inhibition of HDAC4 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1754771 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1917541 | Inhibition of HDAC8 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID1469311 | Induction 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%) | 2018 | Journal 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 |
AID420634 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC50 after 4 hrs by Western blot | 2009 | European 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. |
AID246077 | Effective Concentration of compound to inhibit the growth of human SK-OV-3 cells | 2005 | Journal 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. |
AID1572355 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1826601 | Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1451831 | Inhibition 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 assay | 2017 | Journal 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. |
AID1739581 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1826598 | Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1856988 | Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by substrate addition and measured after 30 mins by multimode microplate reader analysis | 2022 | Journal 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. |
AID663381 | Growth inhibition of human MDA-MB-435 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1515910 | Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1704067 | Inhibition of c-MET(unknown origin) using FAM labelled peptide substrate preincubated for 10 mins followed by substrate addition and measured by microplate reader method | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID1784976 | Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1576456 | Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID1205628 | Growth inhibition of human MDA-MB-231 cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID1251321 | Growth inhibition of human NB4 cells after 72 hrs | 2015 | Bioorganic & 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. |
AID1600729 | Inhibition 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 me | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1355713 | Antifungal activity against FLC resistant Candida albicans 0710922 after 48 hrs in presence of fluconazol by checkerboard microdilution method | 2018 | Journal 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. |
AID1751992 | Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1206752 | Cell 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%) | 2015 | Journal 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. |
AID1476149 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2017 | Journal 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. |
AID1525780 | Inhibition of HADC8 (unknown origin) | 2020 | Journal 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. |
AID274018 | Half life after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1659653 | Antiproliferative activity against human MOLT4 cells incubated for 24 hrs by CCK8 assay | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID316944 | Inhibition of mouse SC9 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID753165 | Cytotoxicity against human HCT116 cells | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID628285 | Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay | 2011 | Journal 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. |
AID1893824 | Inhibition of HDAC in human HeLa nuclear extract measured after 30 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents. |
AID322416 | Cell cycle arrest in human LNCap cells assessed as accumulation at G1 phase relative to control at 1 uM | 2008 | Bioorganic & 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. |
AID723150 | Potentiation 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 assay | 2013 | Journal 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. |
AID659493 | Inhibition of HDAC1 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1478584 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1503841 | Inhibition 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 fluoresce | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models. |
AID1742741 | Genotoxicity in Salmonella typhimurium TA98 by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1485126 | Cell 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 cytometry | 2017 | Journal 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. |
AID1821343 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1206739 | Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1688035 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID348792 | Inhibition of human recombinant C-terminally flag tagged HDAC1 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID1280267 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1486300 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1784988 | Inhibition of HDAC8 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1816711 | Inhibition of HDAC8 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID748985 | Inhibition of HDAC3 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1857036 | Antitumor 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 analysis | 2022 | Journal 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. |
AID1168914 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1600731 | Inhibition 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 mea | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1821349 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID327544 | Increase in p21waf1 re-expression in human HCT116 cells at 10 uM after 24 hrs relative to control | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID619192 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID84278 | Concentration required for the antiproliferation of Human HT1080 fibrosarcoma cells | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC). |
AID1600658 | Inhibition 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 method | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID1234892 | Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1282245 | Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1677493 | Cytotoxicity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID308652 | Increase in p27kip1 gene expression in PANC1 cells after 48 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID619161 | Oral bioavailability in nude BALB/c mouse at 50 mg/kg | 2011 | Journal 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. |
AID1206740 | Cytotoxicity against human U937 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1848626 | Cytotoxicity against human 786-0 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1897469 | Inhibition 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 | |||
AID1545831 | Antiproliferative activity against human HepG2 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1282230 | Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID473180 | Induction of HDAC-mediated histone hyperacetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA | 2010 | Journal 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. |
AID1266085 | Inhibition of human HDAC in HeLa cells nuclear extract at 12.5 uM by fluorimetric assay | 2016 | Bioorganic & 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. |
AID723462 | Inhibition of human HDAC6 by fluorescence assay | 2013 | Journal 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. |
AID328799 | Inhibition of HDAC6 at 10 uM | 2008 | Journal 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. |
AID1826628 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1418669 | Antioxidant 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 assay | 2018 | Bioorganic & 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. |
AID1439349 | Inhibition 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 hrs | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID1597938 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID605535 | Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1775566 | Inhibition of full length human N-terminal GST-tagged HDAC6 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | 2021 | Journal 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 |
AID1702065 | Inhibition 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 assay | 2018 | Journal 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. |
AID374821 | Inhibition of wild type His-tagged HDAC7 catalytic domain T515-L952 expressed in Escherichia coli | 2009 | Journal 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. |
AID1201648 | Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1126992 | Induction 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%) | 2014 | Journal 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. |
AID1599792 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID538413 | Selectivity index, ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC6 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Inhibitors selective for HDAC6 in enzymes and cells. |
AID1775563 | Inhibition 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 assay | 2021 | Journal 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 |
AID274067 | AUC after i.p. dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID545853 | Inhibition of HDAC in Plasmodium falciparum 3D7 by fluorescent activity assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1861256 | Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1065967 | Inhibition of HDAC8 catalytic domain (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID476827 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1441692 | Protection 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) | 2017 | Journal 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. |
AID1434359 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1764799 | Inhibition 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 assay | 2021 | Journal 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. |
AID1851614 | Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation | 2022 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 74 | Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives. |
AID1401371 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1431818 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID605536 | Antiproliferative activity against human A549 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID732153 | Inhibition of HDAC4 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1864680 | Inhibition 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 | |||
AID1900934 | Toxicity 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) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID476643 | Antiproliferative activity against human U937 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1623538 | Selectivity index, ratio of IC50 for human recombinant HDAC11 to IC50 for human recombinant HDAC6 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1833061 | Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID1518787 | Antiproliferative activity against human MOLM14 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID274032 | Inhibition of HCT116 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID488276 | Inhibition of HDAC6 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | On the inhibition of histone deacetylase 8. |
AID1401544 | Antiproliferative activity against human L428 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1449329 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID411253 | Inhibition of HDAC1/2 from human HeLa cells nuclear extract by cell free fluorimetric assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1888582 | Inhibition 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 | |||
AID420652 | Toxicity 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 weeks | 2009 | European 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. |
AID1535346 | Growth inhibition of human U266 cells after 72 hrs by MTT assay | 2019 | Bioorganic & 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. |
AID1915585 | Inhibition of HDAC3 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1614137 | Inhibition 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 | |||
AID723455 | Potentiation 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 assay | 2013 | Journal 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. |
AID1566808 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1785348 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1816184 | Inhibition of HDAC6 (unknown origin) incubated for 60 mins by microplate reader analysis | |||
AID669762 | Inhibition of human recombinant HDAC2 after 30 mins by fluorometric assay | 2012 | Journal 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. |
AID1545761 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Indole: A privileged scaffold for the design of anti-cancer agents. |
AID1890351 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1861654 | Inhibition of HDAC2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1515882 | Induction 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%) | 2019 | Journal 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. |
AID1898938 | Induction of DNA damage in human A2780 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID631668 | Inhibition of human recombinant full-length HDAC3 using fluorophore conjugated substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). |
AID1697198 | Cytotoxicity against human PC3 cells by colorimetric method | 2020 | Bioorganic & 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. |
AID395034 | Antitumor 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 22 | 2009 | Bioorganic & 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. |
AID723138 | Potentiation 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 assay | 2013 | Journal 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. |
AID1164924 | Induction 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 control | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID492801 | Inhibition of human recombinant HDAC1 at 5 uM after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID1174683 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID760497 | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1599777 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1861657 | Inhibition of HDAC8 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID622260 | Inhibition of HDAC6 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1702200 | Toxicity 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%) | 2018 | Journal 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. |
AID1865270 | Inhibition of HDAC in human MV4-11 cells assessed as upregulation of acetylated alpha-tubulin level incubated for 24 hrs by Western blot analysis | 2022 | Journal 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. |
AID1754779 | Downregulation of RELA (p65 ) gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1280268 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1655902 | Inhibition 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) | 2020 | ACS 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. |
AID1282242 | Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1566810 | Inhibition of recombinant full length HDAC6 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1556028 | Inhibition of SIRT1 in human MCF7 cells assessed as H3K9Ac expression at 0.1 uM measured after 24 hrs by Western blot analysis relative to H3 | 2019 | Journal 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 |
AID704015 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID1469373 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID288450 | Growth inhibition of LOX-IMVI cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID723438 | Potentiation 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 assay | 2013 | Journal 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. |
AID732446 | Inhibition of human ES2 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID482940 | Inhibition of HDAC1 in human COLO205 cells assessed as induction of histone H3 acetylation | 2010 | Bioorganic & 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. |
AID492811 | Inhibition of HDAC in human NB4 cells assessed as increase in acetylate tubulin level at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID461250 | Inhibition of HDAC in human HeLa cell nuclear extract | 2010 | Journal 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. |
AID723130 | Potentiation 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 assay | 2013 | Journal 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. |
AID1917529 | Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID1688024 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID672026 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID663384 | Growth inhibition of human SK-MEL-5 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID420321 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 by fluorescence polarization assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1702086 | Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1864243 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1321730 | Inhibition 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 control | 2016 | Journal 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. |
AID1550118 | Induction 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%) | 2019 | Journal 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. |
AID476644 | Antiproliferative activity against human Jurkat JA16 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID593547 | Inhibition of human HDAC1 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID414986 | Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal 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. |
AID1308521 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay | 2016 | Bioorganic & 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. |
AID1762495 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1200974 | Solubility of the compound in PBS measured after overnight incubation by LYSA assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1246513 | Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1248351 | Inhibition 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 analysis | 2015 | Bioorganic & 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. |
AID1649504 | Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability measured after 72 hrs by tryphan blue assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | |
AID1487001 | Inhibition of HDAC3 (unknown origin) by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1433294 | Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs by SYBR gold staining based alkaline comet assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1537559 | Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID90212 | Inhibitory activity against histone deacetylase (HDAC1 and HDAC2) isolated from K562 erythroleukemia cells | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. |
AID1390963 | Inhibition of HDAC6 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis | 2018 | Bioorganic & 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). |
AID343694 | Inhibition of HDAC in human HeLa cells assessed as induction of histone H3 hyperacetylation after 24 hrs | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles. |
AID1126985 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID748112 | Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1439348 | Inhibition 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 hrs | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID616002 | Inhibition of HDAC1 using KI-177 as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1901163 | Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1401475 | Selectivity ratio of IC50 for HDAC2 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1451822 | Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Journal 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. |
AID1235115 | Cytotoxicity against human KG1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1280283 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID316909 | Inhibition of human DU145 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID663397 | Growth inhibition of human BT549 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1709348 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1398820 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1348937 | Effect on CDH1 gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID619056 | Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID420516 | Inhibition of HDAC in human IGROV1 cells assessed as histone-H4 acetylation at IC50 after 4 hrs by Western blot | 2009 | European 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. |
AID1832800 | Inhibition of human recombinant HDAC6 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader | 2021 | Journal 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. |
AID329921 | Inhibition of human HDAC1 in U937 cells at 5 uM | 2008 | Bioorganic & 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. |
AID1514597 | Antiproliferative activity against human HCCLM3 cells after 48 hrs by MTT assay | 2019 | Bioorganic & 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. |
AID1578478 | Inhibition 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 assay | 2020 | ACS 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. |
AID1833060 | Anticancer activity against human SK-HEP1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID329931 | Induction of apoptosis in human U937 cells at 5 uM after 30 hrs | 2008 | Bioorganic & 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. |
AID269673 | Antiproliferative activity against human MDA-MB-231 cells by SRB assay | 2006 | Bioorganic & 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. |
AID1409641 | Inhibition of HDAC in human A549 cells using Boc-K(Ac)-AMC as substrate by fluorescence assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy. |
AID1875507 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID1380947 | Antiproliferative activity against human KG1 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID605531 | Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1599780 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID613341 | Inhibition of human ERG by automated Q-patch assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1765323 | Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1848559 | Inhibition of HDAC in human HCT-116 cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1407000 | Induction of cell cycle arrest in human NB4 cells assessed as accumulation at G1 phase after 30 hrs by propidium iodide-based FACS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID723152 | Potentiation 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 assay | 2013 | Journal 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. |
AID1622962 | Inhibition of HDAC3 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID350719 | Inhibition of human recombinant HDAC6 by fluorimetry | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1742678 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1401546 | Antiproliferative activity against human DG75 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1126984 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID545855 | Antimalarial activity against Plasmodium falciparum 7G8 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1441633 | Inhibition of recombinant human cPLA2alpha expressed in Sf9 cells assessed as formation of 7-hydroxycoumarin from of 7-hydroxycoumarinyl-gamma-linolenate by fluorospectrometer analysis | 2017 | Journal 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. |
AID328829 | Toxicity 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 weeks | 2008 | Journal 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. |
AID1742184 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID659641 | Inhibition of HDAC in human DU145 cells assessed as histone H4 acetylation at 2.5 to 5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1622914 | Inhibition of HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1655889 | Inhibition 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) | 2020 | ACS 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. |
AID1742658 | Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1848620 | Cytotoxicity against human HCC 2998 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1406992 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1548248 | Inhibition 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 | |||
AID605620 | Cell 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 analysis | 2010 | Journal 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. |
AID1763816 | Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID753149 | Inhibition of HDAC3 (unknown origin) | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID1897365 | Inhibition of HDAC1 (unknown origin) | |||
AID1690833 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1165110 | Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID420317 | Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID274065 | Clearance after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1245686 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1576453 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID1739572 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1901227 | Half life in rat liver microsomes by LC-MS/MS analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1433260 | Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID541651 | Inhibition of human HDAC9 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1129784 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1164192 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1742183 | Inhibition of HDAC7 (unknown origin) using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1848616 | Cytotoxicity against human DU-145 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1727741 | Inhibition of HDAC4 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID482945 | Inhibition of HDAC5 | 2010 | Bioorganic & 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. |
AID1566041 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID1293565 | Inhibition 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 fluorescenc | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1832805 | Inhibition of human HDAC3 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm | 2021 | Journal 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. |
AID1861263 | Selectivity index, ratio of IC50 for inhibition of HDAC2 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID753148 | Inhibition of HDAC2 (unknown origin) | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID1650415 | Inhibition of HDAC in human Cal27 cells | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID753146 | Inhibition of HDAC6 (unknown origin) | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID1361646 | Cell 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%) | 2018 | Journal 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. |
AID1614128 | Inhibition 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 | |||
AID511062 | Inhibition of HDAC in human HeLa cells at 1 uM after 15 mins | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1550129 | Induction 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%) | 2019 | Journal 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. |
AID1775547 | Inhibition of HDAC3 (unknown origin) | 2021 | Journal 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 |
AID1832799 | Binding affinity to human BRD4 domain 1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry assay | 2021 | Journal 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. |
AID1737143 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID781047 | Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID1487015 | Inhibition of HDAC1 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method | 2017 | Bioorganic & 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. |
AID1873402 | Inhibition of HDAC1 (unknown origin) preincubated for 90 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID90663 | Inhibition of Histone deacetylase 1 (HDAC1) of HeLa nuclear extracts | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID414980 | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells | 2009 | Journal 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. |
AID663360 | Growth inhibition of human HT-29 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1591715 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1826626 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID404450 | Antimalarial activity against Plasmodium falciparum TM91C235 by hypoxanthine uptake | 2008 | Journal 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. |
AID385229 | Inhibition of HDAC1 | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Structural origin of selectivity in class II-selective histone deacetylase inhibitors. |
AID1771455 | Antiproliferative activity against human U-937 cells assessed as cell growth inhibition after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID544096 | Selectivity index, ratio of LC50 for mouse RAW264.7 cells to IC50 for Plasmodium falciparum | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID605396 | Inhibition of human recombinant HDAC6 using fluor de Lys as substrate by fluorometric analysis | 2010 | Journal 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. |
AID1832797 | Cytotoxicity against human TALL-1 cells assessed as cell viability at 5 uM by CellTiter-Glo luminescent assay | 2021 | Journal 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. |
AID90197 | Inhibitory concentration against histone deacetylase activity | 2001 | Journal 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. |
AID1339567 | Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS 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. |
AID717824 | Inhibition of HDAC3 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1578898 | Induction 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 control | 2019 | Journal 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. |
AID1742175 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1764801 | Inhibition 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 assay | 2021 | Journal 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. |
AID499814 | Inhibition of Plasmodium falciparum HDAC1 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1421602 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1439773 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa. |
AID1476119 | Inhibition 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 ATP | 2017 | Journal 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. |
AID274034 | Microsome stability: percent compound remaining | 2007 | Bioorganic & 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. |
AID1709361 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID527319 | Growth inhibition of human HeLa cells after 72 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases. |
AID1825926 | Inhibition 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 | |||
AID308648 | Increase in p21WAF1/CIP1 gene expression in PANC1 cells after 24 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID663398 | Growth inhibition of human T47D cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID747252 | Inhibition of human recombinant HDAC1 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1737146 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1742762 | Induction of apoptosis in mouse 4T1 cells implanted in BALB/c mouse assessed as increase in caspase-3 cleavage by immunohistochemistry method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1690840 | Disaggregation 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 control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID329922 | Inhibition of human HDAC4 in U937 cells at 5 uM | 2008 | Bioorganic & 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. |
AID1578480 | Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay | 2020 | ACS 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. |
AID1764800 | Inhibition 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 assay | 2021 | Journal 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. |
AID618017 | Antitumor 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 control | 2011 | Journal 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. |
AID1384231 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID384317 | Inhibition of maize histone deacetylase 1A | 2008 | European 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. |
AID446336 | Metabolic stability in human liver microsomes assessed as half life | 2010 | Journal 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. |
AID350731 | Growth inhibition of human RXF631L cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1321700 | Inhibition of HDAC1 (unknown origin) | 2016 | Journal 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. |
AID1739584 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID300834 | Growth inhibition of human ACHN cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID1486676 | Inhibition 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 analysis | 2017 | Bioorganic & 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. |
AID1543954 | Induction 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%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1915602 | Cytotoxicity against human A2780P cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID652749 | Inhibition of recombinant human HDAC5 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1566816 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID710837 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID1599722 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1865263 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1886181 | Inhibition 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 control | 2022 | Journal 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. |
AID1518782 | Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1812445 | Inhibition of human recombinant HDAC6 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1129772 | Increase in p21 protein expression in human Jurkat cells at 10 uM after 24 hrs by FACS flow cytometric analysis | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID526536 | Growth inhibition of human HCT15 cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1336947 | Induction 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%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1365022 | Inhibition 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 assay | 2017 | Bioorganic & 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. |
AID1533327 | Inhibition 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 method | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor. |
AID1515908 | Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1469335 | Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID1622986 | Inhibition of HDAC8 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1742229 | Antimetastatic 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 analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1873381 | Inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1476158 | Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID540210 | Clearance in human after iv administration | 2008 | Drug 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. |
AID1294805 | Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate by fluorometric assay | 2016 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10 | A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors. |
AID760508 | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1282275 | Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumor mass change at 50 mg/kg, ip q2d for 12 days | 2016 | Journal 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. |
AID1406988 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1597937 | Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1547248 | Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1177043 | Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1848627 | Cytotoxicity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID621737 | Inhibition of HDAC1 by fluorescent activity assay | 2011 | Bioorganic & 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. |
AID1202593 | Cytotoxicity against human HeLa cells after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID90691 | Inhibition of maize Histone deacetylase 2 | 2004 | Journal 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. |
AID1275638 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1478601 | Induction of apoptosis in human K562 cells after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1702100 | Inhibition 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 analysis | 2018 | Journal 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. |
AID604082 | Inhibition of JMJD2E | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Inhibitors of histone demethylases. |
AID303347 | Inhibition of HDAC in HeLa nuclear extract in presence of DTT | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. |
AID421216 | Inhibition of HDAC1 from human HeLa cells at 5 uM | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID605527 | Inhibition of HDAC1 in human HCT116 cells assessed as induction of histone H3K9 acetylation after 30 hrs by Western blot analysis | 2010 | Journal 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. |
AID717820 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1439352 | Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter 96 AQueous Non-Radioactive assay | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID747253 | Growth inhibition of human DU145 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1215092 | Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 up to 46 uM after 24 hrs by luminescent analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1398819 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1543945 | Inhibition of human recombinant HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID499812 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum D6 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1206754 | Antitumor 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 control | 2015 | Journal 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. |
AID1594438 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10 | Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors. |
AID622256 | Inhibition of HDAC3 after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1514599 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID672034 | Ratio of IC50 for human HDAC2 preincubated for 24 hrs to IC50 for human HDAC2 preincubated for 5 mins | 2012 | Bioorganic & 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. |
AID1202585 | Inhibition of His-tagged HDAC8 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID1466062 | Inhibition of recombinant human full length HDAC4 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID655474 | Restoration of CFTR deltaF508 mutant trafficking to cell surface as glycoforms in human CFBE41o cells at 1 uM after 24 hrs by Western blotting | 2011 | ACS 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. |
AID1240552 | Induction 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%) | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID492803 | Inhibition of human recombinant HDAC1 after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID1548290 | Induction 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%) | |||
AID1326528 | Toxicity in nude mouse xenografted with human HCT116 cells assessed as change in body weight at 200 mg/kg, po qd | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1865261 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1469299 | Induction 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%) | 2018 | Journal 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 |
AID1890310 | Inhibition of HDAC3 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1897466 | Inhibition 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 | |||
AID1363797 | Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID310186 | Antitumor activity against MDA-MB-231 cells xenografted BALB/c nude mouse at 30 mg/kg, ip for 15 days | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID526533 | Growth inhibition of human MDA-MB-231 cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1273873 | Metabolic stability in mouse liver microsomes assessed as compound remaining at 1 uM preincubated for 10 mins measured after 30 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1739587 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1900917 | Induction 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 analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID352524 | Antiproliferative activity against human Panc 04.03 cells by MTT assay | 2009 | Bioorganic & 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. |
AID347807 | Inhibition of human HDAC8 at 0.50 uM | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1486294 | Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID593548 | Inhibition of human HDAC3 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID652764 | Inhibition of HDAC8 in human HeLa cells nuclear extract using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1141761 | Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorimetric analysis | 2014 | Journal 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. |
AID1890323 | Inhibition of HDAC1 in mouse CT26 cells assessed as accumulation of acetylated H3 level at 6 uM after 24 hrs by Western blotting analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1426428 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID663358 | Growth inhibition of human HCT116 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID775834 | Inhibition 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 control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1355714 | Synergistic antifungal activity against FLC resistant Candida albicans 0304103 assessed as FIC index after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1742223 | Cmax in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1769653 | Inhibition of ALK G1202R mutant (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1141783 | Inhibition of HDAC in human HCT116 cells assessed as increase in histone-H3 acetylation after 3 hrs by Western blotting analysis | 2014 | Journal 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. |
AID353354 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay | 2009 | Journal 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. |
AID1622904 | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1676594 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1633416 | Inhibition of human recombinant GSK3beta up to 50 uM using GSM as substrate incubated for 30 mins by luminescence based assay | 2019 | ACS 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. |
AID1383985 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1704064 | Inhibition 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 method | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID1811364 | Inhibition of HDAC4 (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID1864238 | Stabilization 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 assay | 2022 | Journal 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. |
AID1826596 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1547282 | Inhibition of HDAC in human HCT116 cells assessed as increase in acetylated histone H3 expression level measured after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1653143 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID481554 | Cytotoxicity against human KB cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1380954 | Inhibition 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 assay | 2018 | Journal 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. |
AID1383988 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1410014 | Selectivity index, ratio of CC50 for human U937 cells to EC50 for reactivation of latent HIV1 infected in human U1 cells | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor. |
AID1337293 | Therapeutic index, ratio of IC50 for mouse TAMH cells to IC50 for human cancer cells | 2016 | Journal 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. |
AID1848583 | Inhibition of full length C-terminal his6-tagged human recombinant HDAC2 (1 to 488 residues) | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1702067 | Inhibition 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 assay | 2018 | Journal 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. |
AID1415668 | Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP expression at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID446345 | Clearance in CD1 mouse at 15 mg/kg, po | 2010 | Journal 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. |
AID1415646 | Inhibition of HDAC1 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1433291 | Induction 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 cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1821965 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | |||
AID1890332 | Stability in mouse liver microsomes assessed as half-life and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID780580 | Inhibition of Topoisomerase 2 (unknown origin) assessed as impairment of pBR322 DNA decatenation at 100 uM after 30 mins by agarose gel electrophoresis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. |
AID1487042 | Inhibition 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 addition | 2017 | Bioorganic & 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. |
AID384316 | Inhibition of maize histone deacetylase 1B | 2008 | European 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. |
AID90682 | Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation | 2002 | Journal 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. |
AID1240549 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID1487046 | Inhibition of HDAC3 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1326518 | Inhibition 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 analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1312876 | Antitumor 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 control | 2016 | Journal 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. |
AID1783062 | Antifungal activity against fluconazole-resistant Candida tropicalis 5008 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1898953 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID541653 | Inhibition of human HDAC10 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID476832 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1548268 | Induction 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 | |||
AID1578505 | Induction 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 %) | 2020 | ACS 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. |
AID1861653 | Inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1422514 | Inhibition of HDAC in MEF assessed as increase in histone H3K18 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1431817 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID274099 | Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 50% of isolates after 48h. | 2007 | Bioorganic & 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. |
AID1497923 | Induction 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 analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | Development of the first small molecule histone deacetylase 6 (HDAC6) degraders. |
AID1200973 | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac)AMC as substrate | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1848594 | Induction 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1383989 | Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1751984 | Inhibition of HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID1826650 | Antitumor 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 control | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1203896 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1816212 | Induction 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%) | |||
AID663391 | Growth inhibition of human SN12C cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1282240 | Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1597930 | Inhibition of HDAC in human HeLa cell nuclear extracts at 1 uM | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1515914 | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID304373 | Inhibition of HDAC | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. |
AID1441662 | Anti-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 method | 2017 | Journal 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. |
AID1547300 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1550084 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | Journal 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. |
AID411259 | Cytotoxicity against human NCI-H69 cells after 72 hrs by trypan blue exclusion assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1614131 | Inhibition 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 | |||
AID1816206 | Induction 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%) | |||
AID1384230 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1599728 | Cytotoxicity against human Meso163 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1702199 | Toxicity 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 12 | 2018 | Journal 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. |
AID1436790 | Growth inhibition of human NCI-H292 cells in FBS containing medium after 72 hrs using compound after sonication in presence of LDL by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity. |
AID1855261 | Induction 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%) | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1742719 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID496801 | Inhibition of human HDAC1 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1126966 | Selectivity ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2014 | Journal 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. |
AID1825927 | Inhibition 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 | |||
AID761585 | Inhibition of HDAC in human HeLa cell extract using fluor de Lys as substrate at 1 uM after 15 mins by fluorometric analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID90351 | Concentration required to inhibit human Histone deacetylase (HDAC) enzyme by 50% | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4 | Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1164178 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1399809 | Clearance in human hepatocytes assessed per million cells at 1 uM after 5 to 90 mins by LC-MS/MS analysis | 2018 | Bioorganic & 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. |
AID374827 | Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID274063 | Half life after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID404449 | Antimalarial activity against Plasmodium falciparum W2 by hypoxanthine uptake | 2008 | Journal 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. |
AID255818 | Inhibitory concentration against Histone deacetylase 1B in maize | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates. |
AID1543929 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID525021 | Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 5 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1487045 | Inhibition of HDAC2 (unknown origin) assessed as remaining enzyme activity at 1 uM by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1127007 | Induction 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%) | 2014 | Journal 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. |
AID1821345 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID748114 | Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1901229 | Half life in human liver microsomes by LC-MS/MS analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID473191 | Growth inhibition of human BJ cells after 48 hrs by MTT assay | 2010 | Journal 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. |
AID1503585 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design. |
AID637888 | Inhibition of recombinant human HDAC1 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | 2012 | Bioorganic & 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. |
AID1234893 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1543930 | Antiproliferative activity against human SMMC7721 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1887681 | Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID1550325 | Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as combination index after 48 hrs in presence of ruxolitinib by MTT assay | 2019 | Journal 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. |
AID1848601 | Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1502981 | Antiproliferative activity against human MGC803 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1702058 | Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay | 2018 | Journal 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. |
AID1885672 | Synergistic antiproliferative activity against human HFL1 cells at 2.5 to 12.5 uM measured after 72 hrs in presence of CDDO-Me by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy. |
AID473190 | Growth inhibition of human MUF cells at 0.05 to 100 uM after 48 hrs by MTT assay | 2010 | Journal 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. |
AID618087 | Toxicity 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 8 | 2011 | Journal 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. |
AID246081 | Effective Concentration of compound to inhibit the growth of human NCI-H226 cells | 2005 | Journal 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. |
AID1469491 | Antitumor 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 days | 2018 | Journal 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 |
AID1421902 | Antiplasmodial activity against drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID732874 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1293562 | Antiproliferative activity human HCT116 cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1459948 | Antiproliferative activity against human PC3 cells measured after 48 hrs by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1549141 | Antifungal activity against azole-sensitive Cryptococcus neoformans H99 after 72 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID1481749 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
AID1901171 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1511969 | Selectivity 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 | 2019 | ACS 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. |
AID1848301 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID632973 | Cytotoxicity against human PC3 cells | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1702062 | Inhibition 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 b | 2018 | Journal 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. |
AID1848624 | Cytotoxicity against human KM12 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1888416 | Inhibition of fungal filamentation in azole-resistant Candida albicans 0304103 assessed as reduction in yeast-hypha transition at 64 ug/ml by inverted microscopic analysis | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID1127008 | Induction 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%) | 2014 | Journal 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. |
AID1614127 | Inhibition 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 | |||
AID1312869 | Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay | 2016 | Journal 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. |
AID1389951 | Cytotoxic activity against human MCF7 cells assessed as reduction in cell viability at 4 uM after 24 hrs by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID347868 | Growth inhibition of human Colon cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1732193 | Cytotoxicity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition. |
AID1873383 | Inhibition of HDAC3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID761582 | Inhibition of full length His-tagged human recombinant HDAC6 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID208381 | Concentration required to reassume their usual morphology of T/5 cells | 1995 | Journal 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. |
AID1476146 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2017 | Journal 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. |
AID1547350 | Antitumor 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 19 | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1401376 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID297482 | Cytotoxicity against human SKBR3 cells | 2007 | Journal 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. |
AID1518783 | Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID347875 | Growth inhibition of human CNS cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1361651 | Induction 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%) | 2018 | Journal 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. |
AID1515913 | Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1545842 | Antiproliferative activity against human A549 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID297472 | Inhibition of HDAC in HeLa cells assessed as induction of human histone H3 hyperacetylation | 2007 | Journal 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. |
AID1861305 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation at S phase measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1550324 | Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs in presence of ruxolitinib by MTT assay | 2019 | Journal 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. |
AID527043 | Cytotoxicity against human NCI-H522 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1901174 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1816966 | Cytotoxicity against human CEM cells assessed as cell death incubated for 20 hrs measured by DNS assay | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their |
AID1864216 | Inhibition of HDAC in human HeLa nuclear extract incubated for 30 mins by fluorescence-based Glo-luminescence assay | 2022 | Journal 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. |
AID1689773 | Inhibition 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 control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID1164902 | Inhibition of HDAC6 in human A549 cells assessed as tubulin acetylation after 17 to 18 hrs by cytoblot assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1482120 | Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1707507 | Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID1816200 | Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | |||
AID605538 | Antiproliferative activity against doxorubicin-resistant human COR-L23 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1355706 | Antifungal activity against FLC resistant Candida albicans 0304103 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1677515 | Binding 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1888590 | Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay | |||
AID1164906 | Inhibition of HDAC1 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1336944 | Induction 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%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1742221 | Half life in Beagle dog at 20 mg/kg, po by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1901172 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID732876 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1639365 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1898906 | Antiproliferative activity against human Z138 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1515911 | Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID313734 | Inhibition of HDAC6 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID324949 | Inhibition of HDAC3 in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID717817 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1390025 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID482957 | Half life in rat liver microsome | 2010 | Bioorganic & 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. |
AID1205630 | Growth inhibition of human HCT15 cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID1467240 | Inhibition 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 fluorometri | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID1129779 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID476641 | Antiproliferative activity against human SK-BR-3 cells after 48 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID525019 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR protein level at 1 uM after 1 hr by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1269319 | Cytotoxicity against human A2780S cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID1240548 | Inhibition of HDAC1/2 in human HeLa cells nuclear extracts using acetylated histone peptide as substrate after 30 mins by Color de Lys assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID765198 | Cytotoxicity against human MDA-MB-231 cells | 2013 | Bioorganic & 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. |
AID1466065 | Inhibition of HDAC in human PC3 cells assessed as increase in histone H3 acetylation at 1 uM after 24 hrs by Western blot analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1742657 | Cytotoxicity against human B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID663388 | Growth inhibition of human A498 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID482966 | Clearance in mouse at 10 mg/kg, iv | 2010 | Bioorganic & 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. |
AID1141768 | Cytotoxicity against human A549 cells by MTT assay | 2014 | Journal 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. |
AID1337288 | Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutant after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1730888 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1887685 | Cytotoxicity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID1141797 | Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2014 | Journal 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. |
AID670513 | Inhibition of EGFR derived from human A431 cell membrane assessed as inhibition of poly-Glu-Tyr phosphorylation after 30 mins by ELISA assay | 2012 | Bioorganic & 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. |
AID1623533 | Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1863441 | Inhibition of HDAC9 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1454032 | Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate by fluorimetric method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1066163 | Cytotoxicity against human HCT116 cells at 50 uM after 72 hrs | 2014 | Journal 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. |
AID609498 | Half life in human liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1548288 | Induction 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%) | |||
AID1742704 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID623020 | Inhibition of human HDAC1 expressed in Escherichia coli using fluorogenic substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay | 2011 | European 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. |
AID1466058 | Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID672023 | Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis | 2012 | Bioorganic & 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. |
AID1764252 | Inhibition 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 measu | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID269674 | Antiproliferative activity against human NCI-H23 cells by SRB assay | 2006 | Bioorganic & 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. |
AID524991 | Inhibition 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 control | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1702155 | n-Octanol/water distribution coefficient, logD of the compound at pH 7.4 | 2018 | Journal 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. |
AID1769654 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID663347 | Growth inhibition of human MOLT4 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID90350 | Inhibitory activity against histone deacetylase (HDAC) enzyme obtained from H1299 human lung carcinoma cell lysates | 2003 | Journal 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). |
AID1141243 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys (acetyl)-AMC as fluorogenic substrate after 30 mins by spectrophotometry | 2014 | Bioorganic & 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. |
AID1897805 | Inhibition 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 anal | 2022 | Journal 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. |
AID1742684 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1170740 | Inhibition of human recombinant HDAC1 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID443645 | Binding affinity to pyridoxal-5'-phosphate assessed as formation of PLP-aldoxime at 5 mM after 1 hr by UV/vis spectroscopy | 2009 | Journal 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. |
AID1178599 | Inhibition of human HDAC4 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1487096 | Inhibition of HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID1164196 | Inhibition of HDAC6 in human MCF7 cells assessed as hyperacetylation of tubulin at 5 uM after 24 hrs by Western blot analysis relative to control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1486299 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1155329 | Antimalarial 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 counting | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1487008 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID1732191 | Cytotoxicity against human HuT78 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition. |
AID1401543 | Antiproliferative activity against human OCI-LY3 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID414981 | Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | 2009 | Journal 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. |
AID1751986 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID243634 | In vitro inhibition against human Histone deacetylase | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors. |
AID1401368 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1164926 | Effect on p21 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1227043 | Stability in human plasma assessed as compound remaining after 1 hr by HPLC analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1303631 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1515883 | Induction 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%) | 2019 | Journal 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. |
AID1671983 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase measured after 24 hrs | 2019 | Bioorganic & 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. |
AID1273877 | Inhibition of human CYP2C19 using 3-cyano-7-ethoxycoumarin as substrate at 10 uM after 30 mins by fluorimetric analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1399812 | Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method | 2018 | Bioorganic & 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. |
AID1861656 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1849167 | Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1164785 | Inhibition of HDAC10 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1622942 | Cytotoxicity against human AML cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID420506 | Antiproliferative activity against cisplatin-resistant human IGROV1 cells after 72 hrs | 2009 | European 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. |
AID663341 | Inhibition of HDAC in human MDA-MB-231 cells assessed as stimulation of histone H3 acetylation incubated for 24 hrs by Western blot | 2012 | Journal 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. |
AID1832681 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1312868 | Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay | 2016 | Journal 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. |
AID316895 | Inhibition of human MCF7 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID544399 | Antimalarial activity against Plasmodium falciparum infected in mouse RAW264.7 cells | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID723424 | Potentiation 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 assay | 2013 | Journal 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. |
AID1754780 | Downregulation of RELB gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1864242 | Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated H4 level at 1.25 to 5 uM by Western blot analysis | 2022 | Journal 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. |
AID329916 | Induction of histone H4 hyperacetylation in human U937 cells | 2008 | Bioorganic & 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. |
AID1876462 | Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence plate reader assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID759309 | Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1599723 | Cytotoxicity against human Meso13 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID297486 | Cytotoxicity against human proliferating RKOp21 cells | 2007 | Journal 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. |
AID1164028 | Inhibition of human recombinant HDAC4 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID732447 | Inhibition of human PC3 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1155335 | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1541450 | Cytotoxicity against human CAL27 cells assessed as reduction in cell survival measured after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1821967 | Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | |||
AID1587864 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1816207 | Induction 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%) | |||
AID1418670 | GPx-like activity of the compound assessed as velocity for H2O2 reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & 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. |
AID1441635 | Inhibition 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 analysis | 2017 | Journal 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. |
AID1915538 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID328801 | Inhibition of HDAC8 expressed in Escherichia coli | 2008 | Journal 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. |
AID1312925 | Inhibition 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 method | 2016 | Journal 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. |
AID1279130 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors. |
AID1605977 | Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1821342 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1614226 | Induction 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%) | |||
AID1848625 | Cytotoxicity against human SW620 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1469326 | Induction 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%) | 2018 | Journal 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 |
AID1548258 | Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay | |||
AID1832682 | Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID670012 | Inhibition of human recombinant HDAC6 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID781051 | Inhibition of HDAC in human HeLa cell nuclear extracts using Fluor de Lys as substrate by fluorescence assay | 2013 | Bioorganic & 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. |
AID1296346 | Inhibition 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 assay | 2016 | Journal 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. |
AID1653119 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1816381 | Inhibition of JAK2 (unknown origin) assessed as inhibition rate at 10 nM incubated for 60 mins by microplate reader analysis relative to control | |||
AID1647330 | Anti-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 measured | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID329928 | Inhibition of human HDAC4 in U937 cells assessed as residual activity at 5 uM | 2008 | Bioorganic & 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. |
AID760518 | Therapeutic index, ratio of GI50 for human HMEC to GI50 for human SK-BR-3 cells | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1622931 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1856998 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID1365026 | Selectivity ratio of IC50 for recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 for recombinant human HDAC2 | 2017 | Bioorganic & 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. |
AID1415653 | Inhibition of HDAC8 in human HepG2 cells assessed as increase in acetylated-histone H3 level at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1774968 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12 | Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. |
AID1819504 | Inhibition of HDAC2 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2022 | Journal 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. |
AID1361631 | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1482100 | Inhibition of HDAC 8 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1396961 | Antiproliferative activity against human MCF7 cells | 2018 | Bioorganic & 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). |
AID1898903 | Antiproliferative activity against human Ramos cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1915568 | Cytotoxicity against human PC-3 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1502978 | Antiproliferative activity against human PC3 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1566804 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID760504 | Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1166496 | Inhibition of human recombinant full length HDAC1 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins | 2014 | Bioorganic & 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. |
AID1502987 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID526535 | Growth inhibition of human NUGC3 cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1337289 | Antiproliferative activity against human NKYS cells after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1709352 | Selectivity index, ratio of IC50 for human HS5 cells to IC50 for human NAMALVA cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID524994 | Inhibition of HDAC9 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1578156 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1742176 | Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1742750 | Antitumor 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 34 | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1482098 | Inhibition of HDAC 2 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1234906 | Antitumor activity against human H7402 cells xenografted in mouse assessed as tumor increment ratio at 100 mg/kg/day, po for 16 days relative to control | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID609507 | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect High5 cells using Boc-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors. |
AID374822 | Inhibition of C-terminal His-tagged HDAC8 expressed in Escherichia coli | 2009 | Journal 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. |
AID1437239 | Inhibition of HDAC6 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID1702060 | Inhibition 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 assay | 2018 | Journal 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. |
AID545858 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID618013 | Cell 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 analysis | 2011 | Journal 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. |
AID1380956 | Inhibition 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 assay | 2018 | Journal 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. |
AID1384207 | Inhibition of HDAC2 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID503688 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID652757 | Down regulation of HDAC7 in human CFBE41o cells at 0.2 to 5 uM by Western blot analysis | 2011 | ACS 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. |
AID1269317 | Cytotoxicity against mouse NIH/3T3 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID1742739 | Inhibition of human ERG | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID374811 | Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells | 2009 | Journal 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. |
AID1431811 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1888584 | Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay | |||
AID519587 | Toxicity in neonatal foreskin fibroblasts | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1355708 | Antifungal activity against FLC resistant Candida albicans 100 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1449327 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1415667 | Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase3 expression at 5 uM after 48 hrs by Western blot analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1336948 | Induction 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%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1859937 | Antiproliferation activity against human U-937 cells assessed as reduction in cell viability at 5 to 50 uM measured after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1205629 | Growth inhibition of human ACHN cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID1127331 | Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1173502 | Inhibition of N-terminal GST-tagged human HDAC4 (627 to 1085 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID717819 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1401504 | Cytotoxicity against human Jurkat cells assessed as cell viability at 1 uM after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID488273 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | On the inhibition of histone deacetylase 8. |
AID373085 | Antitumor 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 postxenografting | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID781048 | Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID404448 | Antimalarial activity against Plasmodium falciparum D6 by hypoxanthine uptake | 2008 | Journal 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. |
AID392408 | Induction of histone H3 acetylation in human T24 cells after 3 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Sulfamides as novel histone deacetylase inhibitors. |
AID1487090 | Increase 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 untreat | 2017 | Bioorganic & 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. |
AID420511 | Cell cycle arrest in human IGROV1 cells assessed as accumulation at sub-G1 phase at IC90 after 24 hrs using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID482953 | Antiproliferative activity against human PC3 cells | 2010 | Bioorganic & 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. |
AID1129787 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1336924 | Cytotoxicity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1384209 | Inhibition of HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1511156 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1702135 | Inhibition 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 %) | 2018 | Journal 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. |
AID1812467 | Antiplasmodial 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 assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1605974 | Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID310126 | Growth inhibition of human H460 cells by SRB assay | 2007 | Bioorganic & 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. |
AID1275641 | Growth inhibition of human HCT116 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1390811 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
AID1478582 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1386685 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1547257 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1591854 | Inhibition 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 contro | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID1266812 | Antiproliferative activity against human LoVo cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1348932 | Upregulation of TNFalpha gene expression in human A549 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1487091 | Increase 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 untreated | 2017 | Bioorganic & 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. |
AID1485125 | Cell 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 cytometry | 2017 | Journal 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. |
AID1164927 | Effect on acetylated histone H3 expression in human BE(2)-C cells at 10 uM after 24 hrs by immunoblot method relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID90690 | In vitro for anti-HD2 (Histone deacetylase 2) activity in maize | 2002 | Journal 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. |
AID1337285 | Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1764815 | Inhibition of Nanoluc-fused HDAC1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay | 2021 | Journal 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. |
AID1164918 | Antiproliferative activity against human BE(2)-C cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1784985 | Inhibition of HDAC1 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1764298 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1173499 | Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID1785342 | Inhibition of recombinant human SIRT2 measured after 30 mins by fluorescence microplate reader assay | |||
AID525032 | Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 1 uM | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1383993 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1639367 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID603540 | Toxicity in human MDA-MB-231 cells xenografted athymic nude mouse assessed as signs of toxicity at 90 mg/kg, ip qd for 21 days | 2011 | Journal 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. |
AID1690839 | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation after 24 hrs by thioflavin-T fluorescence method | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1848584 | Inhibition of full length C-terminal FLAG-tagged human recombinant HDAC6 expressed inSf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1275640 | Growth inhibition of human MCF7 cells after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1688034 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID503692 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1390010 | Inhibition 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 ass | 2018 | Bioorganic & 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. |
AID1578496 | Induction 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 %) | 2020 | ACS 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. |
AID619142 | Apparent permeability from apical to basolateral side of human Caco2 cells | 2011 | Journal 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. |
AID663383 | Growth inhibition of human SK-MEL-28 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1816186 | Inhibition of HDAC1 (unknown origin) incubated for 60 mins using microplate reader analysis | |||
AID1174705 | Antitumor activity against human U937 cells xenografted in athymic nude mouse at 120 mg/kg/day, po after 16 days relative to control | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1403179 | Inhibition of Akt phosphorylation in human HepG2 cells at 2 uM after 48 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1576461 | Induction 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 | |||
AID1200982 | AUC (0 to infinity) in ICR mouse at 10 mg/kg, iv | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1623528 | Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID670971 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID313730 | Inhibition of HDAC2 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID1449321 | Antiproliferative activity against human ONS76 cells after 72 hrs by Celltiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID297471 | Inhibition of recombinant HDAC1 in HeLa cells | 2007 | Journal 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. |
AID1373250 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold. |
AID1451829 | Inhibition 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 assay | 2017 | Journal 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. |
AID1511151 | Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1174684 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID619264 | Antitumor 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 | 2011 | Journal 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. |
AID1688044 | Upregulation of acetylated H3 level in human HL-60 cells at 2 uM measured after 12 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID274077 | Inhibition of HCT116 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID1537566 | Cell 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 %) | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID373076 | Inhibition of human recombinant HDAC3 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1384210 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID316935 | Inhibition of HDAC5 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1164783 | Inhibition of HDAC6 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1205632 | Growth inhibition of human NUGC3 cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID1336926 | Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1600656 | Inhibition 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 method | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID1514603 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID348802 | Inhibition of HDAC7 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID628436 | Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal 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. |
AID1677512 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1234909 | Toxicity in human H7402 cells xenografted mouse assessed as change in body weight at 100 mg/kg/day, po for 16 days | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1578500 | Induction 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 %) | 2020 | ACS 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. |
AID246062 | Effective Concentration of compound to inhibit the growth of human St-4 cells | 2005 | Journal 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. |
AID1785335 | Inhibition of HDAC4 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | |||
AID1572359 | Inhibition 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 control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID447579 | Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies. |
AID607635 | Inhibition of HDAC6 in human Hela cells assessed as increase in alpha-tubulin acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. |
AID1355745 | Antitumor 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 control | 2018 | Journal 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. |
AID1410327 | Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID1737150 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1890518 | Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID659634 | Antiproliferative activity against human DU145 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1821265 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1848615 | Cytotoxicity against human PC-3 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1861335 | Inhibition of HDAC in human OCILY3 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 2.5 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1164036 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1549163 | Inhibition 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 fluorimetry | 2020 | Journal 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. |
AID1321732 | Inhibition 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 control | 2016 | Journal 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. |
AID1421915 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID348803 | Inhibition of HDAC8 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID1413067 | Inhibition of nuclear HDAC in human SKOV3 cells assessed as increase in acetylated histone H3 levels at 10 uM after 1 hr by immunoblot method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition. |
AID1599765 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1127328 | Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID628286 | Antiproliferative activity against human HeLa cells after 24 hrs by XTT assay | 2011 | Journal 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. |
AID1060989 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors. |
AID540213 | Half life in human after iv administration | 2008 | Drug 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. |
AID1326513 | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1410330 | Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID1441678 | Protection 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 method | 2017 | Journal 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. |
AID1235110 | Cytotoxicity against human U937 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1861254 | Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1173501 | Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & 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. |
AID208382 | Concentration required to reduce cell proliferation of T/5 cells | 1995 | Journal 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. |
AID1274872 | Inhibition of HDAC2 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1897369 | Inhibition of FGFR1 (unknown origin) at 10 nM relative to control | |||
AID1206756 | Antitumor 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 control | 2015 | Journal 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. |
AID1126981 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1401556 | Antiproliferative activity against human MM487 cells at 10 uM after 72 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1599725 | Cytotoxicity against human A549 cells assessed as cell permeability measured after 72 hrs by CellTox Green assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID628211 | Antiproliferative activity against human HeLa cells after 72 hrs by XTT assay | 2011 | Journal 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. |
AID1699970 | Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay | 2020 | Bioorganic & 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. |
AID1819523 | Induction 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 control | 2022 | Journal 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. |
AID1128978 | Inhibition of human HDAC-1 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1339569 | Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS 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. |
AID760509 | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID663354 | Growth inhibition of human NCI-H322M cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1164913 | Inhibition of HDAC8 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1482099 | Inhibition of HDAC 3 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1330947 | Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1547261 | Inhibition of human recombinant His-tagged BRD2 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1548289 | Induction 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%) | |||
AID663348 | Growth inhibition of human SR cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID723120 | Potentiation 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 assay | 2013 | Journal 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. |
AID1245687 | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID297494 | Cytotoxicity against human Saos2 cells | 2007 | Journal 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. |
AID1771456 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID1861266 | Selectivity index, ratio of IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID420329 | Inhibition of HDAC from RT extract | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1462219 | Inhibition of human BRD4 bromo domain 2 at 0.5 uM | 2017 | Bioorganic & 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. |
AID1890312 | Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1361653 | Induction 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%) | 2018 | Journal 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. |
AID1587866 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1819533 | Toxicity 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 analysis | 2022 | Journal 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. |
AID1655789 | Inhibition of human recombinant HDAC3 using AMC-K(Ac)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID1873400 | Inhibition of HDAC1 (unknown origin) preincubated for 30 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1515906 | Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID527317 | Inhibition of HDAC in human HeLa cell nuclear extracts by fluorimetric assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases. |
AID1487038 | Inhibition 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 addition | 2017 | Bioorganic & 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. |
AID1550105 | Inhibition 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 analysis | 2019 | Journal 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. |
AID348801 | Inhibition of HDAC5 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID760491 | Cytotoxicity against human SW620 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1702057 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay | 2018 | Journal 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. |
AID673992 | Inhibition of recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1361649 | Induction 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%) | 2018 | Journal 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. |
AID1234894 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1482101 | Inhibition of HDAC 4 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1785021 | Metabolic 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 analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1865298 | Toxicity in BALB/c mouse allografted with mouse 4T1 cells assessed as body weight loss at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID1511134 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1597970 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1486672 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1848579 | Inhibition 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1174691 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1336949 | Induction 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%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID269668 | Inhibition of HeLa cell HDAC | 2006 | Bioorganic & 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. |
AID663335 | Growth inhibition of human SW620 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1605968 | Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1246507 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1825923 | Inhibition 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 | |||
AID1784981 | Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1784978 | Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1630599 | Inhibition 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 assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID316907 | Inhibition of human RFX631L cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1623532 | Inhibition of HDAC10 (unknown origin) by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1847777 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID1282279 | Antitumor activity against human HCT116 cells xenografted in Balb/c nude mouse assessed as tumor mass change at 100 mg/kg, po q2d for 8 days | 2016 | Journal 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. |
AID269671 | Antiproliferative activity against human LOX-IMVI cells by SRB assay | 2006 | Bioorganic & 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. |
AID1433234 | Induction 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 cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID420517 | Inhibition of HDAC in human IGROV1 cells assessed as histone-H4 acetylation at IC80 after 4 hrs by Western blot | 2009 | European 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. |
AID1380955 | Inhibition 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 assay | 2018 | Journal 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. |
AID1421921 | Selectivity 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 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID385231 | Inhibition of HDAC9 | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Structural origin of selectivity in class II-selective histone deacetylase inhibitors. |
AID775828 | Inhibition of TPCK-treated trypsin (unknown origin) at 10 uM preincubated for 10 mins prior to substrate addition measured for 30 mins by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1339570 | Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS 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. |
AID1493592 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID1783108 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
AID1861344 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID1865266 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1464876 | Anti-proliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID603218 | Inhibition of HDAC in human HeLa cell extracts assessed as conversion of dithiothreitol to dithiol after 1 hr by Flour-de-Lys assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
AID1441647 | Anti-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 method | 2017 | Journal 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. |
AID1476148 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2017 | Journal 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. |
AID481560 | Cytotoxicity against human Bel7402 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1864227 | Inhibition of full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay | 2022 | Journal 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. |
AID482955 | Thermodynamic solubility at pH 7.4 | 2010 | Bioorganic & 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. |
AID663373 | Growth inhibition of human SF295 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1275591 | Inhibition of human recombinant HDAC2 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. |
AID749389 | Inhibition of human recombinant HDAC3 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
AID1697196 | Inhibition of HDAC in human HeLa nuclear extract using fluoroscence-labeled acetylated peptide as substrate by fluorometric assay | 2020 | Bioorganic & 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. |
AID1600661 | Antiproliferative activity against human OE19 cells assessed as reduction in cell viability incubated for 72 hrs by presto blue assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID300832 | Inhibition of HDAC in HeLa cells | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID673998 | Growth inhibition of human HL60 cells after 72 hrs by XTT assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID753166 | Cytotoxicity against human K562 cells | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID618100 | Toxicity 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 22 | 2011 | Journal 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. |
AID1533326 | Inhibition 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 method | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor. |
AID476648 | Therapeutic ratio, EC50 for human PBMC to EC50 for human 937 cells | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1821274 | Inhibition of HDAC8 (unknown origin) incubated for 30 mins by microplate reader assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID525009 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1266819 | Inhibition of HDAC6 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | 2015 | Journal 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. |
AID663394 | Growth inhibition of human MCF10A cells after 48 hrs by MTT assay | 2012 | Journal 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. |
AID1248349 | Inhibition 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 analysis | 2015 | Bioorganic & 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. |
AID1709358 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1855246 | Binding affinity to calf thymus DNA at 50 uM incubated for 30 mins and measured by UV-vis absorption spectroscopy | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1566812 | Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1337292 | Antiproliferative activity against mouse TAMH cells after 24 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1201652 | Antiproliferative activity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1848280 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID622259 | Inhibition of HDAC3 assessed as residual activity at 125 nM after 30 mins by Fluor de Lys fluorescence assay | 2011 | Bioorganic & 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. |
AID1655791 | Inhibition of human recombinant HDAC5 using AMC-K(TFA)GL as substrate by fluorescence based assay | 2020 | ACS 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. |
AID465150 | Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID297492 | Cytotoxicity against human A431 cells | 2007 | Journal 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. |
AID1600730 | Inhibition 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 | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1126991 | Induction 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%) | 2014 | Journal 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. |
AID366643 | Inhibition of HDAC8 after 17 hrs | 2008 | Journal 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. |
AID1454056 | Growth inhibition of human A2780 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1861261 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1401474 | Selectivity ratio of IC50 for HDAC1 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1127010 | Induction 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%) | 2014 | Journal 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. |
AID1890341 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1915551 | Antiproliferative activity against non-small cell lung cancer cell line (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1825804 | Toxicity in ip dosed BALB/c mouse assessed as maximum tolerated dose measured after 2 weeks | 2022 | Journal 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. |
AID350730 | Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID1566825 | Antiproliferative activity against human AML patient derived primary leukemia cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1235112 | Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1280278 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1227029 | Inhibition of human recombinant HDAC1 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1548271 | Induction 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%) | |||
AID1819527 | Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID414720 | Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal 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. |
AID1459945 | Inhibition of HDAC activity in human HeLa cell nuclear extract using fluorometric substrate measured after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1200988 | Oral bioavailability in ICR mouse at 50 mg/kg | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1600728 | Inhibition 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 fo | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID525007 | Inhibition 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 control | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID632971 | Cytotoxicity against human SW620 cells | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1739583 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1336954 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID618181 | Antitumor 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 9 | 2011 | Journal 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. |
AID613295 | Antiproliferative activity against human HCT116 cells assessed as growth inhibition | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1848633 | Cytotoxicity against human UO-31 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1466060 | Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID619260 | Antitumor 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 22 | 2011 | Journal 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. |
AID1686358 | Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay | 2016 | Journal 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. |
AID1292166 | Induction 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 analysis | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Novel spiropyrazolone antitumor scaffold with potent activity: Design, synthesis and structure-activity relationship. |
AID1898908 | Antiproliferative activity against human THP-1 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID605395 | Inhibition of human recombinant HDAC5 using fluor de Lys as substrate by fluorometric analysis | 2010 | Journal 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. |
AID1293571 | Inhibition of human HDAC10 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1826622 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID481569 | Antitumor 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 control | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1227050 | Cytotoxicity against mouse NIH/3T3 cells assessed as cell proliferation after 70 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1739590 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1578484 | Cytotoxicity against human MRC9 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay | 2020 | ACS 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. |
AID1599768 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1421910 | Selectivity index, ratio of IC50 for human HepG2A16 cells to IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1550095 | Inhibition of recombinant human JAK2 at 10 uM using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay | 2019 | Journal 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. |
AID1848281 | Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID1275647 | Cytotoxicity against HEK293 cells assessed as growth inhibition after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID420510 | Cell cycle arrest in human IGROV1 cells assessed as accumulation at sub-G1 phase at IC80 after 24 hrs using propidium-iodide staining by flow-cytometry | 2009 | European 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. |
AID1275639 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID274110 | Inhibition of HDAC1 (mean IC50) | 2006 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23 | A series of novel, potent, and selective histone deacetylase inhibitors. |
AID1915574 | Inhibition 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 mins | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1401541 | Antiproliferative activity against human JeKo1 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1129797 | Inhibition of HDAC in human Jurkat cells assessed as perforin expression after 48 hrs by FACS flow cytometric analysis relative to control | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1355691 | Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay | 2018 | Journal 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. |
AID1282298 | Inhibition 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 analysis | 2016 | Journal 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. |
AID1421625 | Antiproliferative activity against human HEL 92.1.7 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1865251 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SHP099 by CCK-8 assay | 2022 | Journal 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. |
AID765206 | Cytotoxicity against human H69 cells | 2013 | Bioorganic & 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. |
AID619042 | Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay | 2011 | Journal 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. |
AID1128555 | Inhibition of human HDAC-2 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1280306 | Inhibition of human KDAC1 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1623527 | Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1379289 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2017 | ACS 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. |
AID1704066 | Inhibition 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 method | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID461268 | Antiproliferative activity against human SCC25 cells | 2010 | Journal 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. |
AID1769655 | Antiproliferative activity against human SKNBE2 cells harboring wild type ALK assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1633676 | Neuroprotective 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 MT | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1337280 | Antiproliferative activity against human Jurkat cells | 2016 | Journal 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. |
AID1875508 | Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID1464875 | Anti-proliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID375039 | Toxicity in ip dosed BALB/c nu/nu mouse assessed as maximum tolerated dose | 2009 | Journal 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. |
AID1339578 | Inhibition 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 method | 2017 | ACS 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. |
AID1614253 | Antitumor 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 | |||
AID1655896 | Inhibition 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) | 2020 | ACS 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. |
AID1752942 | Selectivity 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 | |||
AID1486324 | Genotoxicity in Salmonella typhimurium TA1535 at 50 times antiproliferative IC50 by Ames test | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1511139 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID322420 | Cell cycle arrest in human LNCap cells assessed as accumulation at G2/M phase relative to control at 1 uM | 2008 | Bioorganic & 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. |
AID1441645 | Anti-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 hrs | 2017 | Journal 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. |
AID1215095 | Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay relative to SR12813 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1690103 | Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID1462221 | Inhibition of recombinant human HDAC1 after 30 mins by fluorescence assay | 2017 | Bioorganic & 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. |
AID1128556 | Inhibition of human HDAC-3/NCOR-2 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID347808 | Inhibition of human HDAC1 | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1535340 | Inhibition 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 assay | 2019 | Bioorganic & 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. |
AID546546 | Inhibition of HDAC assessed as histone H3K'9+14 acetylation levels by cell based histone H3 hyperacetylation assay | 2010 | Journal 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. |
AID105421 | Inhibitory concentration against MDA-435 cells proliferation | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Histone deacetylase inhibitors. |
AID1248354 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID1263143 | Antagonist activity at ERalpha in human T47D-KBLuc cells assessed as inhibition of E2-induced transcriptional activity by luciferase reporter gene assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID1066166 | Cytotoxicity against human LNCAP cells at 50 uM after 72 hrs | 2014 | Journal 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. |
AID1897384 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID1503842 | Selectivity 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 cells | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models. |
AID1742745 | Genotoxicity in Salmonella typhimurium WP2 uvrA (pKM 101) by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1383991 | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1454679 | Decrease in alcohol intake in C57BL/6J mouse at 50 mg/kg, ip relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
AID1487017 | Inhibition of HDAC3 in human U937 cells assessed as increase in acetylated-histone H3 level at 5 uM incubated for 18 hrs by Western blot method | 2017 | Bioorganic & 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. |
AID527321 | Growth inhibition of human HUT78 cells after 72 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases. |
AID1434357 | Growth inhibition of human NCI-H23 cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1821961 | Inhibition 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 | |||
AID1849166 | Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1547256 | Inhibition of human recombinant His-tagged BRDT BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1885254 | Inhibition of KDM4E (unknown origin) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID1832688 | Inhibition of human HDAC4 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID637887 | Inhibition of Bordetella FB188 HDAH using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | 2012 | Bioorganic & 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. |
AID1164034 | Inhibition of human recombinant HDAC11 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1677495 | induction 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 analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1165105 | Antileishmanial activity against axenic amastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1707466 | Synergistic 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) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID420638 | Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC80 after 24 hrs by Western blot | 2009 | European 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. |
AID1065635 | Inhibition of human recombinant HDAC9 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1529549 | Induction 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%) | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1819546 | Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as fold increase in CD86 expression by flow cytometry analysis relative to control | 2022 | Journal 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. |
AID1578903 | Induction of apoptosis in human Bel7402 cells assessed as increase in cleaved caspase-3 level at 5 uM after 72 hrs by Western blot analysis | 2019 | Journal 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. |
AID1401555 | Antiproliferative activity against human MM473 cells at 10 uM after 72 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID481567 | Antitumor 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 days | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1653098 | Antiproliferative activity against human PC3 cells by CCK8 assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1266811 | Antiproliferative activity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1775564 | Inhibition of full length human C-terminal His-tagged HDAC2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | 2021 | Journal 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 |
AID1250643 | Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1380968 | Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis | 2018 | Journal 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. |
AID1380949 | Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1873384 | Inhibition of HDAC4 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID373084 | Antitumor 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 postxenografting | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1441649 | Anti-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 method | 2017 | Journal 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. |
AID1280277 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1898904 | Antiproliferative activity against human L-428 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID274037 | Hepatocyte stability | 2007 | Bioorganic & 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. |
AID90680 | Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor | 2004 | Journal 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. |
AID1727731 | Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1709353 | Selectivity ratio of IC50 for human HCT-116 cells to IC50 for human Jurkat cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1865242 | Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID352518 | Inhibition of human recombinant HDAC6 | 2009 | Bioorganic & 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. |
AID1702089 | Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID613340 | Antiproliferative activity against human H1299 cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1697200 | Inhibition of HDAC2 (unknown origin) | 2020 | Bioorganic & 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. |
AID1865244 | Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID343690 | Inhibition of HDAC in human HeLa cells | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles. |
AID1401554 | Antiproliferative activity against human MM432 cells at 10 uM after 72 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1234891 | Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1591853 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID540212 | Mean residence time in human after iv administration | 2008 | Drug 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. |
AID1413071 | Antiproliferative activity against human SKOV3 cells at 10 uM measured every 2 hrs for 200 hrs by IncuCyte ZOOM cell confluence assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition. |
AID1864219 | Binding affinity to 5' FAM-labeled c-myc G4-quadruplex DNA Pu22 (unknown origin) at 50 uM by fluorescence quench assay | 2022 | Journal 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. |
AID1707464 | Antifungal activity against Candida albicans 0304103 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID1326519 | Inhibition 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 analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1702061 | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay | 2018 | Journal 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. |
AID1811362 | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID545890 | Specificity index, ratio for IC50 for human HDAC in HeLa cells to IC50 for HDAC in Plasmodium falciparum 3D7 | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1543951 | Induction 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%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1861262 | Inhibition of HDAC8 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID482965 | Apparent permeability from apical to basolateral side of Caco-2 cells | 2010 | Bioorganic & 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. |
AID1415657 | Binding affinity to calf thymus DNA assessed as decrease in maximum absorption wavelength by UV-Vis spectroscopic titration method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1764256 | Induction of histone H-3 expression in human CAL-27 cells for 24 hrs by Western blot analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1469310 | Induction 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%) | 2018 | Journal 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 |
AID1548261 | Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay | |||
AID1336927 | Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1126963 | Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC3 (unknown origin) | 2014 | Journal 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. |
AID1697203 | Induction of apoptosis in human SW620 cells assessed as early apoptotic cells by flow cytometry | 2020 | Bioorganic & 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. |
AID134163 | Antitumor activity against HT1080 cell line in mouse xenograft model after orally dosed once every other day at 100 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
AID1542185 | Inhibition of HDAC7 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1873409 | Inhibition of HDAC3 (unknown origin) preincubated for 5 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1873408 | Inhibition of HDAC2 (unknown origin) preincubated for 120 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID669759 | Growth inhibition of human PC3 cells after 48 hrs by SRB assay | 2012 | Journal 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. |
AID1073051 | Reactivation 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 analysis | 2014 | Journal 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. |
AID1688036 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1742685 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1702063 | Inhibition 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 assay | 2018 | Journal 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. |
AID1060990 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors. |
AID1141770 | Cytotoxicity against human TSGH cells by MTT assay | 2014 | Journal 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. |
AID1177047 | Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID300835 | Growth inhibition of human NCI-H23 cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID438216 | Inhibition of HDAC1/2 from human HeLa cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide. |
AID605541 | Antiproliferative activity against human U937 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1164031 | Inhibition of human recombinant HDAC9 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1898981 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID723463 | Inhibition of human HDAC5 by fluorescence assay | 2013 | Journal 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. |
AID1605969 | Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1251322 | Growth inhibition of human H460 cells after 72 hrs | 2015 | Bioorganic & 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. |
AID1518780 | Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1848623 | Cytotoxicity against human HT-29 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID591326 | Inhibition of HDAC in human HeLa cells at 0.1 uM by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors. |
AID1547260 | Inhibition of human recombinant His-tagged BRD3 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1348936 | Effect on TIMP3 gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1401484 | Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1861259 | Inhibition of HDAC3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1384232 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level after 2 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1401373 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1127318 | Inhibition of HDAC2 in human HeLa cells using KI-104 as substrate after 40 mins by fluorescence analysis | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1126988 | Inhibition of HDAC3 in human U937 cells assessed as increase of intracellular acetylated histone H4 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal 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. |
AID1067346 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1704069 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID1821957 | Inhibition of HDAC in human HeLa nuclear extracts using fluorometric substrate incubated for 30 mins by fluorescence plate reader analysis | |||
AID1478600 | Inhibition 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 analysis | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1622977 | Inhibition 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 min | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1915572 | Inhibition of EGFR (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID288453 | Growth inhibition of human MDA-MB-231 cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID1246526 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human U937 cells | 2015 | Bioorganic & 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. |
AID1487013 | Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC8 (unknown origin) | 2017 | Bioorganic & 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. |
AID1282290 | Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as death at 50 mg/kg, ip q2d for 12 days | 2016 | Journal 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. |
AID1751996 | Inhibition of HDAC8 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. |
AID366648 | Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1260646 | Inhibition of human recombinant HDAC10 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1260639 | Inhibition of human recombinant HDAC3 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1550126 | Induction 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%) | 2019 | Journal 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. |
AID1754768 | Downregulation of SIRT1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID373082 | Inhibition of human recombinant HDAC9 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1898979 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1129008 | Inhibition of human HDAC-6 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1466063 | Inhibition of recombinant human full length HDAC6 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID482958 | Half life in mouse liver microsome | 2010 | Bioorganic & 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. |
AID1547246 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1848634 | Cytotoxicity against human Hs578Bst cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1901161 | Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1164770 | Antitumor 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 weeks | 2014 | Journal 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. |
AID1141798 | Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2014 | Journal 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. |
AID404451 | Antimalarial activity against Plasmodium falciparum TM90C2A by hypoxanthine uptake | 2008 | Journal 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. |
AID1326512 | Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID734728 | Inhibition of HDAC6 in human LNCAP cells assessed as increase in tubulin polymerization after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1349724 | Inhibition of HDAC2 (unknown origin) | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID615999 | Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors. |
AID1784969 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1826632 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1742648 | Induction of apoptosis in human MDA-MB-231 cells xenografted in BALB/c mouse assessed as increase in caspase-3 cleavage by immunohistochemistry method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1731758 | Inhibition 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 assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates. |
AID1873412 | Inhibition of HDAC3 (unknown origin) preincubated for 90 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1181306 | Inhibition of HDAC1 in human U937 cells assessed as increase in acetyl-histone H3 level at 5 uM by Western blotting method | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID1225987 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1225989 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID765377 | Inhibition of recombinant human HDAC5 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate at 50 uM after 15 to 30 mins | 2013 | Journal 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. |
AID1206743 | Cytotoxicity against human ES2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID605539 | Antiproliferative activity against human MOLT4 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID274069 | Bioavailability after i.p. dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID672032 | Ratio of IC50 for human HDAC1 preincubated for 3 hrs to IC50 for human HDAC1 preincubated for 5 mins | 2012 | Bioorganic & 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. |
AID1449322 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID366650 | Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID80246 | Inhibitory activity against HCT116 human colon cell growth | 2003 | Journal 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). |
AID1699974 | Inhibition of recombinant human HDAC8 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2020 | Bioorganic & 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. |
AID1737153 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1861252 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 7 days | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID1056037 | Antiproliferative activity against human A549 cells after 48 hrs | 2013 | Journal of natural products, Nov-22, Volume: 76, Issue:11 | Total synthesis of schizocommunin and revision of its structure. |
AID1164175 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1250653 | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay | 2015 | Journal 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. |
AID1162218 | Cell 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%) | 2014 | Bioorganic & 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. |
AID1389960 | Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. |
AID1234900 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1266835 | Induction of caspase-3 cleavage in human HCT116 cells at 1 to 5 uM after 48 hrs by western blot analysis | 2015 | Journal 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. |
AID1737135 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID519583 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID382343 | Viability of human DU145 cells after 72 hrs by trypan blue staining | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group. |
AID90520 | Inhibition of in vitro enzyme activity measured in partially purified rat liver Histone deacetylase preparation | 2002 | Journal 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. |
AID1281854 | Antiproliferative activity against human LP-1 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1542179 | Inhibition of HDAC1 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1762492 | Inhibition 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 | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1401533 | Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1821959 | Inhibition 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 | |||
AID1848566 | Ratio of IC50 for cytotoxicity against human RPE cells to IC50 for cytotoxicity against human HCT-116 cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1898924 | Antiproliferative activity against human NCI-H460 cells at 7.4 uM assessed as reduction in p-ERK1/2 level and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID90665 | Inhibitory activity against human Histone deacetylase 1 | 2004 | Journal 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. |
AID1915525 | Antiproliferative activity against human PC-3 cells incubated for 48 hrs by Sulforhodamine B staining method | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID760520 | Cytotoxicity against human SK-BR-3 cells after 72 hrs by WST1 assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1282232 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2016 | Journal 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. |
AID1384234 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1449217 | Inhibition 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 assay | 2017 | Journal 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. |
AID1898982 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID473029 | Ex vivo inhibition of human HDAC1 in human Caco-2 cells by fluorometric cellular activity assay | 2010 | Journal 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. |
AID1549139 | Antifungal activity against azole-resistant Candida albicans 4108 after 48 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID525022 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in total CFTR protein level including CFTR glycoform at 0.1 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1901765 | Selectivity ratio of IC50 for full length human recombinant HDAC8 to IC50 for full length human recombinant HDAC6 | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1550150 | Antitumor 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 control | 2019 | Journal 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. |
AID1848592 | Induction 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1459955 | Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1459956 | Selectivity ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC6 | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1742758 | In 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 method | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1832684 | Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1401591 | Resistance index, ratio of IC50 for human A2780/DX cells to IC50 for human A2780 cells | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID618184 | Toxicity 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 13 | 2011 | Journal 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. |
AID1055355 | Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay | 2013 | Journal 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. |
AID723154 | Potentiation 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 assay | 2013 | Journal 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. |
AID90672 | Inhibitory activity against maize Histone deacetylase 1-B | 2003 | Journal 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. |
AID1548727 | Inhibition 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 analysis | 2020 | Journal 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. |
AID765204 | Cytotoxicity against human Hep3B cells | 2013 | Bioorganic & 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. |
AID273180 | Cell cycle arrest in U937 cells by accumulation at S/G2/M phase at 5 uM after 48 hrs | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID663474 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM | 2012 | Journal 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. |
AID1260640 | Inhibition of human recombinant HDAC4 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID328797 | Inhibition of HDAC4 gain-of-function phenotype expressed in Escherichia coli | 2008 | Journal 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. |
AID1139706 | Inhibition of HDAC in human HeLa cell nuclear extract using acetylated lysine as substrate after 30 mins by spectrophotometric analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives. |
AID1067344 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1765322 | Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1454681 | Decrease in alcohol intake in C57BL/6J mouse at 100 mg/kg, ip relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
AID1548275 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay | |||
AID1811393 | Toxicity 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 analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID1282277 | Antitumor activity against human HCT116 cells xenografted in Balb/c nude mouse assessed as tumor mass change at 50 mg/kg, ip q2d for 9 days | 2016 | Journal 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. |
AID1250642 | Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1141767 | Cytotoxicity against human HONE1 cells by MTT assay | 2014 | Journal 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. |
AID663363 | Growth inhibition of human IGROV1 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1777025 | Inhibition 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 cytometry | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase. |
AID481570 | Antitumor 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 control | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID273173 | Inhibition of mouse HDAC1 | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1251315 | Inhibition of human HDAC2 after 40 mins by fluorescence analysis | 2015 | Bioorganic & 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. |
AID1783092 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1699971 | Resistance index, ratio of of IC50 for human K562/A02 cells to IC50 for human K562 cells | 2020 | Bioorganic & 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. |
AID603530 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1514600 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID1549164 | Inhibition of HDAC1 (unknown origin) after 30 mins by fluorescence based assay | 2020 | Journal 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. |
AID1819517 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID1856995 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID1266834 | Induction of PARP cleavage in human HCT116 cells at 1 to 5 uM after 48 hrs by western blot analysis | 2015 | Journal 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. |
AID1398808 | Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin expression after 8 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID316873 | Inhibition of human HT1080 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1821960 | Inhibition 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 | |||
AID316925 | Inhibition of human HepG2 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1168915 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1274880 | Inhibition of HDAC10 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1653144 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID331900 | Displacement 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 assay | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID1833070 | Antiangiogenesis activity in human Endothelial progenitor cell assessed as inhibition of cell growth measured for 48 hrs | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID1861651 | Antiproliferative activity against human A549 cells measured after 72 hrs | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1337308 | Inhibition 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 method | 2016 | Journal 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. |
AID1406989 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1482123 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1707467 | Synergistic 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 assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID1888588 | Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay | |||
AID395031 | Toxicity in ip dosed athymic mouse assessed as maximum tolerated dose | 2009 | Bioorganic & 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. |
AID1263061 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID1707508 | Inhibition of human HDAC6 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
AID1566815 | Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID619053 | Competitive inhibition of HDAC8 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1688041 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1206751 | Cell 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%) | 2015 | Journal 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. |
AID1550106 | Inhibition 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 analysis | 2019 | Journal 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. |
AID1266100 | Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA | 2016 | Bioorganic & 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. |
AID723468 | Inhibition of HDAC in cisplatin sensitive human KYSE-510 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1280260 | Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID456798 | Antimalarial 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 method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID755621 | Cytotoxicity against human GBC-SD cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID1269325 | Cytotoxicity against human A549 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID775831 | Inhibition of HDAC2 (unknown origin)-mediated deacetylation at 10 uM preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1622932 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID461263 | Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1065971 | Inhibition of HDAC1 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID499803 | Selectivity ratio IC50 for HDAC6 to IC50 for HDAC in human HeLa cells nuclear extract | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1379285 | Inhibition 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 analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors. |
AID1819532 | Toxicity 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 analysis | 2022 | Journal 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. |
AID609494 | Inhibition of CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1398812 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1547284 | Effect on histone H3 expression level in human HCT116 cells measured after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1861342 | Inhibition of HDAC in human DOHH-2 cells assessed as effect on pS6 levels at 2.5 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID527040 | Cytotoxicity against human NCI-H1299 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1765332 | Selectivity 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 HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1558002 | Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay | 2019 | Journal 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. |
AID1811392 | Toxicity 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 fulvestrant | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID755618 | Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID1441643 | Anti-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 hrs | 2017 | Journal 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. |
AID273176 | Induction of granulocytic differentiation of U937 cells measured as CD11c expression level after 48 hrs at 1 uM | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1394884 | Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1401538 | Antiproliferative activity against human A2780/DX cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1572344 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1275635 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID324950 | Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID1775565 | Inhibition 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 assay | 2021 | Journal 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 |
AID1399813 | Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay | 2018 | Bioorganic & 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. |
AID1431822 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1466066 | Inhibition of HDAC in human PC3 cells assessed as increase in alpha-tubulin acetylation at 1 uM after 24 hrs by Western blot analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1863435 | Inhibition of HDAC3 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID723433 | Potentiation 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 assay | 2013 | Journal 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. |
AID1330944 | Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1547333 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1439350 | Inhibition 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 hrs | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID316927 | Inhibition of human CCD1059SK cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID499809 | Antimalarial activity against Plasmodium falciparum D6 after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID669756 | Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader | 2012 | Journal 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. |
AID90696 | Inhibition of maize histone deacetylase 2 | 2004 | Journal 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. |
AID1127006 | Induction 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%) | 2014 | Journal 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. |
AID1164177 | Cell 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 cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1622985 | Inhibition of HDAC6 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID748981 | Inhibition of HDAC6 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1819548 | Antitumor 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 control | 2022 | Journal 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. |
AID618016 | Antitumor 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 control | 2011 | Journal 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. |
AID1633426 | Cytotoxicity against human SH-SY5Y cells at 10 uM incubated for 24 hrs by MTS assay | 2019 | ACS 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. |
AID274095 | Inhibition of mouse HDAC1 (mean) | 2007 | Bioorganic & 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. |
AID663402 | Lipophilicity, log D of the compound in pH 7.4 PBS buffer | 2012 | Journal 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. |
AID723147 | Potentiation 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 assay | 2013 | Journal 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. |
AID1282302 | Inhibition 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 analysis | 2016 | Journal 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. |
AID1754764 | Downregulation of HDAC7 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID723464 | Inhibition of human HDAC4 by fluorescence assay | 2013 | Journal 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. |
AID1550119 | Induction 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%) | 2019 | Journal 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. |
AID1281855 | Antiproliferative activity against human Mino cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1177046 | Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1129790 | Induction 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1451830 | Inhibition 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 assay | 2017 | Journal 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. |
AID1754790 | Downregulation of HDAC8 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1898910 | Antiproliferative 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 assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1846147 | Inhibition of HDAC (unknown origin) incubated for 30 mins by ELISA method | 2021 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 38 | Current status in the discovery of dual BET/HDAC inhibitors. |
AID499810 | Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID420639 | Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC80 after 48 hrs by Western blot | 2009 | European 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. |
AID1784979 | Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1141765 | Cytotoxicity against human HCT116 cells by MTT assay | 2014 | Journal 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. |
AID1720111 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability in presence of erlotinib by MTT assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID1759726 | Fraction unbound in rat plasma | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction. |
AID1482170 | Cytotoxicity against human Caco2 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1550101 | Inhibition 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 assay | 2019 | Journal 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. |
AID1890512 | Inhibition of HDAC3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1467235 | Inhibition 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 fluorom | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID503691 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1771457 | Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID519597 | Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-resistant Plasmodium falciparum Dd2 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1469298 | Induction 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%) | 2018 | Journal 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 |
AID1572353 | Ratio 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 uM | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1421914 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1890321 | Inhibition of HDAC1 in mouse B16 cells assessed as accumulation of acetylated H3 level at 6 uM after 24 hrs by Western blotting analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID541648 | Inhibition of human HDAC4 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1869147 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | |||
AID352521 | Antiproliferative activity against human BxPC3 cells by MTT assay | 2009 | Bioorganic & 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. |
AID1164903 | Inhibition 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-275 | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1605967 | Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1622933 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID461265 | Antiproliferative activity against human MDA-MB-468 cells | 2010 | Journal 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. |
AID1655900 | Inhibition 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) | 2020 | ACS 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. |
AID1758463 | Phototoxicity 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 assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID395023 | Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter assay | 2009 | Bioorganic & 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. |
AID1855253 | Downregulation of SSRP-1 expression in human HCT-116 cells at 1.5 uM measured after 24 hrs by Western blot analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID461301 | Antitumor activity against human HepG2 cells xenografted in nude CD1 mouse at 72 mg/kg, iv daily relative to control | 2010 | Journal 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. |
AID1380939 | Inhibition of VEGFR-2 (unknown origin) at 0.2 uM after 40 mins by kinase-Glo assay relative to control | 2018 | Journal 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. |
AID1543957 | Induction 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%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1762491 | Inhibition 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 | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1396990 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors. |
AID1126983 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1462025 | Antiproliferative activity against human U266 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. |
AID1758468 | Inhibition of human recombinant HDAC6 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1702139 | Inhibition 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 %) | 2018 | Journal 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. |
AID1901766 | Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1865268 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1441658 | Anti-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 hrs | 2017 | Journal 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. |
AID465155 | Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID723469 | Inhibition of HDAC in cisplatin resistant human CAL27 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1677517 | Binding 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1174699 | Induction 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%) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID618024 | Inhibition of MMP2 | 2011 | Journal 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. |
AID1825881 | Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay | |||
AID274022 | AUC after i.p. dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1256444 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1785347 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1816698 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability at 10 uM after 72 hrs by CellTiter-Glo assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1667066 | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1783109 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
AID1897806 | Inhibition 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 analysis | 2022 | Journal 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. |
AID1282237 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1394883 | Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID481548 | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1164908 | Inhibition of HDAC3 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1742679 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1890436 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay | 2022 | Bioorganic & medicinal chemistry, 04-15, Volume: 60 | Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones. |
AID1606020 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 1 to 2 uM after 72 hrs by tryphan blue assay | 2020 | Journal 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. |
AID310127 | Growth inhibition of human HCT116 cells by SRB assay | 2007 | Bioorganic & 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. |
AID1365024 | Inhibition 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 assay | 2017 | Bioorganic & 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. |
AID303349 | Inhibition of HDAC6 in presence of DTT | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. |
AID1441646 | Anti-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 hrs | 2017 | Journal 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. |
AID1869149 | Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | |||
AID1690843 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1545756 | Inhibition of HDAC3 (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Indole: A privileged scaffold for the design of anti-cancer agents. |
AID1753646 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1227033 | Inhibition of human recombinant HDAC8 using MAZ1675 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID316934 | Inhibition of HDAC4 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1459957 | Selectivity ratio of IC50 for recombinant human HDAC2 to IC50 for recombinant human HDAC6 | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1177044 | Inhibition of human HDAC3 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1337196 | Inhibition 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 assay | 2016 | Journal 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. |
AID1897381 | Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID1128563 | Inhibition of human HDAC-11 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1201647 | Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
AID1275077 | Inhibition of recombinant human HDAC1 | 2016 | Bioorganic & 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. |
AID1164188 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1545944 | Antiproliferative activity against human K562 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1572350 | Inhibition of HDAC in human HL60 cells assessed as acetylated H3/GAPDH ratio at 10 uM after 4 hrs by Western blot assay relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID546559 | Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay | 2010 | Journal 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. |
AID1336940 | Inhibition of HDAC in human LNCAP cells assessed as down regulation of COX2 expression at 10 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1764253 | Inhibition 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 fluorimetry | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1282243 | Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1622984 | Inhibition of HDAC2 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1566814 | Antiproliferative activity against human A2780S cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1614247 | Inhibition of HDAC6 in human MV4-11 cells assessed as increase in alpha-tubulin acetylation at 1 uM after 6 hrs by Western blot analysis | |||
AID1752947 | Selective 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 | |||
AID348804 | Antiproliferative activity against human HCT116 cells after 72 hrs by celltiter-blue viability assay | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID297491 | Cytotoxicity against human Cal27 cells | 2007 | Journal 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. |
AID1422520 | Inhibition of HDAC in human HeLa cell extract at 2 uM after 15 to 30 mins by COLOR DE LYS-based colorimetric method | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID525001 | Inhibition of HDAC2 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID503668 | Cytotoxicity against human GM15850 cells at 5 uM after 96 hrs by trypan blue exclusion assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1515917 | Antitumor 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 control | 2019 | Journal 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. |
AID1671981 | Cytotoxicity against human MCF7/ADR cells after 72 hrs by SRB assay | 2019 | Bioorganic & 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. |
AID499813 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W2 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1600734 | Antiproliferative activity against human A2780 cells after 72 hrs by microplate reader based MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
AID1065633 | Inhibition of human recombinant full length HDAC6 after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1406987 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1550128 | Induction 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%) | 2019 | Journal 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. |
AID750106 | Cytotoxicity against human MCF7 cells after 48 hrs by Sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID1816201 | Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | |||
AID1688032 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1282256 | Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1897379 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID1225975 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1349726 | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1784986 | Inhibition of HDAC2 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1246515 | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1511137 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1464871 | Inhibition of HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID663376 | Growth inhibition of human SNB75 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1434355 | Growth inhibition of human ACHN cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1759721 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction. |
AID1293554 | Inhibition of human recombinant HDAC2 using Fluor de Lys Green as substrate incubated for 30 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1917542 | Inhibition of HDAC11 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID672025 | Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 24 hrs measured after 35 mins by spectrofluorometric analysis | 2012 | Bioorganic & 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. |
AID1478583 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1406986 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1537569 | Cell 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 %) | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1897403 | Induction 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%) | |||
AID482943 | Inhibition of HDAC3 | 2010 | Bioorganic & 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. |
AID1321713 | Inhibition 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 control | 2016 | Journal 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. |
AID1245684 | Cytotoxicity against human U937 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID652755 | Inhibition of recombinant human HDAC11 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1280284 | Cytotoxicity against human HL60 cells after 72 hrs by cell titre 96 aqueous cell proliferation assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID723432 | Potentiation 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 assay | 2013 | Journal 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. |
AID1251320 | Growth inhibition of human HCT116 cells after 72 hrs | 2015 | Bioorganic & 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. |
AID1274874 | Inhibition of HDAC4 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID496808 | Activity of human HDAC8 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1348935 | Effect on TNFalpha gene expression in human PC3 cells at IC50 after 12 hrs by RT-PCR method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID481553 | Cytotoxicity against human KB cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1485111 | Inhibition 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 control | 2017 | Journal 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. |
AID488239 | Inhibition of HDAC6 after 10 mins by fluorometric assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID1873399 | Inhibition of HDAC1 (unknown origin) preincubated for 5 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1548249 | Inhibition 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 | |||
AID288447 | Inhibition of LPS-stimulated TNFalpha production in RAW264.7 cells after 24 hrs by ELISA | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID1280264 | Selectivity ratio of IC50 for human HDAC6 to IC50 for human HDAC8 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID628450 | Induction of apoptosis in human HepG2 cells assessed as cleavage of caspase 3 at 1 to 10 uM after 14 hrs by Western blot analysis | 2011 | Journal 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. |
AID1728925 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 5 days by beckman coulter counting method | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones. |
AID1380950 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1876340 | Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID1174702 | Induction 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%) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1478595 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1576451 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID663349 | Growth inhibition of human A549/ATCC cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1260653 | Inhibition of human recombinant HDAC1 by microplate reader assay | |||
AID1622938 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1848613 | Cytotoxicity against human LOX IMVI cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1810049 | Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay | |||
AID1206766 | Inhibition 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 assay | 2015 | Journal 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. |
AID1709365 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1816193 | Inhibition 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 | |||
AID663364 | Growth inhibition of human OVCAR3 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1401539 | Antiproliferative activity against human Mino cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID352751 | Inhibition of His-tagged HDAC8 catalytic domain expressed in Escherichia coli | 2009 | Bioorganic & 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. |
AID1330945 | Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1383995 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1652197 | Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1401375 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1449326 | Inhibition 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID744876 | Cytotoxicity against human NCI-H460 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Discovery of adamantane based highly potent HDAC inhibitors. |
AID621738 | Antiproliferative activity against human HCT116 cells by MTT assay | 2011 | Bioorganic & 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. |
AID628448 | Induction of apoptosis in human HepG2 cells assessed as cleavage of caspase 3 at 1 to 10 uM after 24 hrs by Western blot analysis | 2011 | Journal 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. |
AID1566811 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID605534 | Antiproliferative activity against human MG63 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1266820 | Inhibition of HDAC8 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | 2015 | Journal 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. |
AID300837 | Growth inhibition of human LOX-IMVI cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID755625 | Inhibition 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 assay | 2013 | Bioorganic & 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. |
AID1897383 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
AID1623530 | Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2A by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID732151 | Inhibition of HDAC8 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1280263 | Selectivity ratio of IC50 for human HDAC6 to IC50 for human HDAC1 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1355730 | Toxicity 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 days | 2018 | Journal 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. |
AID717657 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID747260 | Growth inhibition of human HT1080 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1225985 | Inhibition 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 assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID594123 | Inhibition of full length HDAC3/NCoR2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Discovery of histone deacetylase 8 selective inhibitors. |
AID1396958 | Antiproliferative activity against human MDA-MB-231 cells | 2018 | Bioorganic & 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). |
AID1396986 | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors. |
AID1630589 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTS-PMS assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1548274 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay | |||
AID775827 | Binding 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 analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
AID1783065 | Antifungal activity against fluconazole-sensitive Candida albicans SC5314 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1515907 | Antiproliferative activity against human U87 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1578481 | Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay | 2020 | ACS 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. |
AID1856997 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID1164190 | Inhibition of HDAC in human U937 cells assessed as hyperacetylation of p21 at 5 uM after 24 hrs by Western blot analysis relative to control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1380953 | Inhibition 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 assay | 2018 | Journal 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. |
AID1441660 | Inhibition of LTB4 biosynthesis in LPS-induced C57BL/6 mouse model of acute lung injury BLAF at 25 mg/kg, ip by ELISA | 2017 | Journal 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. |
AID1548285 | Induction 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%) | |||
AID1816220 | Induction 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%) | |||
AID1742748 | Antitumor 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 22 | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID373083 | Antiproliferative activity against human HeLa cells after 4 hrs by WST-1 assay | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1263144 | Inhibition of human recombinant HDAC3 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
AID1534485 | Inhibition of HDAC6 in mouse LL/2 cells assessed as reduction in PD-L1 expression at 10 uM after 24 hrs by Western blot analysis | 2019 | Journal 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. |
AID1819500 | Antitumor 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 days | 2022 | Journal 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. |
AID373087 | Antitumor 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 postxenografting | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID1890435 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay | 2022 | Bioorganic & medicinal chemistry, 04-15, Volume: 60 | Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones. |
AID1181314 | Induction 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 method | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID1882978 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer. |
AID492802 | Inhibition of human recombinant HDAC4 at 5 uM after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID1821348 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1126977 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1737145 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1622981 | Cytotoxicity against African green monkey Vero cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1754774 | Induction 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1282261 | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1784991 | Selectivity index, ratio of IC50 for cytotoxicity against human L02 cells to IC50 for antiproliferative activity against human HepG2 cells | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID414721 | Inhibition of wild-type c-Abl by liquid scintillation counting | 2009 | Journal 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. |
AID1384215 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1502984 | Inhibition of MAOB (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1339571 | Inhibition 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 ELISA | 2017 | ACS 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. |
AID1785343 | Inhibition of recombinant human SIRT5 measured after 30 mins by fluorescence microplate reader assay | |||
AID1876465 | Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1622936 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID84266 | Antiproliferative activity against HT1080 (human fibrosarcoma) cell line. | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
AID1865240 | Induction of apoptosis in human MV4-11 cells incubated for 24 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry | 2022 | Journal 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. |
AID1597953 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1849157 | Inhibition 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 analysis | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1422515 | Inhibition of HDAC in MEF assessed as increase in histone H3 acetylation at 2 uM after 6 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways. |
AID1256443 | Inhibition of human HDAC in HeLa cell nuclear extract by fluorometric assay using Fluor de Lys substrate | 2015 | Bioorganic & 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. |
AID637891 | Inhibition of recombinant human HDAC8 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay | 2012 | Bioorganic & 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. |
AID1227044 | Stability in human plasma assessed as compound remaining after 2 hrs by HPLC analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID753167 | Inhibition of HDAC in human Hela cell nuclear extract after 15 mins | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors. |
AID1753833 | Inhibition of recombinant human HDAC1 at 100 nM using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay relative to control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1266091 | Cytotoxicity against human MeT-5A cells | 2016 | Bioorganic & 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. |
AID1702103 | Inhibition 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 analysis | 2018 | Journal 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. |
AID755616 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & 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. |
AID316904 | Inhibition of human NCI-H226 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1816215 | Induction 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%) | |||
AID1478597 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID525014 | Inhibition 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 analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1502980 | Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1063057 | Inhibition of recombinant HDAC2 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1917543 | Selectivity index, ratio IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID1487092 | Inhibition of HDAC1 (unknown origin) | 2017 | Bioorganic & 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. |
AID519582 | Antimalarial activity against Plasmodium falciparum | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1272258 | Cytotoxicity against human MCF7 cells after 72 hrs by CCK8 assay | 2016 | Bioorganic & 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. |
AID1676602 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1469379 | Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID1754789 | Downregulation of HDAC3 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID316899 | Inhibition of HDAC6 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1380967 | Inhibition of HDAC6 in human HeLa cells assessed as increase in intracellular acetyl-tubulin levels at 100 nM after 6 hrs by Western blot analysis | 2018 | Journal 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. |
AID273166 | Inhibition of maize HD2 | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID780585 | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. |
AID1174680 | Inhibition 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 assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID546561 | Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay | 2010 | Journal 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. |
AID710835 | Cytotoxicity against human HCT15 cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID1764288 | Inhibition 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) | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1303622 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1406990 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID1684872 | Toxicity 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) | |||
AID628453 | Antiproliferative activity against human SH-SY5Y cells after 72 hrs by XTT assay | 2011 | Journal 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. |
AID347806 | Inhibition of human HDAC1 at 0.50 uM | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1383990 | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1418666 | Inhibition of recombinant human HDAC6 using fluorogenic HDAC substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence analysis | 2018 | Bioorganic & 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. |
AID1597969 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID519598 | Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID663369 | Growth inhibition of human SKOV3 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1055351 | Cytotoxicity against human HUT78 cells after 72 hrs by MTS-PMS assay | 2013 | Journal 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. |
AID1873391 | Inhibition of HDAC11 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1677510 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID482949 | Inhibition of HDAC10 | 2010 | Bioorganic & 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. |
AID1614190 | Induction 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%) | |||
AID1421925 | Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1273874 | Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM preincubated for 10 mins measured after 30 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1502982 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1355716 | Synergistic antifungal activity against FLC resistant Candida albicans 0710922 assessed as FIC index after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1486675 | Inhibition 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 analysis | 2017 | Bioorganic & 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. |
AID1487007 | Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID1363799 | Inhibition 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 assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID378556 | Induction of P21WAF1 gene expression in human ARP1 cells | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | 4-Hydroxybenzoyl derivative from the aqueous extract of the hydroid Campanularia sp. |
AID1056038 | Antiproliferative activity against human HeLa cells after 48 hrs | 2013 | Journal of natural products, Nov-22, Volume: 76, Issue:11 | Total synthesis of schizocommunin and revision of its structure. |
AID1433251 | Antiproliferative activity against human CMS cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID619058 | Half life in mouse liver microsomes | 2011 | Journal 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. |
AID1065957 | Cytotoxicity against human Jurkat gamma1 cells assessed as growth inhibition at 20 uM after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID1126965 | Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2014 | Journal 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. |
AID1486293 | Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1578149 | Inhibition of HDAC1 (unknown origin) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID683277 | Antiproliferative activity against human BE(2)-C cells after 72 hrs by Alamar blue assay | 2012 | Bioorganic & 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. |
AID297473 | Cytotoxicity against HeLa cells | 2007 | Journal 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. |
AID1164183 | Inhibition 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 assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1855252 | Downregulation of SPT16 expression in human HCT-116 cells at 1.5 uM measured after 24 hrs by Western blot analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID456800 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID618015 | Cell 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 analysis | 2011 | Journal 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. |
AID1537555 | Inhibition 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 assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1065628 | Inhibition of human recombinant full length HDAC2 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1206762 | Inhibition of full length human recombinant HDAC1 expressed in baculovirus using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay | 2015 | Journal 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. |
AID473174 | Ex vivo inhibition of human HDAC6 in human Caco-2 cells by fluorometric cellular activity assay | 2010 | Journal 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. |
AID1386681 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1622979 | Cytotoxicity against human MCF7 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1065961 | Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID1514612 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID1274876 | Inhibition of HDAC6 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts. |
AID1482117 | Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1671979 | Cytotoxicity against human HCT-116 cells after 72 hrs by SRB assay | 2019 | Bioorganic & 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. |
AID1548300 | Induction 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%) | |||
AID1355712 | Antifungal activity against FLC resistant Candida albicans 0710922 assessed as fluconazol MIC50 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1356282 | Cytotoxicity 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 | |||
AID1826599 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID526531 | Inhibition of HDAC | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Property based optimization of δ-lactam HDAC inhibitors for metabolic stability. |
AID1449218 | Inhibition of human recombinant HDAC8 expressed in Escherichia coli using Z-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate measured after 90 mins by fluorescence assay | 2017 | Journal 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. |
AID1764249 | Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1873411 | Inhibition of HDAC3 (unknown origin) preincubated for 60 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1649884 | Inhibition of HDAC8 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview. |
AID1548247 | Inhibition 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 | |||
AID1754798 | Downregulation of SIRT5 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1901762 | Inhibition of full length human recombinant HDAC6 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1742740 | Genotoxicity in Salmonella typhimurium TA97a by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID308646 | Antiproliferative activity against human PANC1 cells | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID1174704 | Antitumor activity against human U937 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 120 mg/kg/day, po after 16 days | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID304371 | Inhibition of human IMPDH 1 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. |
AID461261 | Antiproliferative activity against human MCF7 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1533328 | Selectivity 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 cells | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor. |
AID619057 | Half life in human liver microsomes | 2011 | Journal 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. |
AID1164912 | Inhibition of HDAC7 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1280273 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID328802 | Inhibition of HDAC5 at 10 uM | 2008 | Journal 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. |
AID1515912 | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1605970 | Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1898905 | Antiproliferative activity against human U2932 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID492812 | Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID1864266 | Antitumor 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 days | 2022 | Journal 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. |
AID1864252 | Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability | 2022 | Journal 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. |
AID1897367 | Inhibition of FGFR1 (unknown origin) | |||
AID1597955 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1897373 | Inhibition of HDAC2 (unknown origin) | |||
AID1704070 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors. |
AID1487004 | Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2017 | Bioorganic & 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. |
AID1410013 | Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor. |
AID609725 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
AID1578507 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells incubated for 18 hrs by annexin V FITC and PI based flow cytometry | 2020 | ACS 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. |
AID1876467 | Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1276240 | Inhibition 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 analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation. |
AID461256 | Antiproliferative activity against human HepG2 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID1275656 | Toxicity 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 dosing | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1599771 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1518828 | Antimalarial activity against ring stage Plasmodium falciparum K1 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1890517 | Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1742706 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID274075 | Inhibition of MCF7 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID511067 | Inhibition of HDAC10 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1275247 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC. |
AID1529548 | Induction 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%) | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1819529 | Antitumor 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 days | 2022 | Journal 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. |
AID503687 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1434353 | Growth inhibition of human PC3 cells measured after 5 days by sulforhodamine-B assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1649503 | Cytotoxicity against mouse L929 cells assessed as reduction in cell viability measured after 72 hrs by tryphan blue assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | |
AID411261 | Cytotoxicity against human primary lung fibroblasts after 72 hrs by trypan blue exclusion assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1399543 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID1379288 | Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay | 2017 | ACS 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. |
AID1876464 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1622934 | Inhibition of recombinant human HDAC6 using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1321725 | Passive membrane permeability of the compound at 50 uM after 18 hrs by PAMPA | 2016 | Journal 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. |
AID445125 | Inhibition of human recombinant his tagged HDAC4 expressed in baculovirus assessed as residual activity at 5 uM | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group. |
AID348797 | Inhibition of HDAC2 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID620531 | Reactivation of MeCp2 mutant expression in human GM11272 cells at 10 to 100 nM by PCR method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression. |
AID1762500 | Cytotoxicity against mouse Neuro2a cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo 2.0 Luminescent cell assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1739566 | Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 20 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1742181 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1859953 | Cytotoxicity against mouse NIH3T3 cells assessed as inhibition of cell growth by neutral red uptake assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1901158 | Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1063059 | Inhibition of HDAC in human K562 cell extract using Fluor-de-Lys deacetylase as substrate preincubated for 45 mins measured after 15 mins by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID90675 | In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells | 2002 | Journal 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. |
AID613298 | In vitro cardiac safety index, ratio of IC50 for human ERG to IC50 for human HCT116 cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1549140 | Antifungal activity against azole-resistant Candida tropicalis 5008 after 48 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID1312892 | Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as mortality at 50 mg/kg, ip administered every 2 days for 11 days | 2016 | Journal 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. |
AID1215094 | Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1321734 | Inhibition 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 control | 2016 | Journal 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. |
AID1355728 | Antitumor 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 control | 2018 | Journal 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. |
AID1511149 | Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID288448 | Inhibition of LPS-stimulated NO production in RAW264.7 cells after 24 hrs by ELISA | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID482956 | Half life in human liver microsome | 2010 | Bioorganic & 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. |
AID482947 | Inhibition of HDAC7 | 2010 | Bioorganic & 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. |
AID750107 | Cytotoxicity against human HCT116 cells after 48 hrs by Sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID1566807 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1599727 | Cytotoxicity against human Meso13 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1816227 | Induction 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%) | |||
AID352749 | Inhibition of His-tagged HDAC4 catalytic domain expressed in Escherichia coli | 2009 | Bioorganic & 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. |
AID1899585 | Inhibition of HDAC class 1 in human HT-29 cells using Boc-Lys-Ac as substrate incubated for 3 hrs by microplate reader assay | |||
AID1296348 | Inhibition 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 assay | 2016 | Journal 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. |
AID603539 | Toxicity in human MDA-MB-231 cells xenografted athymic nude mouse assessed as change in body weight at 90 mg/kg, ip qd for 21 days | 2011 | Journal 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. |
AID1181331 | Potentiation 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 Assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID1633669 | Neurotoxicity against rat CGN cells assessed as cell viability at 25 uM incubated for 24 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1917536 | Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID408880 | Inhibition of HDAC1 | 2008 | Journal 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. |
AID1165113 | Cytotoxicity against human DU145 cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID1742654 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1454053 | Growth inhibition of human MCF7 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID541644 | Inhibition of human HDAC1 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1371075 | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1907399 | Inhibition of HDAC1 (unknown origin) using trypsin and LGK(Ac)-AMC as substrates incubated for 1 hr and measured by fluorescence assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Dual-acting antitumor agents targeting the A |
AID1876466 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID90347 | Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells. | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Trifluoromethyl ketones as inhibitors of histone deacetylase. |
AID1155336 | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1677509 | Up regulation of BAX protein in human HeLa cells at 0.3 to 3 uM after 6 to 12 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1206764 | Inhibition 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 assay | 2015 | Journal 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. |
AID603535 | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1888586 | Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay | |||
AID1446915 | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | 2017 | Bioorganic & 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. |
AID1326514 | Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID347870 | Growth inhibition of human ovarian cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1550115 | Inhibition 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 analysis | 2019 | Journal 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. |
AID674001 | Growth inhibition of human MCF7 cells after 72 hrs by XTT assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1898954 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID760495 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID780586 | Inhibition 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 assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. |
AID1200981 | Plasma clearance in ICR mouse | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1469372 | Cytotoxicity against human Hep3B cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2018 | Journal 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 |
AID619055 | Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1280307 | Inhibition of human KDAC3 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1739565 | Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 100 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1864264 | Antitumor 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 days | 2022 | Journal 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. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug 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. |
AID1486670 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID670101 | Antitumor activity against human A549 cells xenografted in nude mouse assessed as tumor growth delay at 200 mg/kg, po administered QD till end point | 2012 | Journal 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. |
AID1426427 | Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID347871 | Growth inhibition of human Leukemia cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1825925 | Inhibition 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 | |||
AID1727732 | Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1441673 | Anti-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 7 | 2017 | Journal 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. |
AID420644 | Antitumor 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 weeks | 2009 | European 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. |
AID755627 | Inhibition of HDAC isolated from human HeLa cell nuclear extract after 30 mins by fluorescence assay | 2013 | Bioorganic & 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. |
AID1606018 | Induction of necrosis in human HEK293 at 1 to 2 uM after 72 hrs by propidium iodide/Annexin-V staining based flow cytometry | 2020 | Journal 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. |
AID1659236 | Inhibition of human HDAC6 after 30 mins by microplate reader analysis | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6. |
AID1482134 | Induction 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%) | 2017 | Journal 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. |
AID1556035 | Inhibition 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-tubulin | 2019 | Journal 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 |
AID1901054 | Inhibition of HDAC1 (unknown origin) using trypsin and Ac-peptide as substrates | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID637889 | Inhibition of recombinant human HDAC6 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | 2012 | Bioorganic & 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. |
AID1819506 | Inhibition of HDAC8 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2022 | Journal 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. |
AID1572342 | Inhibition of recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1250650 | Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID717795 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID749388 | Inhibition of human recombinant HDAC6 expressed in High5 insect cells using Boc-Lys (-acetyl)-AM) as substrate after 24 hrs by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
AID1917544 | Selectivity index, ratio IC50 for inhibition of HDAC11 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification 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. |
AID527046 | Inhibition of AKT phosphorylation in human A549 at 5 uM after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID350726 | Growth inhibition of human SNB78 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID545859 | Antimalarial activity against Plasmodium falciparum HB3 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1321735 | Inhibition 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 control | 2016 | Journal 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. |
AID1469312 | Induction 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%) | 2018 | Journal 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 |
AID1898900 | Antiproliferative activity against human MM432 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1200980 | Inhibition of HDAC6 in human NCI-H929 cells assessed as induction of tubulin acetylation after 24 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1266808 | Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | 2015 | Journal 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. |
AID544090 | Antimalarial activity against drug-resistant Plasmodium falciparum D6 infected in Aotus lemurinus lemurinus monkey | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1548260 | Antiproliferative activity against human KM3 cells incubated for 48 hrs by MTT assay | |||
AID1373247 | Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold. |
AID1572345 | Selectivity ratio of IC50 for recombinant human HDAC8 to IC50 for N-terminal GST-tagged human HDAC6 | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1861670 | Induction of apoptosis in human HCT-116 cells at 2000 nM measured after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1659646 | Inhibition of HDAC in human HeLa cell extracts assessed as inhibition of substrate deacetylation using Boc-Lys (acetyl)-AMC as substrate by fluorescence based assay | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID1203894 | Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1469178 | Downregulation of HDAC6 protein expression in human MV4-11 cells at 5 uM after 24 hrs by Western blot analysis | 2018 | Journal 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. |
AID1861336 | Inhibition 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 analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID328810 | Antiproliferative activity against human renal epithelial cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID1178593 | Inhibition 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 fluorometry | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID1758495 | Antiproliferation activity against human U-87 MG cells assessed as growth inhibition measured after 1 hr by MTT assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID446342 | AUC (0 to infinity) in CD1 mouse at 5 mg/kg, iv | 2010 | Journal 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. |
AID328794 | Inhibition of HDAC2 | 2008 | Journal 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. |
AID1250644 | Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1355689 | Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay | 2018 | Journal 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. |
AID1275637 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Identification 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. |
AID1371052 | Antilieshmanial activity against amastigote stage of Leishmania donovani by fluorimetric assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1742659 | Cytotoxicity against human PLC cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID90343 | In vitro inhibitory activity against histone deacetylase (HDAC) isolated from HeLa nuclear extract at a concentration of 100 uM | 2003 | Bioorganic & 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. |
AID1821322 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1273868 | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID673999 | Growth inhibition of human Jurkat cells after 72 hrs by XTT assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1667067 | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1821340 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1206765 | Inhibition of human recombinant HDAC4 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay | 2015 | Journal 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. |
AID274012 | Percent inhibition of CYP450 2D6 at 1uM concentration | 2007 | Bioorganic & 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. |
AID525002 | Inhibition of HDAC3 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1469288 | Induction 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%) | 2018 | Journal 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 |
AID1659658 | Induction 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 control | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID1898951 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1245690 | Inhibition 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 assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1251318 | Growth inhibition of human IGROV1 cells after 72 hrs | 2015 | Bioorganic & 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. |
AID1754784 | Induction 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1758466 | Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1591851 | Inhibition 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 contro | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID760374 | Half life in mouse liver microsomes at 0.4 ug/mL by HPLC-MS analysis in presence of NADPH | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1266841 | Induction 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 analysis | 2015 | Journal 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. |
AID1441694 | Protection 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) | 2017 | Journal 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. |
AID1769650 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1873407 | Inhibition of HDAC2 (unknown origin) preincubated for 90 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1433258 | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1352478 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID1441642 | Anti-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 micro | 2017 | Journal 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. |
AID737908 | Selectivity index, ratio of IC50 for mouse MEF cells to IC50 for human A549 cells | 2013 | Journal 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. |
AID1170749 | Cytotoxic activity against human EB3 cells after 3 days by MTT assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1129792 | Induction of apoptosis in human Jurkat cells assessed as caspase 8 activation at 10 uM after 24 hrs by FACS flow cytometric analysis relative to control | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID297496 | Cytotoxicity against human WM 266-4 cells | 2007 | Journal 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. |
AID1898495 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2021 | Journal 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. |
AID1901162 | Antiproliferative activity against human SGC-7901 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1181304 | Inhibition of human recombinant HDAC4 using non-histone trifluoroacetyl lysine substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID1441656 | Anti-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 hrs | 2017 | Journal 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. |
AID482942 | Inhibition of HDAC2 | 2010 | Bioorganic & 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. |
AID1462023 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. |
AID1819859 | Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay | 2021 | Journal 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. |
AID1600660 | Antiproliferative activity against human OE33 cells assessed as reduction in cell viability incubated for 72 hrs by presto blue assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics. |
AID1578910 | Induction of autophagy in human Bel7402 cells assessed as upregulation of LC3-2 level at 5 uM after 24 to 72 hrs by Western blot analysis | 2019 | Journal 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. |
AID1303628 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID459821 | Inhibition of HDAC in human HeLa cell nuclear extract by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors. |
AID1684874 | Antitumor 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 | |||
AID476654 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1066165 | Antimigratory activity against human LNCAP cells at 50 uM after 72 hrs | 2014 | Journal 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. |
AID1900903 | Cytotoxicity against mouse GL26 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID482948 | Inhibition of HDAC9 | 2010 | Bioorganic & 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. |
AID1170744 | Inhibition of human recombinant HDAC6 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1898952 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1330927 | Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | 2017 | Bioorganic & 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. |
AID1515902 | Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID274070 | Half life after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID408883 | Inhibition of HDAC8 | 2008 | Journal 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. |
AID1591717 | Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1722281 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17 | The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells. |
AID1545859 | Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1659654 | Antiproliferative activity against human K562 cells incubated for 24 hrs by CCK8 assay | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID1622954 | Inhibition of HDAC in human HeLa nuclear extract | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1177055 | Cytotoxicity against rat L6 cells | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1873404 | Inhibition of HDAC2 (unknown origin) preincubated for 5 mins | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID605540 | Antiproliferative activity against human HUT78 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1543662 | Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
AID1281849 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1676595 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1688042 | Induction of HDAC3 degradation in human HL-60 cells assessed as decrease in HDAC3 level at 2 uM incubated for 12 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID297479 | Cytotoxicity against human MCF7 cells | 2007 | Journal 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. |
AID708275 | Growth inhibition of human QGY7701 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID1622908 | Inhibition of HDAC in human HeLa cytosolic extract using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1753832 | Inhibition 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 control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1676589 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID352750 | Inhibition of C-terminal FLAG tagged HDAC6 | 2009 | Bioorganic & 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. |
AID1303692 | Potentiation 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) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1418671 | GPx-like activity of the compound assessed as velocity for tert-butyl hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & 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. |
AID1876463 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1578907 | Induction 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 method | 2019 | Journal 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. |
AID1897470 | Inhibition 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 | |||
AID1260655 | Binding affinity to Zn2+ assessed as Zn2+/compound complex formation by ITC analysis | |||
AID481545 | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1653096 | Antiproliferative activity against human HepG2 cells by CCK8 assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID222292 | Compound was tested for anti-proliferative activity in human hepatocytes | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1659648 | Inhibition of HDAC2 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID487875 | Inhibition of HDAC in human A549 cells assessed as induction of histone H4 hyperacetylation at IC50 concentration after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | New aryldithiolethione derivatives as potent histone deacetylase inhibitors. |
AID1173495 | Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay | 2014 | Bioorganic & 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. |
AID1777022 | Inhibition of HDAC6 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase. |
AID1129010 | Inhibition of human HDAC-8 using RHKK(Ac) as substrate by fluorescence assay | 2014 | Journal 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. |
AID1437552 | Inhibition of human HDAC1 using H3(1-21)K9 after 60 mins by fluorescence assay | 2017 | Journal of natural products, 01-27, Volume: 80, Issue:1 | Monascustin, an Unusual γ-Lactam from Red Yeast Rice. |
AID1055715 | Antiproliferative activity against human AsPC1 cells after 48 hrs by SRB assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1441690 | Protection 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 method | 2017 | Journal 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. |
AID1452275 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. |
AID626563 | Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 1 uM by fluorescence spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22 | 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors. |
AID1178601 | Inhibition of human HDAC6 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors. |
AID511069 | Inhibition of HDAC in human HeLa cells at 10 uM after 15 mins | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1401374 | Inhibition 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 method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1865304 | Antitumor 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 control | 2022 | Journal 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. |
AID473183 | Growth inhibition of human Caco-2 cells after 48 hrs by MTT assay | 2010 | Journal 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. |
AID748980 | Inhibition of HDAC5 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1434361 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1205631 | Growth inhibition of human NCI-H23 cells after 5 days by sulforhodamine B assay | 2015 | Journal 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. |
AID586606 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID1065636 | Inhibition of human recombinant HDAC7 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1367349 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Synthesis and biological evaluation of Santacruzamate-A based analogues. |
AID539709 | Inhibition of human HDAC after 30 mins | 2010 | Bioorganic & 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. |
AID1897392 | Induction 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%) | |||
AID288452 | Growth inhibition of ACHN cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID1647329 | Anti-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 ventr | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1514610 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID1545755 | Inhibition of HDAC1 (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Indole: A privileged scaffold for the design of anti-cancer agents. |
AID1605981 | Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1206767 | Inhibition 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 assay | 2015 | Journal 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. |
AID1690844 | Inhibition 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 s | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1348914 | Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID609506 | Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors. |
AID1164905 | Solubility of the compound in phosphate buffer at pH 6.5 after 1 to 2 hrs by LYSA | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1322165 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID1449681 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1819503 | Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2022 | Journal 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. |
AID1888426 | Toxicity 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 days | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID605530 | Antiproliferative activity against human A2780 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID408889 | Cytotoxicity against human Hup T3 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1578506 | Induction 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 %) | 2020 | ACS 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. |
AID1785328 | Inhibition 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 | |||
AID1541453 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1898980 | Induction 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%) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID604137 | Inhibition 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 blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). |
AID780587 | Inhibition 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 assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. |
AID1885698 | Toxicity in ICR mouse assessed as effect on AST level at 12 umol/kg, ip measured after 12 hrs in presence of CDDO-Me | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Redox-Activatable Theranostic Co-Prodrug for Precise Tumor Diagnosis and Selective Combination Chemotherapy. |
AID1282258 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1547273 | Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1898907 | Antiproliferative activity against human NB-4 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1647339 | Anti-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 administer | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID446335 | Metabolic stability in mouse liver microsomes assessed as half life | 2010 | Journal 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. |
AID1206741 | Cytotoxicity against human 3AO cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal 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. |
AID1250646 | Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1783068 | Antifungal activity against fluconazole-sensitive Candida albicans 4108 assessed as inhibition of fungal growth | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections. |
AID1349732 | Toxicity 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 days | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1482172 | Cytotoxicity against human PC3 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1702137 | Inhibition 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 %) | 2018 | Journal 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. |
AID1907401 | Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Dual-acting antitumor agents targeting the A |
AID1293578 | Antitumor 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 control | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1863436 | Inhibition of HDAC4 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1587863 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1848614 | Cytotoxicity against human IGROV-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1865239 | Inhibition 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 analysis | 2022 | Journal 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. |
AID473181 | Induction of HDAC-mediated alpha-tubulin acetylation in human HepG2 cells at 5 uM after 6 hrs by indirect ELISA | 2010 | Journal 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. |
AID683274 | Inhibition of HDAC1 by fluorometric assay | 2012 | Bioorganic & 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. |
AID1821277 | Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1614251 | Antitumor 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 | |||
AID1431813 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1898897 | Antiproliferative activity against human A2780 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1888587 | Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay | |||
AID1576452 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay | |||
AID1361645 | Cell 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%) | 2018 | Journal 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. |
AID1742228 | Antitumor 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 analysis | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID300838 | Growth inhibition of human HCT15 cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID1326517 | Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated alpha-tubulin after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1401901 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID1578492 | Induction 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 %) | 2020 | ACS 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. |
AID1415637 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 60 mins by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1399542 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID1454057 | Growth inhibition of human OVCAR5 cells after 3 days by WST1 assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1515839 | Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1819536 | Toxicity 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 analysis | 2022 | Journal 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. |
AID240505 | Inhibitory concentration against histone deacetylase of HeLa cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design. |
AID1361634 | Inhibition of HDAC6 (unknown origin) after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID1119182 | Cytotoxicity against human MCF10A cells after 96 hrs by MTA reduction assay | 2012 | MedChemComm, , Volume: 3, Issue:1 | Polyamine-based small molecule epigenetic modulators. |
AID414717 | Inhibition of human recombinant HDAC1 expressed in HEK293 cells | 2009 | Journal 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. |
AID482941 | Inhibition of HDAC8 | 2010 | Bioorganic & 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. |
AID1441707 | Anti-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 7 | 2017 | Journal 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. |
AID1162226 | Induction 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%) | 2014 | Bioorganic & 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. |
AID541647 | Inhibition of human HDAC8 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1550158 | Toxicity 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 ruxolitinib | 2019 | Journal 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. |
AID1139708 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives. |
AID392409 | Induction of alpha tubulin acetylation in human T24 cells after 3 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Sulfamides as novel histone deacetylase inhibitors. |
AID1384224 | Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1753837 | Antiproliferative activity against human MGC803 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID274025 | Half life after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1380940 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1614140 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay | |||
AID525017 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in mutant Fdelta508 CFTR mRNA level at 5 uM after 8 hrs by RT-PCR | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1355711 | Antifungal activity against FLC resistant Candida albicans 0710922 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1401382 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1664945 | Inhibition 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 assay | 2020 | ACS 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. |
AID1239050 | Inhibition 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 hrs | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID749696 | Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 expression at 2.5 to 5 uM after 24 hrs by Western blot analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1623534 | Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID1762490 | Inhibition 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 a | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1566802 | Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1462030 | Half life in rat plasma at 200 uM by HPLC analysis | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. |
AID1469377 | Induction 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%) | 2018 | Journal 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 |
AID1702085 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1355688 | Inhibition 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 assay | 2018 | Journal 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. |
AID723472 | Inhibition of HDAC in cisplatin sensitive human MDA-MB-231 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1737151 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1890343 | Antitumor 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1816194 | Inhibition of TYK2 (unknown origin) incubated for 40 min in presence of ATP by microplate reader analysis | |||
AID420509 | Induction of apoptosis in human IGROV1 cells at IC90 after 72 hrs by TUNEL assay | 2009 | European 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. |
AID781049 | Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID292437 | Antiproliferative activity against HeLa cells by alamar blue assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Trithiocarbonates: exploration of a new head group for HDAC inhibitors. |
AID1785340 | Inhibition of recombinant human HDAC9 measured after 30 mins by fluorescence microplate reader assay | |||
AID1266086 | Inhibition of HDAC in human MeT-5A cells assessed as hisone H3 acetylation at 5 uM after 16 hrs by BRET assay | 2016 | Bioorganic & 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. |
AID1390013 | Inhibition 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 assay | 2018 | Bioorganic & 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. |
AID1758526 | Permeability of compound by PAMPA-BBB assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID1702069 | Inhibition 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 assay | 2018 | Journal 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. |
AID710838 | Cytotoxicity against human ACHN cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID1482171 | Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1246514 | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & 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. |
AID1441672 | Anti-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 7 | 2017 | Journal 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. |
AID1754800 | Downregulation of SIRT7 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1754796 | Downregulation of SIRT3 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID525023 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 5 uM by RT-PCR | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1614193 | Induction 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%) | |||
AID1774970 | Inhibition 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 assay | 2021 | ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12 | Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. |
AID1890336 | Antitumor 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 days | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID619140 | Kinetic solubility of the compound at pH 7 with 2.5% DMSO | 2011 | Journal 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. |
AID1421912 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1337260 | Antiproliferative activity against human MCF7 cells up to 72 hrs by MTT assay | 2016 | Journal 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. |
AID1578885 | Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay | 2019 | Journal 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. |
AID1897396 | Induction 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%) | |||
AID1898899 | Resistance index, ratio of IC50 for human A2780 cells to IC50 for A2780-DX cells | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID503690 | Inhibition 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 assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10 | Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1810052 | Inhibition 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 | |||
AID511064 | Inhibition of HDAC2 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1865259 | Inhibition 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 method | 2022 | Journal 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. |
AID461264 | Antiproliferative activity against human NCI-H2122 cells | 2010 | Journal 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. |
AID663370 | Growth inhibition of human PC3 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1373248 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold. |
AID1816191 | Inhibition of recombinant HDAC10 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | |||
AID350717 | Inhibition of human recombinant HDAC2 by fluorimetry | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID366651 | Cytotoxicity against HMEC after 72 hrs by MTT assay | 2008 | Journal 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. |
AID663385 | Growth inhibition of human UACC257 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID762189 | Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay | 2013 | Journal 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. |
AID623098 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2011 | European 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. |
AID1141762 | Cytotoxicity against human KB cells by MTT assay | 2014 | Journal 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. |
AID1421926 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1630628 | Inhibition of HDAC in human MOLT4 cells assessed as H3K9 acetylation at 2.5 uM after after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID352752 | Antiproliferative activity against human HCT116 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Bioorganic & 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. |
AID1240551 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID1065631 | Inhibition 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 assay | 2013 | Journal 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. |
AID1576464 | Induction 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%) | |||
AID744874 | Cytotoxicity against human HCT116 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Discovery of adamantane based highly potent HDAC inhibitors. |
AID481568 | Antitumor 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 days | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1901170 | Inhibition of HDAC6 in human HCT-116 cells assessed as increase in alpha-tubulin acetylation at 5 uM measured after 6 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID544400 | Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation after 3.5 hrs by SDS-PAGE | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1639363 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1361629 | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1864678 | Inhibition 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 | |||
AID1239056 | Inhibition of HDAC in human RPMI8226 cells assessed as upregulation of acetylated alpha-tubulin level at 1 uM after 24 hrs by Western blot analysis | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID1486322 | Genotoxicity in Salmonella typhimurium TA100 at 50 times antiproliferative IC50 by Ames test | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID626565 | Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release by fluorescence spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22 | 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors. |
AID1865294 | Antitumor 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 SHP099 | 2022 | Journal 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. |
AID1548246 | Inhibition 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 | |||
AID134164 | Antitumor activity against HT1080 cell line in mouse xenograft model after orally dosed once every other day at 30 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
AID749705 | Inhibition of HDAC in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1848283 | Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID1127011 | Induction of apoptosis in human U937 cells assessed as viable cells using annexin-V/propidium iodide staining after 12 to 24 hrs by flow cytometry analysis | 2014 | Journal 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. |
AID541656 | Growth inhibition of human HCT116 cells after 48 hrs by SRB assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID619051 | Competitive inhibition of HDAC6 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID723460 | Inhibition of human HDAC11 by fluorescence assay | 2013 | Journal 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. |
AID1464867 | Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate after 15 mins by fluorescence assay | 2017 | Bioorganic & 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. |
AID1697197 | Cytotoxicity against human SW620 cells by colorimetric method | 2020 | Bioorganic & 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. |
AID1816197 | Inhibition 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 | |||
AID1215090 | Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1421614 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
AID1537558 | Antiproliferative activity against human IMR32 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer Glo assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID765212 | Cytotoxicity against human MiaPaCa cells | 2013 | Bioorganic & 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. |
AID328793 | Inhibition of HDAC1 | 2008 | Journal 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. |
AID717804 | Inhibition of HDAC6 using Fluor-de-Lys as substrate assessed as remaining activity at 125 nM pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1467238 | Inhibition 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 fluorome | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID1605971 | Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1205634 | Induction of myc-tagged RUNX3 acetylation in human HEK293 cells assessed as RUNX3 level at 1 uM after 24 hrs by immunoprecipitation analysis relative to TSA | 2015 | Journal 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. |
AID1380938 | Inhibition 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 assay | 2018 | Journal 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. |
AID663336 | Growth inhibition of human COLO205 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1476161 | Antiproliferative activity against human KHYG cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1698865 | Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID329927 | Inhibition of human HDAC1 in U937 cells assessed as residual activity at 5 uM | 2008 | Bioorganic & 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. |
AID1667090 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1808546 | Inhibition 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 | 2021 | Journal 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). |
AID1482103 | Inhibition of HDAC 9 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1164173 | Induction of apoptosis in human K562 cells using annexin-V/PI staining by flow cytometry | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1202600 | Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation after 24 hrs by Western blotting analysis | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID1126962 | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2014 | Journal 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. |
AID482968 | Elimination half life in mouse at 10 mg/kg, iv | 2010 | Bioorganic & 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. |
AID1861309 | Induction of apoptosis in human DOHH-2 cells measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
AID473193 | Growth inhibition of human HepG2 cells after 48 hrs by MTT assay | 2010 | Journal 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. |
AID1702101 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1164922 | Cytotoxicity against human BE(2)-C cells at 2 uM after 3 to 9 days by CCK-8 assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1765328 | Inhibition 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 assa | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1393285 | Inhibition 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 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds. |
AID1825882 | Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay | |||
AID1174689 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1899584 | Inhibition of HDAC class 2a in human HT-29 cells using Boc-Lys-TFA as substrate incubated for 3 hrs by microplate reader assay | |||
AID1390014 | Inhibition 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 assay | 2018 | Bioorganic & 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. |
AID1816198 | Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | |||
AID1482105 | Inhibition of HDAC 11 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | 2017 | Journal 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. |
AID1487010 | Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID1518839 | Resistance ratio of IC50 for antimalarial activity against ring stage Plasmodium falciparum K1 to IC50 for antimalarial activity against ring stage Plasmodium falciparum 3D7 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID663379 | Growth inhibition of human MALME-3M cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1832670 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1865254 | Inhibition 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 assay | 2022 | Journal 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. |
AID1888404 | Antifungal activity against azole-resistant Candida albicans 0304103 assessed as fungal growth inhibition incubated for 48 hrs by CLSI based checkerboard microdilution assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. |
AID313736 | Inhibition of HDAC8 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID603531 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2011 | Journal 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. |
AID1730889 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID593546 | Inhibition of human HDAC2 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1739586 | Inhibition 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 DMSO | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1898911 | Antiproliferative 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 assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1572379 | Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter blue-reagent based assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1547334 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1572378 | Ratio 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 uM | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID404443 | Cytotoxicity against human Mia Paca2 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID663350 | Growth inhibition of human EKVX cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID674002 | Growth inhibition of human HEK293 cells after 72 hrs by XTT assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1155337 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for exo-erythrocytic form of Plasmodium berghei | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID482969 | Oral bioavailability in mouse at 10 mg/kg, iv | 2010 | Bioorganic & 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. |
AID1312930 | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of acetylated alpha-tubulin level at 2 uM after 6 hrs by Western blot method | 2016 | Journal 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. |
AID1591855 | Inhibition 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 contr | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
AID546550 | Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells | 2010 | Journal 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. |
AID1250641 | Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1486673 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1832690 | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1441682 | Anti-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) | 2017 | Journal 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. |
AID605619 | Cell 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 analysis | 2010 | Journal 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. |
AID605392 | Inhibition of human recombinant HDAC1 using fluor de Lys as substrate by fluorometric analysis | 2010 | Journal 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. |
AID1599786 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID708277 | Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID1511132 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID274171 | Antiproliferative activity against HCT116 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID247946 | Concentration required to inhibit human LNCaP prostate carcinoma cells | 2005 | Journal 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. |
AID1282238 | Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1542186 | Inhibition of HDAC8 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1065632 | Inhibition of human recombinant full length HDAC8 using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1859928 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID1890307 | Inhibition of recombinant human HDAC1 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1518786 | Antiproliferative activity against human OPM2 cells incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID765392 | Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID481571 | Cytotoxicity against mouse S180 cells assessed as growth inhibition at 100 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1293560 | Antiproliferative activity against human HT-29 cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1742629 | Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in acetylated alpha-tubulin incubated for 8 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1826631 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1915537 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1206736 | Inhibition of HDAC1/HDAC2 in human HeLa cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2015 | Journal 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. |
AID1915552 | Antiproliferative activity against breast cancer cell line (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1390016 | Antiproliferative activity against human A549 cells after 96 hrs by MTT assay | 2018 | Bioorganic & 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. |
AID1431815 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1441652 | Anti-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 ELISA | 2017 | Journal 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. |
AID1816689 | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1312926 | Inhibition 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 method | 2016 | Journal 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. |
AID760505 | Inhibition of HDAC8 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHK(Ac)K(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1449675 | Inhibition 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 assay | 2017 | Bioorganic & 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. |
AID1466059 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID765391 | Inhibition of GST-tagged recombinant human HDAC3/NcoR1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID1547258 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1476150 | Antiproliferative activity against human HL60 cells | 2017 | Journal 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. |
AID663357 | Growth inhibition of human COLO205 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1752945 | Selectivity 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 | |||
AID461254 | Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay | 2010 | Journal 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. |
AID652750 | Inhibition of recombinant human HDAC6 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1164915 | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1548730 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis | 2020 | Journal 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. |
AID1633991 | Inhibition of HDAC3 in human HuH7 cells assessed as increase in histone H3 K9/K14acetylation at varying concentrations incubated for 24 hrs by Western blot analysis | 2019 | Bioorganic & 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). |
AID1622910 | Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID652761 | Restoration 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 control | 2011 | ACS 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. |
AID1055352 | Selectivity ratio of IC50 for human recombinant HDAC6 to IC50 for human recombinant HDAC2 | 2013 | Journal 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. |
AID1763821 | Inhibition of human recombinant HDAC8 incubated for 15 mins by fluorogenic assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID1622900 | Cytotoxicity against human HCT116 cells after 72 hrs by CellTiter-Glo assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1737147 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1826641 | Induction 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%) | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID781046 | Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay | 2013 | Bioorganic & 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. |
AID1742664 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1876477 | Induction 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 analysis | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1578499 | Induction 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 %) | 2020 | ACS 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. |
AID348800 | Inhibition of HDAC4 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID1441632 | Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay | 2017 | Journal 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. |
AID297500 | Cytotoxicity against vincristine resistant human CCRF-CEM cells | 2007 | Journal 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. |
AID1543931 | Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
AID1864223 | Cytotoxicity against human BT-549 cells assessed as reduction in cell viability measured after 48 hrs | 2022 | Journal 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. |
AID366647 | Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1671970 | Retention time of the compound by HPLC method | 2019 | Bioorganic & 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. |
AID734740 | Inhibition of HDAC6 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition. |
AID1486296 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1227053 | Cytotoxicity against african green monkey Vero cells cells assessed as cell proliferation after 70 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1785330 | Inhibition 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 | |||
AID1863172 | Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID1478590 | Inhibition 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 method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID446344 | Half life in CD1 mouse at 15 mg/kg, po | 2010 | Journal 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. |
AID1067345 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1832689 | Inhibition of human HDAC5 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID347874 | Growth inhibition of human prostate cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID1578501 | Induction 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 %) | 2020 | ACS 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. |
AID1819555 | Antitumor 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 analysis | 2022 | Journal 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. |
AID1260644 | Inhibition 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 | |||
AID1901768 | Cytotoxicity against human MRC9 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1901786 | Binding affinity to full length HDAC6-NanoLuc fusion protein (unknown origin) expressed in HeLa cells assessed as residence time by NanoBRET assay | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1525776 | Inhibition of HADC6 (unknown origin) | 2020 | Journal 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. |
AID1898894 | Antiproliferative activity against human NCI-H460 cells incubated for 24 hrs followed by incubating in drug-free medium for 48 hrs and measured by SRB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID673990 | Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID750109 | Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay | 2013 | Bioorganic & 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. |
AID764219 | Inhibition of HDAC in human HeLa cell extract using Fluor deLys as substrate by fluorimetric assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1771459 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID1848631 | Cytotoxicity against human SN12C cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1337253 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID208379 | Tested for morphological alterations in T/5 cells after administration along with DMSO (0.1%) | 1995 | Journal 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. |
AID732143 | Inhibition of HDAC7 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal 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. |
AID1464873 | Anti-proliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1361659 | Antitumor 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 implantation | 2018 | Journal 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. |
AID1890330 | Stability in mouse plasma incubated for 6 hrs in presence of NADPH and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1742665 | Cytotoxicity against human NCI-1581 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1280269 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID408885 | Inhibition of HDAC6 | 2008 | Journal 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. |
AID1141764 | Cytotoxicity against human PC3 cells by MTT assay | 2014 | Journal 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. |
AID1467236 | Inhibition 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 fluorome | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID670514 | Inhibition 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 fluorimetry | 2012 | Bioorganic & 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. |
AID1762496 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID1897807 | Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2022 | Journal 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. |
AID737909 | Cytotoxicity against human HS68 cells after 72 hrs by MTT assay | 2013 | Journal 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. |
AID1182316 | Antiproliferative activity against hTERT expressing immortalized human HPNE cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1688022 | Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition after 72 hrs by trypan blue staining based cell counting assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1260645 | Inhibition of human recombinant HDAC9 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID760511 | Inhibition of HDAC2 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1128557 | Inhibition of human HDAC-4 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1371071 | Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID765390 | Inhibition of recombinant human HDAC8 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | 2013 | Journal 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. |
AID1189850 | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Hydroxamic acids block replication of hepatitis C virus. |
AID663386 | Growth inhibition of human UACC62 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1365023 | Inhibition of recombinant human HDAC2 preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay | 2017 | Bioorganic & 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. |
AID297481 | Cytotoxicity against human MDA-MB-231cells | 2007 | Journal 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. |
AID544092 | Antimalarial activity against drug-resistant Plasmodium falciparum TM91C235 | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1164186 | Inhibition 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 assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1383992 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1240550 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID1771458 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID1597954 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID748979 | Inhibition of HDAC in human K562 cells | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID655476 | Inhibition of recombinant human HDAC1 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1380985 | Antitumor 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 control | 2018 | Journal 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. |
AID1698860 | Inhibition of HDAC1 (unknown origin) at 100 nM relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors. |
AID1177048 | Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1452273 | Inhibition of HDAC1 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. |
AID1303632 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1055350 | Cytotoxicity against human HCT116 cells after 96 hrs by MTS-PMS assay | 2013 | Journal 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. |
AID1915598 | Inhibition of HDAC5 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID748978 | Inhibition of HDAC8 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | A cyclodextrin-capped histone deacetylase inhibitor. |
AID1647327 | Anti-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 recognition | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1550102 | Inhibition 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 assay | 2019 | Journal 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. |
AID1383998 | Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
AID1433303 | Induction 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 control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1730853 | Antiproliferation activity against human NCI-H838 cells incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1901764 | Inhibition of full length human recombinant HDAC11 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
AID1275076 | Inhibition of HDAC in human HeLa nuclear extract | 2016 | Bioorganic & 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. |
AID1486677 | Inhibition 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 analysis | 2017 | Bioorganic & 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. |
AID1597935 | Antiproliferative activity against human SGC7901 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID440823 | Inhibition of human recombinant N-terminal FLAG-tagged HDAC7 (438-915) expressed in baculovirus after 10 mins by fluorimetric analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. |
AID1155330 | Cytotoxicity against human HepG2 cells after 48 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID619046 | Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1485113 | Inhibition 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 control | 2017 | Journal 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. |
AID1514595 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA | 2019 | Bioorganic & 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. |
AID1690838 | Inhibition 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 fluorescence | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. |
AID1864221 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs | 2022 | Journal 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. |
AID1126997 | Induction 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%) | 2014 | Journal 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. |
AID1356299 | Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay | |||
AID1246524 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for imatinib resistant human IR-K562 cells | 2015 | Bioorganic & 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. |
AID1566036 | Selectivity 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 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
AID1826630 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1321728 | Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation after 2 hrs by Western blot analysis | 2016 | Journal 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. |
AID1550152 | Drug 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 analysis | 2019 | Journal 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. |
AID414726 | Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal 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. |
AID1597927 | Inhibition of HDAC8 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1897368 | Inhibition of FGFR1 (unknown origin) at 100 nM relative to control | |||
AID593550 | Inhibition of human HDAC5 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1848578 | Inhibition 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 analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1173497 | Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay | 2014 | Bioorganic & 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. |
AID1481748 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
AID1753639 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1848282 | Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID1622930 | Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1753835 | Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1832692 | Inhibition 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 method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1821264 | Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1742180 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. |
AID1394900 | Inhibition 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 analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1737655 | Cytotoxicity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | |||
AID1591716 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1633673 | Immunomodulatory 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 analysis | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
AID1897467 | Inhibition 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 | |||
AID438218 | Selectivity ratio of IC50 for HDAC8 to IC50 for HDAC1/2 from human HeLa cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide. |
AID297495 | Cytotoxicity against human U87MG cells | 2007 | Journal 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. |
AID1282253 | Cytotoxicity against human K562 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID717793 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1576465 | Induction 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%) | |||
AID1769657 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1129794 | Induction 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1303560 | Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 to 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID492804 | Inhibition of human recombinant HDAC4 after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID1401392 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1250658 | Selectivity ratio of GI50 for human DU145 cells to GI50 for human HLF cells | 2015 | Journal 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. |
AID1431814 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1653145 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID286791 | Effect on alpha tubulin acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Bispyridinium dienes: histone deacetylase inhibitors with selective activities. |
AID1597929 | Antiproliferative activity against human NCI-H226 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1433284 | Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID711155 | Inhibition of HDAC6 by fluorometric assay | 2012 | Journal 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. |
AID310180 | Inhibition of HDAC in HeLa cell lysates | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID1515983 | Inhibition of HDAC in human MM1S cells assessed as increase in histone H3 acetylation at 100 nM measured after 6 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity. |
AID1676600 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID527206 | Inhibition of ERK phosphorylation in human A549 at 5 uM after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1856994 | Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID329914 | Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay | 2008 | Bioorganic & 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. |
AID465151 | Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1723744 | Selectivity index, ratio of IC50 for inhibition of human recombinant HDAC1 to IC50 for inhibition of human recombinant HDAC6 | 2020 | Journal 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. |
AID1433239 | Induction of apoptosis in p53 null human U937 cells at 2 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1760292 | Antiproliferative activity against human A549 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1525779 | Inhibition of HADC3 (unknown origin) | 2020 | Journal 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. |
AID1421908 | Cytotoxicity against human HepG2A16 cells expressing GFP-fused CD81 after 48 hrs by bioluminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID708272 | Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID1165106 | Selectivity ratio of IC50 for axenic amastigote stage of Leishmania donovani to IC50 for amastigote stage of Leishmania donovani infected in human THP1 cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
AID619261 | Antitumor 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 22 | 2011 | Journal 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. |
AID1312903 | Toxicity 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 dose | 2016 | Journal 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. |
AID1067343 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID1245689 | Ratio of IC50 for Class 1 histone deacetylase in human PC3 cells to IC50 for Class 1 histone deacetylase isolated from human HeLa cell nuclear extracts | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID90211 | Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Heterocyclic ketones as inhibitors of histone deacetylase. |
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug 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. |
AID652766 | Induction of CFTR deltaF508 mutant protein expression in cystic fibrosis patient lung cells relative to control | 2011 | ACS 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. |
AID1785333 | Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | |||
AID1816224 | Induction 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%) | |||
AID1437251 | Inhibition of HDAC6 in mouse B16F10 cells assessed as accumulation of acetylated tubulin at 20 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID1141769 | Cytotoxicity against human MCF7 cells by MTT assay | 2014 | Journal 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. |
AID1915569 | Cytotoxicity against human MCF7 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID499802 | Inhibition of HDAC6 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID605394 | Inhibition of human recombinant HDAC3 using fluor de Lys as substrate by fluorometric analysis | 2010 | Journal 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. |
AID675300 | Antiproliferative activity against human HCT116 cells after 5 days by Alamar Blue assay | 2012 | Bioorganic & 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. |
AID1303686 | Inhibition of HDAC3 in human Jurkat cells extract after 30 mins by immunoprecipitation assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1826634 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID780575 | Inhibition of HDAC in human HeLa cell nuclear extracts using Color de LysTM after 30 mins | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors. |
AID1119181 | Cytotoxicity against human MCF7 cells after 96 hrs by MTA reduction assay | 2012 | MedChemComm, , Volume: 3, Issue:1 | Polyamine-based small molecule epigenetic modulators. |
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AID609493 | Inhibition of human ERG by automated patch clamp assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID637890 | Inhibition of recombinant human HDAC7 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay | 2012 | Bioorganic & 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. |
AID1630595 | Inhibition of HDAC in human MOLT4 cells assessed as H3K23 acetylation at 2.5 uM after after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID699752 | Inhibition of SIRT5 | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Substrates for efficient fluorometric screening employing the NAD-dependent sirtuin 5 lysine deacylase (KDAC) enzyme. |
AID1250666 | Inhibition 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 analysis | 2015 | Journal 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. |
AID1655786 | Inhibition of human EZH2 using core histone as substrate incubated for 1 hr by fluorescence based assay | 2020 | ACS 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. |
AID1437244 | Cytotoxicity against human A375 cells assessed as growth inhibition after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID1476166 | Cytotoxicity against human AC10 cells assessed as cell viability after 24 hrs by CellTiter-Glo assay | 2017 | Journal 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. |
AID1246521 | Cytotoxicity against human U937 cells assessed as reduction in cell viability | 2015 | Bioorganic & 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. |
AID1462223 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay | 2017 | Bioorganic & 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. |
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AID303346 | Growth inhibition of MCF7 cells | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. |
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AID1702153 | Metabolic stability in mouse liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis | 2018 | Journal 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. |
AID748101 | Inhibition of HDAC6 in human HeLa cells assessed as increase in alpha tubulin acetylation at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1337278 | Antiproliferative activity against human HL60 cells | 2016 | Journal 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. |
AID1452276 | Antiproliferative activity against human U937 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. |
AID1901154 | Inhibition 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 assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1730854 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID663332 | Growth inhibition of human A549 cells after 72 hrs by MTT assay | 2012 | Journal 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. |
AID90677 | Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi) | 2002 | Journal 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. |
AID1478592 | Inhibition of HDAC6 (unknown origin) using substrate after 30 mins by fluorometric analysis | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1688039 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1129781 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1808547 | Inhibition 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 assay | 2021 | Journal 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). |
AID1845459 | Inhibition of HDAC1 (unknown origin) | 2021 | Journal 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? |
AID1515927 | Antitumor 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 week | 2019 | Journal 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. |
AID1542188 | Inhibition of HDAC10 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID1482116 | Cytotoxicity against human HL60 cells assessed as growth inhibition after 48 hrs by MTT assay | 2017 | Journal 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. |
AID1702049 | Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1454052 | Growth inhibition of human K562 cells after 3 days by counting method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID586615 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation | 2011 | Antimicrobial 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. |
AID1415662 | Induction of apoptosis in human HepG2 cells at 5 uM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry relative to control | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
AID1888589 | Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay | |||
AID1897374 | Inhibition of HDAC8 (unknown origin) | |||
AID1497926 | Induction 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 analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | Development of the first small molecule histone deacetylase 6 (HDAC6) degraders. |
AID1897366 | Inhibition of HDAC6 (unknown origin) | |||
AID1760296 | Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1390023 | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1848612 | Cytotoxicity against human SNB-75 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1898916 | Inhibition of HDAC6 in human NCI-H460 cells at 7.4 uM assessed as increase in alpha-tubulin acetylation measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1129771 | Inhibition 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 control | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1578895 | Inhibition of HDAC in human Bel7402 cells assessed as increase in acetylated histone h3 expression at 5 uM incubated for 72 hrs by Western blot analysis | 2019 | Journal 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. |
AID1356296 | Inhibition of HDAC derived from human HeLa nuclear extract at 1 uM by fluorimetric assay relative to control | |||
AID767621 | Cytotoxicity against human HT1080 cells | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Inhibitory effects of p-dodecylaminophenol on the invasiveness of human fibrosarcoma cell line HT1080. |
AID1384228 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1321703 | Inhibition of HDAC6 (unknown origin) | 2016 | Journal 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. |
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AID1164030 | Inhibition of human recombinant HDAC7 after 60 mins by fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1181308 | Inhibition of HDAC1 in human U937 cells assessed as increase in p21WAF1/CIP1 level at 5 uM by Western blotting method | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID546563 | Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay | 2010 | Journal 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. |
AID524999 | Inhibition of HDAC6 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID628210 | Antiproliferative activity against human HeLa cells after 48 hrs by XTT assay | 2011 | Journal 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. |
AID1462226 | Inhibition of BRD4/HDAC1 in human OCI-AML3 cells assessed as reduction in myc expression levels at 1 uM after 24 hrs by Western blot analysis | 2017 | Bioorganic & 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. |
AID1763815 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID274064 | Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID1398801 | Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1275078 | Inhibition of recombinant human HDAC6 | 2016 | Bioorganic & 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. |
AID465156 | Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID499801 | Selectivity ratio IC50 for HDAC8 to IC50 for HDAC in human HeLa cells nuclear extract | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID1630602 | Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic substrate at 10 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID663400 | Growth inhibition of human MCF7 cells after 48 hrs by MTT assay | 2012 | Journal 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. |
AID747255 | Growth inhibition of HUVEC by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1541456 | Inhibition 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 measu | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1566809 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID670014 | Selectivity index, ratio of IC50 for human recombinant HDAC6 to IC50 for human recombinant HDAC1 | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID1202583 | Inhibition of His-tagged HDAC1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID1282250 | Cytotoxicity against human U266 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID748108 | Inhibition of HDAC7 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
AID1162219 | Cell 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%) | 2014 | Bioorganic & 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. |
AID525035 | Inhibition of CFTR transcription assessed as decrease of CFTR protein level at 50 uM by immunoblot method | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID764217 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1469396 | Induction 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%) | 2018 | Journal 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 |
AID1487094 | Inhibition of HDAC3 (unknown origin) | 2017 | Bioorganic & 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. |
AID1753636 | Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1771467 | Inhibition of HDAC (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID1630629 | Inhibition of HDAC in human MOLT4 cells assessed as H4K12 acetylation at 2.5 uM after after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1055353 | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | 2013 | Journal 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. |
AID1202595 | Cytotoxicity against human A549 cells at 100 uM after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
AID1731759 | Inhibition 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 assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates. |
AID1614134 | Inhibition 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 | |||
AID1652196 | Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1763818 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human MCF7 cells | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy. |
AID1622939 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1266856 | Antitumor 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) | 2015 | Journal 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. |
AID1127332 | Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID732872 | Inhibition 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 analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1433296 | Induction 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 control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID659635 | Antiproliferative activity against human SKMES1 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1398805 | Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1623523 | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate-3 by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID476650 | Toxicity in FVB mouse assessed as mortality at 50 mg/kg, po administered 5 times per week for 2 weeks measured up to 1 month | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1864228 | Inhibition of full length recombinant N-terminal GST-tagged human HDAC11 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay | 2022 | Journal 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. |
AID1348916 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities. |
AID1816687 | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1486301 | Antiproliferative activity against human U937 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID274031 | Inhibition of MCF7 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID1245685 | Cytotoxicity against human U266 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID476649 | Toxicity in FVB mouse assessed as mortality at 50 mg/kg, po administered 5 times per week for 2 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1128559 | Inhibition of human HDAC-6 using RHKK(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID1233269 | Inhibition of human recombinant HDAC6 after 15 mins by fluorogenic assay | 2015 | Journal 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. |
AID1845908 | Reversal 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 cytometry | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
AID1848621 | Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID732443 | Inhibition of human HCT116 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1239057 | Inhibition of HDAC in human RPMI8226 cells assessed as upregulation of acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID420636 | Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC50 after 24 hrs by Western blot | 2009 | European 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. |
AID392399 | Inhibition of human recombinant N-terminal histidine-tagged HDAC6 expressed in baculovirus by fluorimetry | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Sulfamides as novel histone deacetylase inhibitors. |
AID1702133 | Inhibition 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 %) | 2018 | Journal 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. |
AID1864222 | Cytotoxicity against human SUM159PT cells assessed as reduction in cell viability measured after 48 hrs | 2022 | Journal 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. |
AID1466402 | Antitumor 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 days | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. |
AID1848588 | Induction of ferroptosis in human NCI-H522 cells assessed as viability at 5 uM incubated after 60 hrs by microscopic analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID1659652 | Inhibition of HDAC8 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID652747 | Inhibition of recombinant human HDAC3-NCoR2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1808550 | Inhibition 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 assay | 2021 | Journal 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). |
AID1181310 | Induction 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 method | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID404444 | Cytotoxicity against human Panc 04.03 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1865273 | Induction 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 cytometry | 2022 | Journal 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. |
AID1225982 | Inhibition 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 assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1627671 | Inhibition of HDAC in human HL60 cells assessed as upregulation of alphatubulin acetylation levels at 2 uM after 18 hrs by SDS-PAGE analysis | 2016 | Bioorganic & 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. |
AID1566821 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1876461 | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence plate reader assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1816685 | Inhibition of recombinant LSD1 (157 to 852 residues) (unknown origin) expressed in Escherichia coli BL21 (DE) using H3K4me2 as substrate by amplex red assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID545856 | Antimalarial activity against Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1293559 | Antiproliferative activity against human LoVo/DX cells assessed as reduction in cell number after 72 hrs by cell counter analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID1667075 | Inhibition of HDAC1 in human MDA-MB-231 cells assessed as accumulation of acetylated H4 at 1.5 uM by western blot analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1164904 | Inhibition 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-275 | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1384227 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, 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. |
AID1845320 | Inhibition of BRD4 (unknown origin) by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Current status in the discovery of dual BET/HDAC inhibitors. |
AID274013 | Inhibition of CYP450 3A4 | 2007 | Bioorganic & 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. |
AID1410341 | Inhibition of HDAC in human HCT116 cells assessed as decrease in acetylated histone H3 levels after 12 hrs by Western blot analysis | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors. |
AID780574 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors. |
AID1487093 | Inhibition of HDAC2 (unknown origin) | 2017 | Bioorganic & 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. |
AID1865257 | Induction 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 cytometry | 2022 | Journal 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. |
AID663405 | Half life in mouse plasma | 2012 | Journal 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. |
AID1439355 | Inhibition of HDAC6 in human RPMI8226 cells assessed as increase in tubulin acetylation at 3 uM after 24 hrs by western blot analysis | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
AID1887690 | Cytotoxicity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo. |
AID1897394 | Induction 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%) | |||
AID626562 | Inhibition of HDAC in human HeLa cell extract assessed as fluorophore release at 0.1 uM by fluorescence spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22 | 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors. |
AID366641 | Inhibition of HDAC2 after 17 hrs | 2008 | Journal 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. |
AID732445 | Inhibition of human A549 cell proliferation after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID366646 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID670104 | Antitumor activity against human A549 cells xenografted in nude mouse assessed as tumor growth inhibition at 200 mg/kg, po administered QD till end point | 2012 | Journal 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. |
AID1487009 | Selectivity index, ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2017 | Bioorganic & 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. |
AID1821269 | Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1129777 | Cell 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1819502 | Inhibition of HDAC in human HeLa nuclear extract using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2022 | Journal 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. |
AID1754755 | Inhibition 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 analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1765331 | Selectivity index, ratio of IC50 for human recombinant full length HDAC6 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID327545 | Increase in acetylated histone H3 level in human HCT116 cells at 10 uM after 24 hrs relative to control | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID1775567 | Inhibition of human G9a enzyme using histone monomethyl-H3K9 peptide as substrate incubated for 1 hr in presence of SAM by TR-FRET assay | 2021 | Journal 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 |
AID316893 | Inhibition of HDAC8 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1819513 | Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | Journal 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. |
AID527039 | Cytotoxicity against human NCI-H2126 by SRB assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Selenium-containing analogs of SAHA induce cytotoxicity in lung cancer cells. |
AID1572340 | Cytotoxicity against human HepaRG cells assessed as cell viability at 100 uM after 24 hrs by CellTiter blue-reagent based assay relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1234899 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1816968 | Cytotoxicity against human HeLa cells assessed as cell death incubated for 20 hrs measured by DNS assay | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their |
AID1266095 | Inhibition of HDAC6 (unknown origin) by fluorimetric assay | 2016 | Bioorganic & 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. |
AID1401482 | Selectivity 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 lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1441653 | Anti-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 alone | 2017 | Journal 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. |
AID1401547 | Antiproliferative activity against human NB4 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID511068 | Inhibition of HDAC in human HeLa cells at 0.1 uM after 15 mins | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1403160 | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1861650 | Antiproliferative activity against human SW480 cells measured after 72 hrs | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies. |
AID1487002 | Inhibition of HDAC6 (unknown origin) by ELISA-based assay | 2017 | Bioorganic & 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. |
AID1769642 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1303623 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1367347 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Synthesis and biological evaluation of Santacruzamate-A based analogues. |
AID1548259 | Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay | |||
AID1863174 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID420637 | Inhibition of HDAC in human IGROV1 cells assessed as p53 acetylation at IC50 after 48 hrs by Western blot | 2009 | European 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. |
AID1578154 | Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1812444 | Inhibition of human recombinant HDAC3 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1848303 | Induction 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%) | 2022 | Bioorganic & medicinal chemistry, Nov-15, Volume: 74 | Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors. |
AID717827 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1855256 | Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1449320 | Antiproliferative activity against human Med8A cells after 72 hrs by Celltiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1441651 | Anti-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 ELISA | 2017 | Journal 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. |
AID1896927 | Antiproliferative activity against human NALM-6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-05, Volume: 75 | Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells. |
AID1273870 | Inhibition of HDAC2 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1709359 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1819535 | Toxicity 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 analysis | 2022 | Journal 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. |
AID1742742 | Genotoxicity in Salmonella typhimurium TA100 by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1845307 | Inhibition of HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Current status in the discovery of dual BET/HDAC inhibitors. |
AID316936 | Inhibition of HDAC7 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1129798 | Inhibition 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1915566 | Cytotoxicity against African green monkey Vero cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1275246 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC. |
AID1170745 | Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1174703 | Induction 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 cytometry | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID1339587 | Growth inhibition of human U937 cells after 44 hrs by MTT assay | 2017 | ACS 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. |
AID324954 | Inhibition of wild type HDAC4 expressed in Escherichia coli at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID1469324 | Induction 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%) | 2018 | Journal 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 |
AID1486321 | Genotoxicity in Salmonella typhimurium TA97 at 50 times antiproliferative IC50 by Ames test | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy. |
AID1511138 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID1861265 | Selectivity index, ratio of IC50 for inhibition of HDAC4 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors. |
AID663473 | Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM | 2012 | Journal 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. |
AID1845914 | Inhibition 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 cytometry | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
AID1534443 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2019 | Journal 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. |
AID1816221 | Induction 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%) | |||
AID274021 | AUC after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID481574 | Cytotoxicity against mouse S180 cells assessed as growth inhibition at 0.1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID246120 | Effective Concentration of compound to inhibit the growth of human MDA-MB-231 cells | 2005 | Journal 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. |
AID1486678 | Inhibition 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 analysis | 2017 | Bioorganic & 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. |
AID1434360 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators. |
AID1235108 | Inhibition 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 assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1622975 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1784980 | Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1061953 | Inhibition of human HDAC3/NCOR2 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1355705 | Antifungal activity against FLC resistant Candida albicans 0304103 after 48 hrs by checkerboard microdilution method | 2018 | Journal 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. |
AID1633433 | Induction of neurogenesis in human SH-SY5Y cells assessed as upregulation of GAP43 mRNA at 1 uM incubated for 24 hrs by RT-PCR analysis | 2019 | ACS 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. |
AID1689776 | Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID695301 | Upregulation of Nanog gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes. |
AID1578157 | Inhibition of FITC-geldanamycin binding to recombinant human full-length C-terminal His-tagged HSP90alpha expressed in Escherichia coli after 3 hrs by fluorescence polarization assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
AID1812436 | Cytotoxicity against human HL-60 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1816723 | Induction 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 %) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1684875 | Antitumor 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) | |||
AID1485114 | Inhibition 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 control | 2017 | Journal 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. |
AID1129799 | Inhibition 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID347872 | Growth inhibition of human renal cancer cells at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Histone deacetylase inhibitors through click chemistry. |
AID366652 | Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1367348 | Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Synthesis and biological evaluation of Santacruzamate-A based analogues. |
AID1486671 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID395022 | Inhibition of recombinant HDAC1 by fluorimetric assay | 2009 | Bioorganic & 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. |
AID1386686 | Inhibition 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 rel | 2018 | Journal 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. |
AID1890513 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1441664 | Anti-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 ELISA | 2017 | Journal 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. |
AID1622972 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1667076 | Inhibition of HDAC6 in human MDA-MB-231 cells assessed as accumulation of acetylated tubulin at 1.5 uM by western blot analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1280274 | Selectivity 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 uM | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1541445 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1784972 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1433254 | Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1572348 | Inhibition of HDAC6 in human HL60 cells assessed as acetylated tubulin/GAPDH ratio at 1 uM after 4 hrs by Western blot assay relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1728924 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 5 days by beckman coulter counting method | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones. |
AID1326527 | Toxicity in nude mouse xenografted with human HCT116 cells assessed as change in body weight at 50 to 100 mg/kg, po qd | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1650411 | Inhibition of recombinant human HDAC4 | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID672024 | Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis | 2012 | Bioorganic & 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. |
AID1403155 | Inhibition of HDAC8 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1441644 | Anti-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 hrs | 2017 | Journal 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. |
AID1401479 | Selectivity 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 cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1622909 | Inhibition of recombinant human GST-fused HDAC1 expressed in HEK293 cells Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1055713 | Antiproliferative activity against human NCI-H460 cells after 48 hrs by SRB assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1482167 | Cytotoxicity against human HL60 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1667070 | Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1380944 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID605533 | Antiproliferative activity against human HepG2 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID1511968 | Inhibition 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 assay | 2019 | ACS 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. |
AID1547265 | Inhibition of HDAC9 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID90214 | Inhibitory activity was tested against histone deacetylase (HDAC). | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
AID1566823 | Antiproliferative activity against human JeKo1 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID1141773 | Induction of apoptosis in human HCT116 cells assessed as increase in p53 protein level at 0.1 to 3 uM after 24 hrs by immunoblotting analysis | 2014 | Journal 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. |
AID1737138 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID241538 | Inhibitory concentration against maize histone deacetylase 1-B (class I HDAC) | 2005 | Journal 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. |
AID1141772 | Cytotoxicity against human HT-29 cells by MTT assay | 2014 | Journal 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. |
AID1846130 | Inhibition of HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 38 | Current status in the discovery of dual BET/HDAC inhibitors. |
AID511065 | Inhibition of HDAC3 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of novel isoxazole-based HDAC inhibitors. |
AID1339568 | Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS 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. |
AID632974 | Cytotoxicity against human AsPC1 cells | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents. |
AID1845917 | Inhibition 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 ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
AID1547331 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID607634 | Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. |
AID1676593 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1821271 | Inhibition of HDAC2 (unknown origin) incubated for 30 mins by microplate reader assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1441661 | Anti-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 method | 2017 | Journal 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. |
AID1653095 | Antiproliferative activity against human A549 cells by CCK8 assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1361644 | Cell 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%) | 2018 | Journal 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. |
AID1321739 | Inhibition 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 control | 2016 | Journal 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. |
AID1578504 | Induction 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 %) | 2020 | ACS 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. |
AID1709349 | Cytotoxicity against human NAMALVA cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1282229 | Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1355735 | Antitumor activity in human HEL cells xenografted in SCID mouse assessed as mouse survival at 10 mg/kg, ip qd measured after 10 days | 2018 | Journal 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. |
AID1406991 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID316926 | Inhibition of human SW620 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1293572 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID492813 | Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
AID496802 | Inhibition of human HDAC2 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID663344 | Growth inhibition of human CCRF-CEM cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID366649 | Antiproliferative activity against human Panc04.03 cells after 72 hrs by MTT assay | 2008 | Journal 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. |
AID1321729 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 after 2 hrs by Western blot analysis | 2016 | Journal 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. |
AID1832693 | Inhibition 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 method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer. |
AID1235109 | Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1739569 | Antiproliferative activity against human HL60 assessed as reduction in cell growth at 20 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1897407 | Induction 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%) | |||
AID404447 | Cytotoxicity against human HPDE6c7 cells | 2008 | Journal 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. |
AID1129795 | Induction 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) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1266840 | Activation 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 analysis | 2015 | Journal 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. |
AID1727743 | Inhibition of HDAC11 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1769651 | Inhibition of ALK (unknown origin) preincubated for 10 mins followed by addition of substrate and ATP for 25 mins by caliper EZ reader method | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID1437243 | Cytotoxicity against mouse B16F10 cells assessed as growth inhibition after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors. |
AID1515982 | Induction of HDAC6 degradation in human MM1S cells assessed as increase in alpha tubulin acetylation at 100 nM measured after 6 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity. |
AID1065630 | Inhibition 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 assay | 2013 | Journal 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. |
AID1312867 | Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay | 2016 | Journal 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. |
AID488275 | Inhibition of HDAC3 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | On the inhibition of histone deacetylase 8. |
AID760501 | Cytotoxicity against human NCI60 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1597973 | Antimigratory activity in human A549 cells at 5 to 10 uM incubated for 12 hrs in presence of mitomycin by inverted microscopic-based wound healing assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1394901 | Inhibition 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 analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1394888 | Inhibition of HDAC in human HeLa nuclear extract using Ac-Lys(Ac)-pNA as substrate measured after 30 mins by fluorometric analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1065634 | Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay | 2013 | Journal 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. |
AID1876471 | Induction 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 %) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors. |
AID1401904 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents. |
AID670970 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID619054 | Competitive inhibition of HDAC9 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID1467234 | Inhibition 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 method | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
AID1869148 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | |||
AID695302 | Upregulation of Sox2 gene expression in C57BL/6 MEF at 100 nM after 24 hrs by quantitative RT-PCR analysis relative to control | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes. |
AID1162485 | Growth inhibition of human HCT116 cells after 72 hrs by CellTiter Glo assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents. |
AID1337279 | Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay | 2016 | Journal 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. |
AID652762 | Inhibition of HDAC3-NCoR2 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | 2011 | ACS 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. |
AID1403153 | Inhibition of HDAC3 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1426426 | Antiparasitic activity against drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as growth inhibition after 48 hrs by SYBR green 1 dye-based flow cytometry | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID760503 | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1511135 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
AID499811 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
AID711156 | Inhibition of HDAC4 by fluorometric assay | 2012 | Journal 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. |
AID1547314 | Increase 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID760519 | Cytotoxicity against human HMEC after 72 hrs by WST1 assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID760373 | Cytotoxicity against HDF after 72 hrs by MTS assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1547259 | Inhibition of human recombinant His-tagged BRD3 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID628287 | Antiproliferative activity against human HepG2 cells after 48 hrs by XTT assay | 2011 | Journal 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. |
AID524998 | Inhibition of HDAC5 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID670013 | Inhibition of human recombinant HDAC1 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID1164798 | Intrinsic clearance in human hepatocytes assessed per million cells at 5 uM by LCMS/MS analysis | 2014 | Journal 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. |
AID1454050 | Induction 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1598103 | Activation 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 cytometry | 2019 | Journal 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. |
AID1614130 | Inhibition 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 | |||
AID1742703 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1251319 | Growth inhibition of human IGROV1/Pt1 cells after 72 hrs | 2015 | Bioorganic & 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. |
AID1737154 | Induction 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%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID1863173 | Inhibition of HDAC3 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay. |
AID1396960 | Antiproliferative activity against human PC3 cells | 2018 | Bioorganic & 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). |
AID1819531 | Toxicity in C57BL/6J mouse implanted with mouse B16-F10 cells assessed as effect on body weight at 60 mg/kg, IG administered for 12 days | 2022 | Journal 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. |
AID603542 | Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader | 2011 | Journal 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. |
AID434539 | Cytotoxicity against human HCT116 cells after 24 hrs by sulforhodamine B assay | 2009 | Bioorganic & 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. |
AID1598093 | Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay | 2019 | Journal 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. |
AID586608 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID1784187 | Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 90 mins by fluorescence based micro plate assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis. |
AID322422 | Antitumor activity against human LNCap cells xenografted SCID mouse model at 20 to 10 mg/kg/day, sc relative to control | 2008 | Bioorganic & 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. |
AID1200985 | AUC (0 to infinity) in ICR mouse at 50 mg/kg, po | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
AID1890334 | Stability in human liver microsomes assessed as half-life and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1126999 | Induction 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%) | 2014 | Journal 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. |
AID1227046 | Drug degradation in human plasma assessed as unidentifiable product formation after 2 hrs by HPLC analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID1349721 | Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1633992 | Inhibition of HDAC6 in human HuH7 cells assessed as increase in alpha-tubulin K40 acetylation at varying concentrations incubated for 24 hrs by Western blot analysis | 2019 | Bioorganic & 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). |
AID761580 | Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID1061955 | Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1361638 | Inhibition of HDAC in human A549 cells assessed as increase in histone H3 acetylation after 24 hrs by Western blot analysis | 2018 | Journal 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. |
AID1487087 | Selectivity index, ratio of IC50 for HDAC6 (unknown origin) to IC50 for HDAC3 (unknown origin) | 2017 | Bioorganic & 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. |
AID1659656 | Antiproliferative activity against human A549 cells incubated for 24 hrs by CCK8 assay | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID1808548 | Inhibition 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 assay | 2021 | Journal 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). |
AID1900936 | Toxicity 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) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID350725 | Growth inhibition of human HBC5 cells after 48 hrs by sulforhodamine B assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID488355 | Agonist 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 analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids. |
AID352522 | Antiproliferative activity against human HUPT3 cells by MTT assay | 2009 | Bioorganic & 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. |
AID1886182 | Inhibition 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 control | 2022 | Journal 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. |
AID1572377 | Ratio 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 uM | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID1742627 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1449682 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1667071 | Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1578476 | Inhibition 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 assay | 2020 | ACS 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. |
AID1166497 | Inhibition of human recombinant full length HDAC3 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins | 2014 | Bioorganic & 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. |
AID1401477 | Selectivity 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 cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1865303 | Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on kidney at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID297484 | Cytotoxicity against human A2780 cells | 2007 | Journal 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. |
AID1676590 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1485112 | Inhibition 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 control | 2017 | Journal 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. |
AID1441675 | Anti-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) | 2017 | Journal 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. |
AID1882457 | Inhibition of HDAC2 (unknown origin) | 2022 | Journal 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. |
AID90344 | Induction of p21 using Histone deacetylase inhibitors | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4 | Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1578495 | Induction 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 %) | 2020 | ACS 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. |
AID593549 | Inhibition of human HDAC4 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID1164914 | Inhibition of HDAC9 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1887063 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis. |
AID1722284 | Inhibition 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 analysis | 2020 | Bioorganic & medicinal chemistry, 09-01, Volume: 28, Issue:17 | The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells. |
AID1380943 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2018 | Journal 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. |
AID1848618 | Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition at 10 uM incubated for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
AID438217 | Inhibition of HDAC8 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide. |
AID1246523 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human K562 cells | 2015 | Bioorganic & 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. |
AID1742663 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1177053 | Antiprotozoan activity against Plasmodium falciparum NF54 IEF forms | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID1541460 | Inhibition 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 assa | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID1865301 | Toxicity in BALB/c mouse model allografted with mouse 4T1 cells assessed as effect on spleen at 40 mg/kg, po qd administered for 12 days | 2022 | Journal 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. |
AID294382 | Inhibition of HDAC by fluorescent assay | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid. |
AID663470 | Half life in mouse liver microsomes | 2012 | Journal 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. |
AID608776 | Inhibition of HDAC in human HeLa cells using Ac-Arg-Gly-Lys(Ac)-AMC as fluorescent substrate after 20 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Structure-based optimization of click-based histone deacetylase inhibitors. |
AID1128561 | Inhibition of human HDAC-8 using RHK(Ac)K(Ac) as substrate | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
AID663352 | Growth inhibition of human NCI-H226 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID420646 | Antitumor 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 weeks | 2009 | European 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. |
AID1740129 | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1875509 | Cytotoxicity against HMEC cells assessed as inhibition of cell growth incubated for 3 days by alamar blue assay | 2022 | ACS medicinal chemistry letters, Oct-13, Volume: 13, Issue:10 | Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. |
AID274169 | Antiproliferative activity against H661 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID609495 | Ratio of IC50 for CYP3A4 to IC50 for human HCT116 cells | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1514613 | Induction 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 %) | 2019 | Bioorganic & 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. |
AID1771460 | Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
AID1886174 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2022 | Journal 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. |
AID1898909 | Antiproliferative 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 assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1742652 | Cytotoxicity against human BT-549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1821963 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | |||
AID1742651 | Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1403180 | Inhibition of ERK1/2 phosphorylation in human HepG2 cells at 2 uM after 48 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1650409 | Inhibition of recombinant human HDAC8 | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. |
AID717658 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1127319 | Antiproliferative activity against human H460 cells assessed as growth inhibition after 72 hrs | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1227030 | Inhibition of human recombinant HDAC2 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release. |
AID737917 | Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis | 2013 | Journal 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. |
AID1281868 | Induction 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%) | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1890333 | Stability in mouse liver microsomes assessed as clearance and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
AID1623524 | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate-3 by fluorescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID618084 | Toxicity 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 19 | 2011 | Journal 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. |
AID1281850 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1901057 | Inhibition of HDAC6 (unknown origin) using trypsin and Ac-peptide as substrates | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID408881 | Inhibition of HDAC2 | 2008 | Journal 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. |
AID1441655 | Anti-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 micro | 2017 | Journal 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. |
AID1398811 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1566824 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy. |
AID316872 | Inhibition of HDAC from human K562 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID476830 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID619141 | 1-Octanol-sodium phosphate buffer distribution coefficient, log D of the compound at pH 7.4 | 2011 | Journal 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. |
AID1406983 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
AID316901 | Inhibition of human MDA-MB-231 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID366642 | Inhibition of HDAC3 after 17 hrs | 2008 | Journal 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. |
AID1476154 | Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1485127 | Cell 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 cytometry | 2017 | Journal 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. |
AID1901152 | Inhibition 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 assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1281869 | Induction 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%) | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID747261 | Growth inhibition of human A549 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry. |
AID1497924 | Induction 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 analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | Development of the first small molecule histone deacetylase 6 (HDAC6) degraders. |
AID1170743 | Inhibition of human recombinant HDAC8 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. |
AID1312899 | Toxicity 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 dose | 2016 | Journal 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. |
AID1421922 | Antimalarial 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 | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID327549 | Cytotoxicity against human HCT116 cells assessed as cell viability after 96 hrs by MTS reduction assay | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID1433301 | Induction 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 control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1401481 | Selectivity 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 lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
AID1303685 | Inhibition of HDAC1 in human Jurkat cells extract after 30 mins by immunoprecipitation assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1690105 | Inhibition of HSP90a (unknown origin) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID480067 | Inhibition of human recombinant HDAC2 preincubated for 1 hr with substrate by protease coupled end-point assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. |
AID663378 | Growth inhibition of human LOXIMVI cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1225977 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1398803 | Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID274066 | AUC after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID304372 | Inhibition of human IMPDH 2 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. |
AID1819554 | Antitumor 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 analysis | 2022 | Journal 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. |
AID1462022 | Inhibition of HDAC in human HeLa nuclear extract preincubated for 5 mins followed by Boc-Lys (acetyl)-AMC addition measured after 10 mins by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. |
AID350722 | Ratio of GI50 for human MKN45 cells to IC50 for HDAC in human HeLa cells | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID725666 | Selectivity 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 analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
AID672027 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID1373246 | Inhibition of HDAC6 (unknown origin) preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold. |
AID1597939 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1727733 | Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID1856996 | Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Journal 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. |
AID1812469 | Antiplasmodial 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 hrs | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. |
AID1401542 | Antiproliferative activity against human U2932 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1441654 | Inhibition of LTB4 biosynthesis in LPS-induced C57BL/6 mouse model of acute lung injury BLAF administered intraperitoneally by ELISA | 2017 | Journal 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. |
AID1164040 | Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1126961 | Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2014 | Journal 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. |
AID421214 | Inhibition of HDAC6 from human HeLa cells at 5 uM | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Recent advances in the development of polyamine analogues as antitumor agents. |
AID586610 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID297470 | Inhibition of HDAC in HeLa cells | 2007 | Journal 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. |
AID524993 | Inhibition 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 control | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1 | Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1439772 | Inhibition 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 assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa. |
AID1308511 | Inhibition of HDAC (unknown origin) | 2016 | Bioorganic & 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. |
AID352519 | Inhibition of human recombinant HDAC2 | 2009 | Bioorganic & 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. |
AID1677516 | Inhibition 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 assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1469495 | Antitumor 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 control | 2018 | Journal 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 |
AID1898921 | Induction of DNA damage in human NCI-H460 cells at 7.4 uM assessed as increase in p-H2AX levels and measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1055349 | Cytotoxicity against human HDF after 72 hrs by MTS-PMS assay | 2013 | Journal 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. |
AID663355 | Growth inhibition of human NCI-H460 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1235113 | Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. |
AID1399559 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID476831 | Toxicity 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) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. |
AID1688043 | Induction of HDAC6 degradation in human HL-60 cells assessed as decrease in HDAC6 level at 2 uM incubated for 12 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1060993 | Inhibition of HDAC in human HeLa cell nuclear extract using fluor de Lys as substrate at 1 uM after 15 mins by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors. |
AID1390011 | Inhibition 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 assay | 2018 | Bioorganic & 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. |
AID1622912 | Inhibition of HDAC1/HDAC2 in human HeLa nuclear extract | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1769656 | Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
AID352525 | Antiproliferative activity against human SU-8686 cells by MTT assay | 2009 | Bioorganic & 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. |
AID1639362 | Inhibition 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 assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors. |
AID1398813 | Antagonist 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 analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 | Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
AID1162227 | Induction 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%) | 2014 | Bioorganic & 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. |
AID1464874 | Anti-proliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID1164782 | Inhibition of HDAC3 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | 2014 | Journal 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. |
AID1336929 | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1869150 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM incubated for 48 hrs by CCK8 assay | |||
AID1869151 | Cytotoxicity against human L02 cells assessed as cell viability at 10 uM incubated for 48 hrs by CCK8 assay | |||
AID1667079 | Inhibition of STAT3 in human MDA-MB-231 cells assessed as upregulation of p-p38 expression after 24 hrs by western blot analysis | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID1061951 | Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors. |
AID1281853 | Antiproliferative activity against human NCI-H929 cells after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy. |
AID1336922 | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID544095 | Cytotoxicity against african green monkey Vero cells by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1709346 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1421906 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID613292 | Plasma concentration in dog at 150 mg/kg, po administered as single dose | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID1177049 | Cytotoxicity against human NCI-H460 cells | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID673993 | Inhibition of recombinant HDAC6 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. |
AID1462216 | Inhibition of recombinant human HDAC1 at 1 uM after 30 mins by fluorescence assay relative to control | 2017 | Bioorganic & 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. |
AID1390021 | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap. |
AID1454034 | Growth inhibition of human HL60 cells after 3 days by counting method | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. |
AID1821337 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1548272 | Induction 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%) | |||
AID482951 | Antiproliferative activity against human HCT116 cells | 2010 | Bioorganic & 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. |
AID1882462 | Inhibition of HDAC6 (unknown origin) | 2022 | Journal 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. |
AID1476152 | Antiproliferative activity against human Jurkat cells | 2017 | Journal 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. |
AID1515884 | Induction 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%) | 2019 | Journal 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. |
AID1394886 | Antiproliferative activity against human NCI-H1975 cells after 48 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1876342 | Inhibition of recombinant full length human HDAC6 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID1321723 | Cytotoxicity against human THLE2 cells assessed as reduction in cell viability after 72 hrs by ATP Vialight assay | 2016 | Journal 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. |
AID1697199 | Cytotoxicity against human NCI-H23 cells by colorimetric method | 2020 | Bioorganic & 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. |
AID1742743 | Genotoxicity in Salmonella typhimurium TA1535 by Ames test | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID1393286 | Inhibition 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 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds. |
AID1549137 | Antifungal activity against azole-resistant Candida albicans 0304103 after 48 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID328806 | Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay | 2008 | Journal 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. |
AID371221 | Inhibition of histone deacetylase in human HeLa cells assessed as induction of histone H3 hyperacetylation | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-mercaptoketone based histone deacetylase inhibitors. |
AID1063036 | Inhibition of recombinant HDAC10 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1 | Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
AID1865248 | Metabolic stability in mouse liver microsome measured at 2 hrs in presence of NADPH | 2022 | Journal 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. |
AID659636 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1732190 | Cytotoxicity against human HH cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition. |
AID1702050 | Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID1873382 | Inhibition of HDAC2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1476155 | Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID70687 | Percent of murine erythroleukemia cells that became benzidine reactive after administration (2.5 uM) | 1995 | Journal 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. |
AID1390012 | Inhibition 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 additi | 2018 | Bioorganic & 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. |
AID591328 | Inhibition of HDAC in human HeLa cells at 10 uM by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors. |
AID1550100 | Inhibition 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 assay | 2019 | Journal 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. |
AID1181303 | Inhibition of human recombinant HDAC1 using histone H3 substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 | 1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. |
AID1702197 | Toxicity 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%) | 2018 | Journal 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. |
AID274014 | Percent inhibition of CYP450 1A2 at 1 uM concentration | 2007 | Bioorganic & 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. |
AID1605965 | Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1065962 | Cytotoxicity against androgen-independent human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24 | Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
AID723467 | Inhibition of HDAC in cisplatin resistant human KYSE-510 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID1337287 | Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1174694 | Inhibition of HDAC3 (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. |
AID446346 | Volume of distribution at steady state in CD1 mouse at 15 mg/kg, po | 2010 | Journal 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. |
AID708276 | Growth inhibition of human Bel7404 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID1203891 | Inhibition of recombinant HDAC8 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors. |
AID1890516 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1361630 | Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1864224 | Inhibition of full length recombinant C-terminal GST-tagged human HDAC1 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay | 2022 | Journal 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. |
AID374812 | Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID1614126 | Inhibition 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 | |||
AID374820 | Inhibition of C-terminal FLAG-tagged HDAC6 expressed in mammalian cells | 2009 | Journal 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. |
AID300833 | Growth inhibition of human PC3 cells after 21 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera. |
AID374826 | Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay | 2009 | Journal 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. |
AID1493602 | Inhibition 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 analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
AID1811371 | Inhibition 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID449262 | Antiproliferative activity against human A549 cells after 2 days by MTT assay | 2009 | European 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. |
AID708271 | Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay | 2012 | Journal 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. |
AID605621 | Cell 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 analysis | 2010 | Journal 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. |
AID1727740 | Inhibition of HDAC3 (unknown origin) by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes. |
AID732875 | Inhibition 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 assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Development of |
AID1764280 | Inhibition 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 | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
AID1845460 | Inhibition of HDAC6 (unknown origin) | 2021 | Journal 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? |
AID1855257 | Antiproliferative activity against mouse MC38 cells after 48 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity. |
AID1337286 | Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo assay | 2016 | Journal 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. |
AID1431816 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1765325 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID749704 | Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1361628 | Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay | 2018 | Journal 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. |
AID1785341 | Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay | |||
AID373080 | Inhibition of human recombinant HDAC7 | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR. |
AID304374 | Antiproliferative activity against human K562 cells after 72 hrs by MTS assay | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. |
AID1537568 | Cell 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 %) | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
AID1466055 | Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo. |
AID1605975 | Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal 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. |
AID1653141 | Cytotoxicity against human SW620 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Quinolone hybrids and their anti-cancer activities: An overview. |
AID1821350 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID274030 | Permeability (Papp) run from pH 6.5-7.4 | 2007 | Bioorganic & 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. |
AID327546 | Increase in acetylated histone H4 level in human HCT116 cells at 10 uM after 24 hrs relative to control | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors. |
AID1337306 | Inhibition 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 method | 2016 | Journal 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. |
AID762188 | Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay | 2013 | Journal 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. |
AID1433252 | Antiproliferative activity against human CMK cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1578502 | Induction 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 %) | 2020 | ACS 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. |
AID258012 | Inhibition of human leukemic CEM cell viability | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. |
AID1525777 | Inhibition of HADC1 (unknown origin) | 2020 | Journal 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. |
AID1849158 | Inhibition 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 analysis | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
AID1655892 | Inhibition 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) | 2020 | ACS 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. |
AID304375 | Differentiation of K562 cells at 0.50 uM after 5 days by MTS assay | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. |
AID609726 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
AID1915597 | Inhibition of HDAC11 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1234902 | Antiproliferative activity against human ES2 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1436788 | Growth inhibition of human NCI-H292 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity. |
AID761584 | Inhibition of HDAC in human HeLa cell extract using fluor de Lys as substrate after 15 mins by fluorometric analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID1897488 | Antitumor 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 | |||
AID1542189 | Inhibition of HDAC11 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
AID440466 | Metabolic stability in Sprague-Dawley rat plasma at 10 uM by LC-MS/MS analysis | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Hydroxamates: relationships between structure and plasma stability. |
AID1404339 | Inhibition 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 assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1897370 | Inhibition of FGFR2 (unknown origin) | |||
AID243592 | Percent inhibition against human histone deacetylase at 100 uM | 2005 | Journal 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. |
AID420642 | Inhibition of HDAC6 in human IGROV1 cells assessed as alpha-tubulin acetylation at IC80 after 24 hrs by Western blot | 2009 | European 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. |
AID1441641 | Anti-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 microsc | 2017 | Journal 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. |
AID462791 | Antiproliferative activity against human SKOV3 cells after 48 hrs by MTT assay | 2010 | Bioorganic & 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. |
AID1240555 | Induction 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%) | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors. |
AID1518779 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1587860 | Inhibition 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 assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
AID1816190 | Inhibition of recombinant HDAC7 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | |||
AID1164194 | Inhibition of HDAC in human MCF7 cells assessed as hyperacetylation of p21 at 5 uM after 24 hrs by Western blot analysis relative to control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. |
AID1659649 | Inhibition of HDAC3 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11 | Environment-sensitive fluorescent inhibitors of histone deacetylase. |
AID670515 | Antiproliferative activity against human A431 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
AID1541558 | Inhibition of HDAC6 in human Cal27CisR cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID214058 | Compound was tested for anti-proliferative activity in U-937 human leukemia cell line | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. |
AID1441665 | Anti-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 ELISA | 2017 | Journal 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. |
AID1688031 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID462790 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2010 | Bioorganic & 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. |
AID1515887 | Induction 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 analysis | 2019 | Journal 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. |
AID90689 | Tested for maize Histone deacetylase 2 inhibitory activity | 2003 | Journal 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. |
AID1273867 | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTitre-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. |
AID1876343 | Inhibition of recombinant full length human HDAC8 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
AID1352481 | Inhibition of HDAC2 in human HeLa cells after 72 hrs by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation. |
AID1321698 | Selectivity ratio of pLC50 for mouse primary glial cells to pLC50 for human THLE2 cells | 2016 | Journal 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. |
AID1742666 | Cytotoxicity against human PANC-1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer. |
AID465158 | Growth inhibition of human Panc 04.03 cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1260638 | Inhibition of human recombinant HDAC2 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | |||
AID1689775 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID288449 | Growth inhibition of HCT15 cells by SRB assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors. |
AID619050 | Competitive inhibition of HDAC5 using KI-104 as substrate by fluorescence assay | 2011 | Journal 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. |
AID545857 | Antimalarial activity against Plasmodium falciparum FCR3 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice. |
AID1689771 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth at 8 uM measured after 72 hrs by CCK-8 assay relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID717821 | Inhibition 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 assay | 2012 | Bioorganic & 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. |
AID1739567 | Antiproliferative activity against human THP-1 assessed as reduction in cell growth at 4 uM by CellTiter-non radioactive cell proliferation assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. |
AID1478587 | Induction 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%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors. |
AID1321619 | Inhibition 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 analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy. |
AID1467032 | Stabilization 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 assay | 2017 | Journal 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. |
AID1826633 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID1234903 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors. |
AID1404298 | Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2 | Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors. |
AID1597956 | Induction 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%) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors. |
AID1737133 | Inhibition 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 assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening. |
AID672035 | Ratio of inhibition of human HDAC3 at 10 uM preincubated for 3 hrs to inhibition of human HDAC3 at 10 uM preincubated for 5 mins | 2012 | Bioorganic & 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. |
AID1890511 | Inhibition of HDAC2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID1859936 | Antiproliferation activity against human HCT-116 cells assessed as reduction in cell viability at 5 to 50 uM measured after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Azetidin-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. |
AID659637 | Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 protein expression at 2.5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID761579 | Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID1548264 | Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay | |||
AID274023 | Oral bioavailability after oral dosing at 5 mg kg-1 | 2007 | Bioorganic & 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. |
AID1689811 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth at 2 uM measured after 72 hrs by CCK-8 assay relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. |
AID659492 | Inhibition of HDAC1/2 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors. |
AID1784189 | Inhibition of recombinant human HDAC1 using ZMAL as substrate incubated for 90 mins by fluorescence based micro plate assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis. |
AID1206753 | Cell 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%) | 2015 | Journal 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. |
AID473192 | Growth inhibition of human MUF cells after 48 hrs by MTT assay | 2010 | Journal 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. |
AID1266831 | Induction of apoptosis in human HCT116 cells at 5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis | 2015 | Journal 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. |
AID1436789 | Growth inhibition of human NCI-H292 cells after 72 hrs in presence of LDL by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity. |
AID1545989 | Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1269321 | Cytotoxicity against human A2780S/CP5 cells assessed as cell growth at 25 uM measured at 72 hrs by CyQuant proliferation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida). |
AID725668 | Inhibition 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 af | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
AID1702056 | Inhibition 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 assay | 2018 | Journal 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. |
AID1777024 | Inhibition 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 assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Intracellular fluorescence competition assay for inhibitor engagement of histone deacetylase. |
AID1550107 | Inhibition 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 analysis | 2019 | Journal 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. |
AID1896951 | Cytotoxicity against human HUVEC cells assessed as reduction in cell viability by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, Nov-05, Volume: 75 | Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells. |
AID1239053 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by CCK8 assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors. |
AID1282244 | Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal 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. |
AID1578888 | Inhibition of human HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2019 | Journal 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. |
AID297480 | Cytotoxicity against human MDA-MB-468 cells | 2007 | Journal 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. |
AID1403181 | Inhibition of HDAC1 in human HepG2 cells assessed as upregulation of acetyl-histone H3 levels at 5 uM after 48 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID1622913 | Inhibition of HDAC3 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1293567 | Inhibition 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 assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity. |
AID717825 | Inhibition of HDAC6 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | 2012 | Bioorganic & 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. |
AID1250645 | Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID613343 | Inhibition of human ERG at 30 uM | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. |
AID316875 | Inhibition of HDAC from human HeLa cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1487012 | Selectivity index, ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC8 (unknown origin) | 2017 | Bioorganic & 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. |
AID1282294 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as death at 100 mg/kg, po q2d for 8 days | 2016 | Journal 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. |
AID1403172 | Antimetastatic activity in human HepG2 cells assessed as reduction in cell invasion at 1 uM after 48 hrs by crystal violet staining-based transwell invasion assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID761583 | Inhibition of full length His-tagged human recombinant HDAC1 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring. |
AID1421917 | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID663472 | Inhibition of human CYP3A4 | 2012 | Journal 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. |
AID310187 | Antitumor activity against MDA-MB-231 cells xenografted BALB/c nude mouse assessed as body weight at 30 mg/kg, ip for 15 days | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors. |
AID1819539 | Antitumor immunity against mouse B16-F10 cells implanted in C57BL/6J mouse assessed as increase in proportion of T cells in spleen by flow cytometry analysis | 2022 | Journal 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. |
AID1431812 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1476159 | Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent assay | 2017 | Journal 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. |
AID1547269 | Inhibition of HDAC3 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1753841 | Selectivity index, ratio of IC50 for inhibition of HDAC2 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
AID1765330 | Selectivity index, ratio of IC50 for human recombinant full length HDAC3 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1702156 | Inhibition of human ERG by fluorescence polarization assay | 2018 | Journal 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. |
AID1897508 | Antiangiogenic 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 | |||
AID1529550 | Cytotoxicity against human PBL cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1164041 | Antiproliferative activity against human U937 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID675296 | Inhibition of HDAC in human HeLa cell extracts using Fluor de Lys as substrate at 0.01 uM by fluorescence assay | 2012 | Bioorganic & 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. |
AID1349722 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID1709360 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1863433 | Inhibition of HDAC1 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1699969 | Antiproliferative activity against human K562 cells by MTT assay | 2020 | Bioorganic & 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. |
AID1623535 | Selectivity index, ratio of IC50 for human recombinant HDAC3 to IC50 for human recombinant HDAC6 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | A novel class of anthraquinone-based HDAC6 inhibitors. |
AID723479 | Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay | 2013 | Journal 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. |
AID609489 | Inhibition of purified recombinant HDAC1 | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. |
AID1864677 | Inhibition 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 | |||
AID1449339 | Inhibition 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 | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
AID1677498 | Induction of mitochondrial membrane potential loss in human HeLa cells at 1 to 3 uM after 24 hrs by TMRE staining based fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells. |
AID1709367 | Induction 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%) | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1821958 | Inhibition 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 | |||
AID1826624 | Synergistic 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-one | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. |
AID274026 | Steady state volume of distribution (Vdss) after i.v. dosing at 1 mg kg-1 | 2007 | Bioorganic & 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. |
AID274097 | Effect of compound on Candida albicans sensitivity to Fluconazole: Minimum inhibitory concentration required to inhibit the growth of 50% of isolates after 24h. | 2007 | Bioorganic & 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. |
AID274078 | Inhibition of MDA-MB-231 cell proliferation (mean of two experiments) | 2007 | Bioorganic & 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. |
AID1890509 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
AID744875 | Inhibition of mouse liver HDAC by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Discovery of adamantane based highly potent HDAC inhibitors. |
AID1502983 | Inhibition of MAOA (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment. |
AID1547343 | Inhibition 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 analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1753637 | Selectivity index, ratio of IC50 for inhibition of human HDAC1 to IC50 for inhibition of human HDAC6 | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
AID1549165 | Inhibition of HDAC6 (unknown origin) after 30 mins by fluorescence based assay | 2020 | Journal 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. |
AID1164910 | Inhibition of HDAC5 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID1511970 | Inhibition 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 assay | 2019 | ACS 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. |
AID1810051 | Inhibition 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 | |||
AID663377 | Growth inhibition of human U251 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1880243 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 3 days by trypan blue assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | The |
AID1535339 | Inhibition 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 assay | 2019 | Bioorganic & 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. |
AID1758465 | Phototoxicity 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 assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy. |
AID1280309 | Inhibition of human KDAC8 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1785345 | Inhibition 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 | |||
AID1206763 | Inhibition 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 assay | 2015 | Journal 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. |
AID1622976 | Inhibition 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 assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1816208 | Induction 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%) | |||
AID1476118 | Cytotoxicity against TAMH cells assessed as cell viability after 24 hrs by CellTiter-Glo assay | 2017 | Journal 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. |
AID1614257 | Toxicity 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 | |||
AID1245683 | Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors. |
AID1225990 | Induction 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%) | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors. |
AID1652191 | Inhibition 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 assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1164037 | Antiproliferative activity against human BGC823 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors. |
AID1676598 | Binding 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 chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
AID1503840 | Inhibition 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 fluoresce | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models. |
AID1821262 | Toxicity 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 method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. |
AID1784977 | Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID1126979 | Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay | 2014 | Journal 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. |
AID1873386 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study. |
AID1808545 | Inhibition 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 assay | 2021 | Journal 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). |
AID1667072 | Cytotoxicity against African Green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2020 | Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6 | Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. |
AID274017 | Percent inhibition of CYP450 2C19 at 1 uM concentration | 2007 | Bioorganic & 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. |
AID297490 | Cytotoxicity against human AsPC1 cells | 2007 | Journal 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. |
AID1752941 | Cytotoxicity 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 | |||
AID1816699 | Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1784975 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma. |
AID593555 | Inhibition of human HDAC10 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | 2011 | Journal 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. |
AID759304 | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID1647336 | Upregulation 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 analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1515904 | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay | 2019 | Journal 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. |
AID1549136 | Antifungal activity against azole-sensitive Candida albicans SC5314 after 48 hrs by spectrophotometry-based serial microdilution method | 2020 | Journal 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. |
AID1266094 | Inhibition of HDAC3 (unknown origin) by fluorimetric assay | 2016 | Bioorganic & 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. |
AID1598094 | Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay | 2019 | Journal 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. |
AID1250648 | Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay | 2015 | Journal 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. |
AID1730867 | cytotoxicity against human HL-7702 cells assessed as reduction of cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1421907 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1514604 | Inhibition 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) | 2019 | Bioorganic & 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. |
AID1173503 | Inhibition 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 assay | 2014 | Bioorganic & 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. |
AID1386705 | Inhibition 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 analysis | 2018 | Journal 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. |
AID1394885 | Antiproliferative activity against human HL60 cells after 48 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1811363 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer. |
AID663346 | Growth inhibition of human K562 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID780588 | Inhibition 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 assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. |
AID1312891 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as mortality at 50 mg/kg, ip administered every 2 days for 8 days | 2016 | Journal 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. |
AID246067 | Effective Concentration of compound to inhibit the growth of human DU-145 cells | 2005 | Journal 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. |
AID1754808 | Upregulation of SIRT2 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1762488 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors. |
AID604138 | Inhibition 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 blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). |
AID609724 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
AID1421920 | Antiplasmodial activity against exo-erythrocytic stage of GFP-Luc-fused Plasmodium berghei ANKA infected in human HepG2 cells after 48 hrs by bioluminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID1326510 | Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID605532 | Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay | 2010 | Journal 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. |
AID344918 | Inhibition of 2-oxoglutarate-dependent human JMJD2E preincubated for 30 mins by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID1403182 | Inhibition of HDAC6 in human HepG2 cells assessed as upregulation of acetyl-alpha-tubulin levels at 5 uM after 48 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
AID241537 | Inhibitory concentration against maize histone deacetylase 1-A (class IIa HDAC) | 2005 | Journal 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. |
AID481546 | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition at 10 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1126995 | Induction 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%) | 2014 | Journal 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. |
AID1280276 | Inhibition 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 control | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
AID1486669 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | Bioorganic & 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. |
AID297483 | Cytotoxicity against human SK-OV-3 cells | 2007 | Journal 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. |
AID1563942 | Inhibition of recombinant HDAC3 (unknown origin) measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. |
AID348793 | Antiproliferative activity against human HeLa cells after 72 hrs by celltiter-blue viability assay | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization of a series of potent and selective ketone histone deacetylase inhibitors. |
AID328795 | Inhibition of HDAC3 | 2008 | Journal 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. |
AID465154 | Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1408193 | Inhibition of MOF in human HCT116 cells assessed as decrease in H4K16 acetylation level after 24 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening. |
AID1897400 | Induction 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%) | |||
AID586607 | Antimalarial 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 serum | 2011 | Antimicrobial 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. |
AID1162220 | Cell 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%) | 2014 | Bioorganic & 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. |
AID1897371 | Inhibition of FGFR3 (unknown origin) | |||
AID1754751 | Inhibition 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 fluoresc | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1882089 | Inhibition of HDAC1 (unknown origin) using fluorimetric substrate incubated for 30 mins by fluorogenic assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Medicinal chemistry updates of novel HDACs inhibitors (2020 to present). |
AID1337255 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1514598 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2019 | Bioorganic & 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. |
AID1816187 | Inhibition of HDAC3 (unknown origin) incubated for 60 mins using microplate reader analysis | |||
AID1326522 | Inhibition of His-tagged full length recombinant human HDAC8 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. |
AID1129791 | Induction 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID1275593 | Inhibition of HDAC in mouse forebrain primary neurons assessed as acetylation of histone H3K9 after 24 hrs by immunofluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. |
AID1547247 | Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Discovery of Thieno[2,3- |
AID1599789 | Inhibition 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 analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling. |
AID1702082 | Antiproliferative activity against human SNU-387 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal 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. |
AID438219 | Inhibition of HDAC6 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide. |
AID1865271 | Inhibition of HDAC in human MV4-11 cells assessed as upregulation of acetylated H3 level incubated for 24 hrs by Western blot analysis | 2022 | Journal 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. |
AID316891 | Inhibition of HDAC | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Histone deacetylase inhibitors: from bench to clinic. |
AID1129788 | Induction 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%) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells. |
AID639364 | Clearance in mouse | 2011 | Journal 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. |
AID1550157 | Toxicity 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 ruxolitinib | 2019 | Journal 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. |
AID1688037 | Induction 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 %) | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects. |
AID1816199 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | |||
AID546560 | Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay | 2010 | Journal 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. |
AID1449227 | Inhibition 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 r | 2017 | Journal 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. |
AID1482168 | Cytotoxicity against human MOLT4 cells assessed as growth inhibition at 5 uM after 48 hrs by MTT assay relative to control | 2017 | Journal 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. |
AID1215097 | Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis relative to dexamethasone | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Identification of clinically used drugs that activate pregnane X receptors. |
AID1303630 | Potentiation 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
AID1260649 | Inhibition 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 | |||
AID710840 | Cytotoxicity against human PC3 cells assessed as growth inhibition by SRB assay | 2012 | Journal 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. |
AID663351 | Growth inhibition of human HOP92 cells after 72 hrs by MTS assay | 2012 | Journal 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. |
AID1900918 | Induction of apoptosis in mouse GL26 cells assessed as proteolytic cleavage of PARP1 incubated for 48 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | |
AID541649 | Inhibition of human HDAC5 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1349718 | Inhibition of NAMPT (unknown origin) using NAM as substrate incubated for 5 mins followed by substrate addition measured after 15 mins by fluorometric method | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1 | Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. |
AID481551 | Cytotoxicity against human HO8910 cells assessed as growth inhibition at 1 ug/ml after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Synthesis and anticancer evaluation of alpha-lipoic acid derivatives. |
AID1864251 | Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability | 2022 | Journal 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. |
AID1164911 | Inhibition of HDAC6 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. |
AID313733 | Inhibition of HDAC5 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). |
AID1754760 | Downregulation of HDAC1 gene expression in human MCF7 cells at 3 uM incubated for 24 hrs by whole transcriptome analysis | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents. |
AID1798524 | HDAC Activity Assay from Article 10.1021/jm800079s: \\A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.\\ | 2008 | Journal 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. |
AID1797826 | HDAC Enzyme Activity Assay from Article 10.1021/jm0703800: \\The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.\\ | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. |
AID1802589 | HDAC2 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.\\ | 2017 | Bioorganic chemistry, 04, Volume: 71 | Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity. |
AID1798419 | HDAC 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.\\ | 2008 | Journal 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. |
AID1800141 | In 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.\\ | 2013 | Chemical 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. |
AID1802011 | HDAC6 fluorescence anisotropy assay from Article 10.1038/nchembio.2134: \\Histone deacetylase 6 structure and molecular basis of catalysis and inhibition\\ | 2016 | Nature chemical biology, 09, Volume: 12, Issue:9 | Histone deacetylase 6 structure and molecular basis of catalysis and inhibition. |
AID1802356 | Inhibitor Competition Assay from Article 10.1021/acschembio.6b00776: \\LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.\\ | 2017 | ACS chemical biology, 01-20, Volume: 12, Issue:1 | LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation. |
AID1801572 | In-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.\\ | 2016 | ACS 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. |
AID1802920 | HDAC Activity Assay from Article 10.3109/14756360903049034: \\Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.\\ | 2010 | Journal 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. |
AID1799021 | pfHDAC-1 Enzyme Assay from Article 10.1021/jm801654y: \\Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.\\ | 2009 | Journal 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. |
AID1798635 | FDH Coupled Inhibition Assay from Article 10.1021/jm800936s: \\Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases.\\ | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID1802398 | Enzymatic 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.\\ | 2013 | The 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. |
AID1800408 | HDAC8 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 simi | 2013 | Biochemistry, 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. |
AID1802059 | In vitro HDAC8 Assay from Article 10.1111/cbdd.12778: \\Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.\\ | 2016 | Chemical biology & drug design, 10, Volume: 88, Issue:4 | Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents. |
AID1794865 | Enzyme inhibition assay from Article 10.3109/14756366.2013.827678: \\Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.\\ | 2014 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 29, Issue:4 | Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors. |
AID1798526 | HDAC Activity Assay from Article 10.1016/j.bmcl.2008.02.025: \\Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.\\ | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
AID1802239 | In 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.\\ | 2017 | Chemical biology & drug design, Jan, Volume: 89, Issue:1 | Design, synthesis, and preliminary bioactivity evaluation of N |
AID1802399 | Proteros 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.\\ | 2013 | The 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. |
AID1794854 | HDAC Activity screening from Article 10.3109/14756366.2013.827675: \\Quinolone-based HDAC inhibitors.\\ | 2014 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 29, Issue:4 | Quinolone-based HDAC inhibitors. |
AID1798196 | Enzyme Inhibition Assay from Article 10.1021/jm7015254: \\Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.\\ | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Structural origin of selectivity in class II-selective histone deacetylase inhibitors. |
AID1800409 | HDAC8 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, tri | 2013 | Biochemistry, 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. |
AID1798784 | HDAC Activity Assay from Article 10.1021/jm801128g: \\Non-peptide macrocyclic histone deacetylase inhibitors.\\ | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Non-peptide macrocyclic histone deacetylase inhibitors. |
AID1801045 | HDAC 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.\\ | 2015 | Bioorganic chemistry, Apr, Volume: 59 | An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors. |
AID1802060 | APN Inhibition Assay from Article 10.1111/cbdd.12778: \\Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents.\\ | 2016 | Chemical biology & drug design, 10, Volume: 88, Issue:4 | Design, synthesis, and biological characterization of tamibarotene analogs as anticancer agents. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1346082 | Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1346066 | Human histone deacetylase 5 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1346068 | Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Bioorganic & 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. |
AID1346080 | Human histone deacetylase 11 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Bioorganic & 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. |
AID1346032 | Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1346090 | Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Bioorganic & 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. |
AID1346068 | Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1346077 | Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1346048 | Human histone deacetylase 10 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Bioorganic & 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. |
AID1346134 | Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS 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. |
AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 2020 | ACS 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. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS 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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2013 | The 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 6 (0.24) | 18.2507 |
2000's | 480 (19.24) | 29.6817 |
2010's | 1591 (63.77) | 24.3611 |
2020's | 418 (16.75) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (53.95) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 181 (7.16%) | 5.53% |
Reviews | 139 (5.50%) | 6.00% |
Case Studies | 38 (1.50%) | 4.05% |
Observational | 1 (0.04%) | 0.25% |
Other | 2,170 (85.80%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
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 1 | 27 participants (Actual) | Interventional | 2010-01-19 | Completed | ||
Phase I Study of the Combination of Vorinostat and Radiation Therapy for the Treatment of Patients With Brain Metastases [NCT00838929] | Phase 1 | 17 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
A Feasibility Study of Vorinostat (SAHA) Combined With Isotretinoin and Chemotherapy in Infants With Embryonal Tumors of the Central Nervous System [NCT00867178] | Phase 1 | 33 participants (Actual) | Interventional | 2009-02-25 | Completed | ||
Phase I Study of Vorinostat in Combination With 13-Cis-retinoic Acid in Patients With Refractory/Recurrent Neuroblastoma [NCT01208454] | Phase 1 | 29 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
Phase I Study on Suberoylanilide Hydroxyamic Acid (Vorinostat) a Histone Deacetylase Inhibitor, in Palliative Radiotherapy for Advanced Tumors. [NCT00455351] | Phase 1 | 15 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
A Phase I Study of Vorinostat and Bortezomib in Children With Refractory of Recurrent Solid Tumors, Including CNS Tumors and Lymphomas [NCT01132911] | Phase 1 | 5 participants (Anticipated) | Interventional | 2010-05-10 | Completed | ||
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 1 | 143 participants (Actual) | Interventional | 2011-04-28 | Completed | ||
A Phase I/II Trial of Vorinostat and Pegylated Liposomal Doxorubicin in Relapsed or Refractory Lymphomas [NCT00785798] | Phase 1/Phase 2 | 17 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to sponsor requested) | ||
The Effect of Vorinostat on ACTH Producing Pituitary Adenomas in Cushing's Disease [NCT04339751] | Phase 2 | 22 participants (Anticipated) | Interventional | 2024-01-03 | Recruiting | ||
Phase I Trial of Ixabepilone and Vorinostat in Metastatic Breast Cancer [NCT01084057] | Phase 1 | 56 participants (Actual) | Interventional | 2010-05-17 | Completed | ||
Vorinostat With Gemcitabine/Clofarabine/Busulfan for Allogeneic Transplantation for Aggressive Lymphomas [NCT04220008] | Phase 2 | 30 participants (Anticipated) | Interventional | 2023-06-01 | Not yet recruiting | ||
A Pilot Study of Peroral Vorinostat (SAHA) in Patients With Refractory Histone Deacetylase-positive Uterine Sarcoma [NCT03509207] | Phase 2 | 3 participants (Actual) | Interventional | 2017-12-14 | Terminated(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 2 | 25 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
Pilot Study of the Effect of Vorinostat on Nervous System Hemangioblastomas In Von Hippel-Lindau Disease [NCT02108002] | Phase 1 | 7 participants (Actual) | Interventional | 2014-04-05 | Completed | ||
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 2 | 282 participants (Actual) | Interventional | 2012-03-01 | Active, not recruiting | ||
A Phase I Clinical Study of L-001079038 in Patients With Solid Tumors [NCT00127127] | Phase 1 | 18 participants (Actual) | Interventional | 2005-06-10 | Completed | ||
A Phase I Study of Pazopanib and Vorinostat in Patients With Advanced Malignancies [NCT01339871] | Phase 1 | 152 participants (Actual) | Interventional | 2011-04-20 | Completed | ||
A Pilot Study to Assess the Safety and Effect on HIV Transcription of Vorinostat in Patients Receiving Suppressive Combination Anti-retroviral Therapy [NCT01365065] | Phase 2 | 20 participants (Actual) | Interventional | 2011-05-31 | Active, not recruiting | ||
High-Dose Vorinostat With Radiation Therapy in the Treatment of Recurrent Glioma [NCT01378481] | Phase 1 | 30 participants (Actual) | Interventional | 2012-06-30 | Terminated | ||
A Phase 2 Clinical Trial Testing the Safety and Efficacy of Voronistat in Pediatric Patients With Drug Resistant Epilepsy [NCT03894826] | Phase 2 | 12 participants (Anticipated) | Interventional | 2018-12-10 | Recruiting | ||
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 2 | 37 participants (Actual) | Interventional | 2019-04-02 | Terminated(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 3 | 661 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
Phase I Clinical Trial of Vorinostat (MK-0683) in Combination With Bortezomib in Patients With Advanced Multiple Myeloma [NCT00111813] | Phase 1 | 34 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
TINI 2: Total Therapy for Infants With Acute Lymphoblastic Leukemia II [NCT05848687] | Phase 1/Phase 2 | 90 participants (Anticipated) | Interventional | 2023-11-01 | Not 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 2 | 8 participants (Actual) | Interventional | 2008-09-30 | Terminated(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 1 | 28 participants (Anticipated) | Interventional | 2019-06-11 | Recruiting | ||
Carfilzomib/SAHA Combined With High-Dose Gemcitabine/Busulfan/Melphalan With Autologous Stem Cell Transplant for Patients With Refractory/Relapsed Myeloma [NCT02114502] | Phase 2 | 0 participants (Actual) | Interventional | 2014-09-30 | Withdrawn | ||
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 2 | 500 participants (Anticipated) | Interventional | 2015-09-30 | Recruiting | ||
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 1 | 18 participants (Actual) | Interventional | 2009-12-16 | Completed | ||
Phase I Clinical Trial of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Pemetrexed and Cisplatin in Patients With Advanced Cancer [NCT00106626] | Phase 1 | 52 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, 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 1 | 30 participants (Anticipated) | Interventional | 2010-05-31 | Terminated(stopped due to Sponsor withdrew support for the study) | ||
Phase I Study of Decitabine, Vorinostat, and Cytarabine in Acute Myeloid Leukemia [NCT01130506] | Phase 1 | 17 participants (Actual) | Interventional | 2010-05-17 | Completed | ||
A Phase I Study of Carboplatin + Paclitaxel and MK0683 in Patients With Chemotherapy-naive Non-Small Cell Lung Cancer (NSCLC) [NCT00424775] | Phase 1 | 3 participants (Actual) | Interventional | 2007-01-31 | Terminated | ||
A Phase I Clinical Trial of Vorinostat in Combination With Gemcitabine Plus Platinum in Patients With Advanced Non-Small Cell Lung Cancer [NCT00423449] | Phase 1 | 61 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
MT2022-06: Phase I Study of FT538 Monotherapy and in Combination With Vorinostat for the Treatment of Persistent Low-Level HIV Viremia [NCT05700630] | Phase 1 | 34 participants (Anticipated) | Interventional | 2024-07-15 | Not yet recruiting | ||
Research In Viral Eradication of HIV Reservoirs [NCT02336074] | Phase 2 | 60 participants (Actual) | Interventional | 2015-11-27 | Completed | ||
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 2 | 83 participants (Actual) | Interventional | 2010-11-15 | Active, not recruiting | ||
Fludarabine/Clofarabine/Busulfan Combined With SAHA in Patients Receiving Allogeneic Hematopoietic Stem Cell Transplantation for Acute Leukemia [NCT02083250] | Phase 1 | 70 participants (Actual) | Interventional | 2014-03-06 | Completed | ||
A Phase I/II Study of First Line Vorinostat With Pemetrexed-cisplatin, in Patients With Malignant Pleural Mesothelioma [NCT01353482] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | Withdrawn(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 3 | 101 participants (Actual) | Interventional | 2010-11-15 | Active, 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 2 | 107 participants (Actual) | Interventional | 2010-10-06 | Completed | ||
Modulation of Autophagy: A Clinical Study of Vorinostat Plus Hydroxychloroquine Versus Regorafenib in Refractory Metastatic Colorectal Cancer (mCRC) Patients (CTMS# 14-2015) [NCT02316340] | Phase 2 | 44 participants (Actual) | Interventional | 2015-02-11 | Completed | ||
Cisplatin and Sodium Thiosulfate Otoprotection With or Without SAHA/Vorinostat Histone Deacetylase Inhibition for Relapsed/Refractory Hepatoblastoma and Other Embryonal Tumors [NCT05756660] | Early Phase 1 | 33 participants (Anticipated) | Interventional | 2023-03-01 | Recruiting | ||
Phase I/II Adaptive Randomized Trial of Bevacizumab Versus Bevacizumab Plus Vorinostat in Adults With Recurrent Glioblastoma [NCT01266031] | Phase 1/Phase 2 | 96 participants (Actual) | Interventional | 2011-07-12 | Completed | ||
A Phase 1 Study of Lenalidomide in Combination With Vorinostat in Pediatric Patients With High Grade or Progressive Central Nervous System Tumors [NCT03050450] | Phase 1 | 8 participants (Actual) | Interventional | 2016-08-10 | Terminated(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 1 | 34 participants (Actual) | Interventional | 2012-04-16 | Completed | ||
A Phase I Study of 131I-MIBG With Dinutuximab +/- Vorinostat for Relapsed/Refractory Neuroblastoma [NCT03332667] | Phase 1 | 45 participants (Actual) | Interventional | 2018-09-12 | Active, 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 2 | 27 participants (Actual) | Interventional | 2011-02-09 | Completed | ||
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 1 | 24 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
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 2 | 58 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
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 1 | 17 participants (Actual) | Interventional | 2017-06-27 | Completed | ||
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 2 | 52 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
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 1 | 33 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
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 2 | 5 participants (Actual) | Interventional | 2008-03-31 | Terminated | ||
A Phase I Clinical Trial of Vorinostat in Combination With Vinorelbine in Patients With Advanced Cancer. [NCT00801151] | Phase 1 | 30 participants (Anticipated) | Interventional | 2009-01-31 | Terminated | ||
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 2 | 14 participants (Actual) | Interventional | 2006-03-31 | Terminated | ||
Phase II Study of Idarubicin, Cytarabine, and Vorinostat in Patients With High-Risk MDS and AML [NCT00656617] | Phase 2 | 106 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
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 1 | 5 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
HDAC Inhibitor Vorinostat in Resistant BRAF V600 Mutated Advanced Melanoma [NCT02836548] | Phase 1/Phase 2 | 22 participants (Anticipated) | Interventional | 2016-06-30 | Recruiting | ||
Phase II Trial of Velcade Plus Vorinostat in the Treatment of High Risk MDS and Relapsed/Refractory AML [NCT00818649] | Phase 2 | 16 participants (Actual) | Interventional | 2009-01-31 | Terminated(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 2 | 35 participants (Anticipated) | Interventional | 2017-10-30 | Recruiting | ||
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 1 | 15 participants (Actual) | Interventional | 2019-02-12 | Completed | ||
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 2 | 15 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
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 1 | 37 participants (Actual) | Interventional | 2017-07-11 | Completed | ||
Phase I of Vorinostat-Iressa Combined Therapy on Resistance by BIM Polymorphysim in EGFR Mutant Lung Cancer [NCT02151721] | Phase 1 | 12 participants (Actual) | Interventional | 2014-06-01 | Active, 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 2 | 50 participants (Actual) | Interventional | 2015-10-08 | Completed | ||
Phase I Trial of Chemoradiation With Capecitabine and Vorinostat in Pancreatic Cancer. [NCT00983268] | Phase 1 | 21 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
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 1 | 30 participants (Actual) | Interventional | 2010-01-15 | Completed | ||
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 2 | 20 participants (Anticipated) | Interventional | 2009-09-30 | Terminated(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 1 | 20 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
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 1 | 23 participants (Actual) | Interventional | 2005-09-30 | Terminated(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 2 | 124 participants (Actual) | Interventional | 2016-03-22 | Active, not recruiting | ||
A Randomized Phase IIa Study of Vorinostat in Patients With Low or Intermediate-1 Risk Myelodysplastic Syndrome [NCT00486720] | Phase 2 | 22 participants (Actual) | Interventional | 2007-06-30 | Terminated | ||
A Phase I Trial of Vorinostat Concurrent With Stereotactic Radiotherapy in Treatment of Brain Metastases From Non-Small Cell Lung Cancer [NCT00946673] | Phase 1 | 17 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Pilot Study Evaluating Surrogates of Response to Short Term Oral Suberoylanilide Hydroxamic Acid (SAHA) in Women With Newly Diagnosed Breast Cancer [NCT00262834] | Phase 2 | 54 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
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 2 | 68 participants (Actual) | Interventional | 2008-05-31 | Active, not recruiting | ||
Phase I Clinical and Pharmacological Study of Suberoylanilide Hydroxamic Acid- SAHA (MSK390) in Patients With Advanced Solid Tumors [NCT00005634] | Phase 1 | 0 participants | Interventional | 2000-01-31 | Completed | ||
An International, Multicenter, Open-Label Study of Vorinostat (MK0683) in Combination With Bortezomib in Patients With Relapsed or Refractory Multiple Myeloma [NCT00773838] | Phase 2 | 143 participants (Actual) | Interventional | 2008-12-01 | Completed | ||
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 1 | 9 participants (Actual) | Interventional | 2009-02-13 | Completed | ||
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 2 | 57 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Phase I Study of Vorinostat in Combination With Niacinamide, and Etoposide for the Treatment of Patients With Relapsed and Refractory Lymphoid Malignancies [NCT00691210] | Phase 1 | 40 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
A Phase I Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of MK0683 in Patients With Advanced Cancer [NCT00750178] | Phase 1 | 30 participants (Actual) | Interventional | 2004-11-01 | Completed | ||
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 2 | 19 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
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 2 | 70 participants (Anticipated) | Interventional | 2007-06-30 | Recruiting | ||
A Phase II Study to Investigate the Efficacy and Tolerability of Vorinostat in Patients Suffering From Advanced, Metastatic Soft Tissue Sarcoma [NCT00918489] | Phase 2 | 40 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
A Phase II Study of Vorinostat (Suberoylanilide Hydroxamic Acid) Plus Rituximab in Indolent Non-Hodgkin's Lymphoma [NCT00720876] | Phase 2 | 30 participants (Actual) | Interventional | 2008-07-23 | Completed | ||
Phase I Study of Carboplatin, Paclitaxel, Bevacizumab and Vorinostat for Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00702572] | Phase 1 | 25 participants (Actual) | Interventional | 2008-04-30 | Terminated(stopped due to Low Enrollment) | ||
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Flavopiridol in Advanced Solid Tumors [NCT00324480] | Phase 1 | 60 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
A Phase I/II of Vorinostat Plus CHOP in Untreated T-cell Non-Hodgkin's Lymphoma [NCT00787527] | Phase 1/Phase 2 | 14 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
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 2 | 61 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
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 2 | 79 participants (Actual) | Interventional | 2010-08-09 | Completed | ||
An International, Multicenter, Randomized, Double-Blind Study of Vorinostat (MK-0683) or Placebo in Combination With Bortezomib in Patients With Multiple Myeloma [NCT00773747] | Phase 3 | 637 participants (Actual) | Interventional | 2008-12-01 | Completed | ||
A Phase I Trial of Vorinostat in Combination With Bevacizumab and Irinotecan in Recurrent Glioblastoma [NCT00762255] | Phase 1 | 19 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
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 2 | 5 participants (Actual) | Interventional | 2009-10-31 | Terminated(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 1 | 16 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
Phase I Study of Induction Therapy With VELCADE and Vorinostat in Patients With Surgically Resectable Non-Small Cell Lung Cancer [NCT00731952] | Phase 1 | 21 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
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 2 | 27 participants (Anticipated) | Interventional | Not 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 1 | 6 participants (Actual) | Interventional | 2016-03-31 | Terminated(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 2 | 12 participants (Actual) | Interventional | 2010-03-31 | Terminated(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 1 | 32 participants (Actual) | Interventional | 2008-10-31 | Terminated(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 2 | 3 participants (Actual) | Interventional | 2009-05-31 | Terminated(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 3 | 0 participants (Actual) | Interventional | Withdrawn(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 2 | 34 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
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 1 | 15 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
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 2 | 54 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
A Phase II Study of MK-0683 in Patients With Polycythaemia Vera and Essential Thrombocythaemia. [NCT00866762] | Phase 2 | 60 participants (Anticipated) | Interventional | 2009-02-28 | Active, 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 2 | 94 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
A Window Trial of Vorinostat in Patients With Ductal Carcinoma in Situ (DCIS) of the Breast [NCT00788112] | Phase 1 | 17 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Bortezomib and Vorinostat as Maintenance Therapy After Autologous Stem Cell Transplant for Multiple Myeloma [NCT00839956] | Phase 2 | 31 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
A Phase 2 Study of Suberoylanilide Hydroxamic Acid (SAHA) in Acute Myeloid Leukemia (AML) [NCT00305773] | Phase 2 | 37 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
Phase II Study of Vorinostat (SAHA) in Combination With Bortezomib (PS-341) in Patients With Recurrent Glioblastoma Multiforme [NCT00641706] | Phase 2 | 44 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
A Phase I Study of Vorinostat in Combination With Lenalidomide and Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma [NCT00642954] | Phase 1 | 31 participants (Actual) | Interventional | 2008-02-13 | Completed | ||
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) | Interventional | 2012-10-31 | Withdrawn(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 2 | 0 participants (Actual) | Interventional | 2010-06-30 | Withdrawn(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 2 | 103 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
A Phase II, Pharmacokinetic and Biologic Correlative Study of Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Advanced Renal Cell Carcinoma (RCC) [NCT00278395] | Phase 2 | 14 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
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 1 | 23 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
A Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Indolent Non-Hodgkin's Lymphoma [NCT00253630] | Phase 2 | 37 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
MK0683 Phase1 Clinical Study - Solid Tumor - [NCT00373490] | Phase 1 | 16 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
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 2 | 23 participants (Actual) | Interventional | 2006-01-31 | Terminated(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 1 | 27 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
A Phase II Trial of Suberoylanilide Hydroxamic Acid (NSC-701852) for Recurrent or Primary Refractory Hodgkin's Lymphoma [NCT00132028] | Phase 2 | 27 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
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 2 | 45 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
A Phase I Study of Sorafenib and Vorinostat in Advanced Hepatocellular Carcinoma [NCT01075113] | Phase 1 | 16 participants (Actual) | Interventional | 2010-08-10 | Completed | ||
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 1 | 60 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
A Phase I Trial of Sirolimus or Everolimus or Temsirolimus (mTOR Inhibitor) and Vorinostat (Histone Deacetylase Inhibitor) in Patients With Advanced Cancer [NCT01087554] | Phase 1 | 249 participants (Anticipated) | Interventional | 2010-03-31 | Active, not recruiting | ||
A Phase II Study of Suberoylanilide Hydroxamic Acid and Bortezomib in Advanced Soft Tissue Sarcomas [NCT00937495] | Phase 2 | 16 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
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 1 | 12 participants (Actual) | Interventional | 2007-04-30 | Terminated(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 3 | 253 participants (Actual) | Interventional | 2007-05-31 | Terminated(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 1 | 71 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
A Phase 1 Study of Pembrolizumab Plus Vorinostat for Relapsed or Refractory Diffuse Large B-Cell Lymphoma, Follicular Lymphoma, and Hodgkin Lymphoma [NCT03150329] | Phase 1 | 52 participants (Actual) | Interventional | 2017-07-18 | Active, 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 2 | 4 participants (Actual) | Interventional | 2012-08-31 | Terminated(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 2 | 15 participants (Anticipated) | Interventional | 2024-04-01 | Not yet recruiting | ||
Vorinostat (SAHA) and Lenalidomide After Autologous Transplant for Patients With Multiple Myeloma [NCT00729118] | Phase 1 | 19 participants (Actual) | Interventional | 2008-09-26 | Completed | ||
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 2 | 2 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to insufficient enrollment) | ||
NPI-0052 and Vorinostat in Patients With Non-small Cell Lung Cancer, Pancreatic Cancer, Melanoma or Lymphoma [NCT00667082] | Phase 1 | 22 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
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 1 | 36 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
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 2 | 15 participants (Actual) | Interventional | 2009-06-30 | Terminated(stopped due to Terminated due to unacceptable toxicity) | ||
A Continuation Clinical Trial of Oral Vorinostat (MK-0683) in Advanced Cancers [NCT00907738] | Phase 2 | 27 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Bortezomib* and Vorinostat as Maintenance Therapy After Autologous Transplant for Non-Hodgkin Lymphoma Using R-BEAM or BEAM Conditioning Transplant Regimen [NCT00992446] | Phase 2 | 27 participants (Actual) | Interventional | 2010-09-02 | Completed | ||
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 2 | 11 participants (Actual) | Interventional | 2009-07-31 | Terminated(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 2 | 10 participants (Actual) | Interventional | 2009-08-31 | Terminated(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 2 | 110 participants (Actual) | Interventional | 2009-09-08 | Completed | ||
Phase I Trial of Vorinostat (NSC-701852, Suberoylanilide Hydroxamic Acid) and Doxorubicin (NSC-123127, Adriamycin) [NCT00331955] | Phase 1 | 40 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
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 1 | 78 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
Phase I/II Intra-patient Dose Escalation Study of Vorinostat in Children With Relapsed Solid Tumor, Lymphoma or Leukemia [NCT01422499] | Phase 1/Phase 2 | 50 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
A Pilot Study of Oral Vorinostat Plus Oral Eltrombopag Support in Patients With Lymphoma (VEIL) [NCT01500538] | Phase 2 | 1 participants (Actual) | Interventional | 2012-10-31 | Terminated(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 2 | 18 participants (Actual) | Interventional | 2009-03-31 | Terminated(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 2 | 56 participants (Actual) | Interventional | 2009-04-15 | Completed | ||
Phase I/II Study of Vorinostat (Suberoylanilide Hydroxamic Acid [SAHA]), Temozolomide, and Radiation Therapy in Patients With Newly Diagnosed Glioblastoma [NCT00731731] | Phase 1/Phase 2 | 125 participants (Actual) | Interventional | 2009-07-10 | Completed | ||
Phase I Clinical Study of MK-0683 in Patients With Relapsed or Refractory Cutaneous T-Cell Lymphoma (CTCL) [NCT00771472] | Phase 1 | 10 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Phase IIb Multicenter Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Advanced Cutaneous T-cell Lymphoma [NCT00091559] | Phase 2 | 74 participants (Actual) | Interventional | 2005-02-03 | Completed | ||
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 2 | 40 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Phase II Trial of Combination Treatment With Vorinostat, Bortezomib and Dexamethasone in Patients With Relapsed and Relapsed Refractory Multiple Myeloma [NCT01720875] | Phase 2 | 16 participants (Actual) | Interventional | 2013-08-09 | Completed | ||
Selective Estrogen Receptor Modulators to Enhance the Efficacy of Viral Reactivation With Histone Deacetylase Inhibitors [NCT03382834] | Phase 2 | 31 participants (Actual) | Interventional | 2018-04-26 | Active, 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 2 | 0 participants (Actual) | Interventional | 2012-04-30 | Withdrawn(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 2 | 25 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
A Pilot Study of Vorinostat to Restore Sensitivity to Aromatase Inhibitor Therapy [NCT01153672] | 8 participants (Actual) | Interventional | 2010-11-30 | Completed | |||
A Phase 1 Study of Paclitaxel and Carboplatin in Solid Tumors (With Focus on Upper Aerodigestive Cancers) in Persons With HIV Infection [NCT01249443] | Phase 1 | 17 participants (Actual) | Interventional | 2013-11-30 | Terminated(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 2 | 30 participants (Actual) | Interventional | 2010-08-06 | Completed | ||
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 2 | 28 participants (Actual) | Interventional | 2010-12-31 | Terminated(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 2 | 135 participants (Anticipated) | Interventional | 2007-11-28 | Active, not recruiting | ||
Temozolomide Plus Vorinostat in Patients With Relapse/Refractory Acute Myeloid Leukemia (AML) [NCT01550224] | Phase 2 | 23 participants (Actual) | Interventional | 2013-05-01 | Completed | ||
Proof of Concept Study of Vorinostat, A Histone Deacetylase Inhibitor, in Patients With Class 2 High Risk Uveal Melanoma [NCT03022565] | Early Phase 1 | 0 participants (Actual) | Interventional | 2020-01-31 | Withdrawn(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 1 | 50 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
A Phase II Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Relapsed Diffuse Large B-Cell Lymphoma (DLBCL) [NCT00097929] | Phase 2 | 18 participants (Actual) | Interventional | 2005-05-01 | Completed | ||
A Phase 1 Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Gemcitabine in Patients With Epithelial Tumors [NCT00243100] | Phase 1 | 21 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
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 1 | 80 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
A Phase I Study of SAHA in Combination With Bortezomib in Relapsed and Refractory Multiple Myeloma [NCT00310024] | Phase 1 | 40 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
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 Access | No longer available | ||||
A Phase 1 Study of Suberoylanilide Hydroxamic Acid (Vorinostat, SAHA) in Combination With Idarubicin in Relapsed or Refractory Leukemia [NCT00331513] | Phase 1 | 40 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
Phase II Evaluation of Suberoylanilide Hydroxamic Acid (NSC 701852) in Patients With Advanced Prostate Cancer That Has Progressed on One Prior Chemotherapy [NCT00330161] | Phase 2 | 29 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
A Phase I Trial of Pembrolizumab and Vorinostat Combined With Temozolomide and Radiation Therapy for Newly Diagnosed Glioblastoma [NCT03426891] | Phase 1 | 21 participants (Actual) | Interventional | 2018-03-16 | Completed | ||
A Phase I Clinical Study of MK0683 in Patients With Malignant Lymphoma [NCT00127140] | Phase 1 | 10 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
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 1 | 54 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Phase II Clinical Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Advanced Multiple Myeloma [NCT00109109] | Phase 1 | 60 participants | Interventional | 2003-12-01 | Terminated | ||
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Capecitabine in Patients With Solid Tumors [NCT00121277] | Phase 1 | 28 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
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 2 | 50 participants (Actual) | Interventional | 2007-12-31 | Terminated | ||
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 2 | 18 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
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 2 | 1 participants (Actual) | Interventional | 2009-01-31 | Terminated(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 2 | 21 participants (Actual) | Interventional | 2011-06-30 | Terminated(stopped due to Unanticipated Toxicities) | ||
A Therapeutic Trial of Bortezomib (Velcade), Vorinostat (SAHA) and Dexamethasone for Relapsed/Refractory Acute Lymphoblastic Leukemia (ALL) [NCT01312818] | Phase 2 | 2 participants (Actual) | Interventional | 2011-06-30 | Terminated(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 2 | 23 participants (Actual) | Interventional | 2010-11-30 | Terminated(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 1 | 15 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
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 2 | 162 participants (Anticipated) | Interventional | 2017-01-31 | Not yet recruiting | ||
A Phase II Study of Bortezomib and Vorinostat in Patients With Refractory or Relapsed MLL Rearranged Hematologic Malignancies [NCT02419755] | Phase 2 | 12 participants (Actual) | Interventional | 2015-04-14 | Terminated(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 2 | 2 participants (Actual) | Interventional | 2011-03-31 | Terminated(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 3 | 4,420 participants (Actual) | Interventional | 2010-05-31 | Active, 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 2 | 60 participants (Anticipated) | Interventional | 2019-10-21 | Recruiting | ||
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 2 | 16 participants (Actual) | Interventional | 2004-12-01 | Terminated | ||
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 2 | 60 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Phase I Clinical Trial of Oral Suberoylanilide Hydroxamic Acid - SAHA (MSK390) in Patients With Advanced Solid Tumors and Hematologic Malignancies [NCT00045006] | Phase 1 | 0 participants | Interventional | 2001-07-31 | Completed | ||
Phase II Study of Oral Suberoylanilide Hydroxamic Acid (SAHA) in Recurrent or Metastatic Transitional Cell Carcinoma of the Urothelium [NCT00363883] | Phase 2 | 14 participants (Actual) | Interventional | 2006-06-30 | Terminated(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 2 | 43 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
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 2 | 31 participants (Actual) | Interventional | 2008-03-31 | Terminated | ||
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 2 | 30 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
Phase 1/2 Study of Vorinostat Therapy in Niemann-Pick Disease, Type C1 [NCT02124083] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2014-04-25 | Completed | ||
Phase I Trial of Carfilzomib (PR-171) in Combination With Vorinostat (SAHA) in Patients With Relapsed/Refractory B-Cell Lymphomas [NCT01276717] | Phase 1 | 20 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
A Dose Escalation Study of Vorinostat in Combination With Palliative Radiotherapy for Patients With Non-Small Cell Lung Cancer [NCT00821951] | Phase 1 | 17 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
Epigenetic Priming for Immune Therapy in ER-Positive Breast Cancer in Biomarker Select Population [NCT04190056] | Phase 2 | 1 participants (Actual) | Interventional | 2021-03-11 | Terminated(stopped due to Change in practice patterns) | ||
Olaparib Combined With High-Dose Chemotherapy for Refractory Lymphomas [NCT03259503] | Phase 1 | 50 participants (Actual) | Interventional | 2019-09-13 | Active, not recruiting | ||
Total Therapy for Infants With Acute Lymphoblastic Leukemia (ALL) I [NCT02553460] | Phase 1/Phase 2 | 50 participants (Actual) | Interventional | 2016-01-29 | Active, not recruiting | ||
A Phase I Study of Suberoylanilide Hydroxamic Acid (SAHA) in Combination With Bortezomib in Patients With Advanced Malignancies [NCT00227513] | Phase 1 | 66 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Phase I/II Clinical Trial of Vorinostat in Patients With Recurrent and/or Metastatic Breast Cancer [NCT00416130] | Phase 1/Phase 2 | 49 participants (Anticipated) | Interventional | 2007-01-31 | Active, 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 1 | 30 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Pilot Study of Curcumin, Vorinostat, and Sorafenib in Patients With Advanced Solid Tumors [NCT01608139] | Phase 1 | 0 participants (Actual) | Interventional | 2012-11-30 | Withdrawn | ||
Histone Deacetylase (HDAC) Inhibition Using Vorinostat (SAHA) After Autologous Hematopoietic Stem Cell Transplantation for High Risk Lymphoma [NCT00561418] | Phase 1 | 23 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
A Clinical Trial to Validate Molecular Targets of Vorinostat in Patients With Aerodigestive Tract Cancer [NCT00735826] | 10 participants (Actual) | Interventional | 2009-03-31 | Completed | |||
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 1 | 24 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
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 1 | 10 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
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 2 | 0 participants (Actual) | Interventional | 2012-01-31 | Withdrawn | ||
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 2 | 52 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
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 1 | 40 participants (Anticipated) | Interventional | 2023-03-31 | Recruiting | ||
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 2 | 21 participants (Actual) | Interventional | 2013-03-31 | Terminated(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 1 | 25 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
A Pilot Study of Vorinostat to Restore Sensitivity to Aromatase Inhibitor Therapy Part B [NCT01720602] | 15 participants (Actual) | Interventional | 2012-11-30 | Completed | |||
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 2 | 37 participants (Actual) | Interventional | 2012-02-10 | Completed | ||
Vorinostat With 131-I MIBG Therapy for Resistant/Relapsed Neuroblastoma: A Phase I Study IND# 105,744 [NCT01019850] | Phase 1 | 27 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
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 2 | 18 participants (Actual) | Interventional | 2009-10-31 | Terminated(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 3 | 372 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
Phase 1b/2 Study of Vorinostat in Combination With Gemcitabine and Docetaxel in Advanced Sarcoma [NCT01879085] | Phase 1/Phase 2 | 37 participants (Actual) | Interventional | 2013-09-24 | Completed | ||
A Phase II Study of Vorinostat in Patients With Advanced Melanoma [NCT00121225] | Phase 2 | 32 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
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 2 | 16 participants (Actual) | Interventional | 2006-08-31 | Completed | ||
A Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) in Patients With Relapsed Non-small Cell Lung Cancer [NCT00138203] | Phase 2 | 16 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
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 1 | 15 participants (Anticipated) | Interventional | 2019-05-01 | Recruiting | ||
A Phase I Study of the mTOR Inhibitor Temsirolimus in Combination With the HDAC Inhibitor Vorinostat in Patients With Metastatic Prostate Cancer [NCT01174199] | Phase 1 | 13 participants (Actual) | Interventional | 2012-02-29 | Terminated(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 2 | 48 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
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 2 | 15 participants (Actual) | Interventional | 2009-04-30 | Terminated(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 2 | 20 participants (Actual) | Interventional | 2012-06-30 | Terminated(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 2 | 260 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
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 2 | 37 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
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 1 | 25 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
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 2 | 25 participants (Actual) | Interventional | 2010-12-31 | Terminated(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 2 | 8 participants (Actual) | Interventional | 2016-06-22 | Terminated(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 2 | 38 participants (Actual) | Interventional | 2015-05-04 | Terminated(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 2 | 61 participants (Actual) | Interventional | 2013-11-07 | Completed | ||
A Pilot Trial of Vorinostat Plus Tacrolimus and Methotrexate to Prevent Graft Versus Host Disease Following Unrelated Donor Hematopoietic Stem Cell Transplantation [NCT01789255] | Phase 2 | 12 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
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 1 | 18 participants (Anticipated) | Interventional | 2015-10-05 | Active, not recruiting | ||
A Phase I Study of MLN9708 and Vorinostat to Target Autophagy in Patients With Advanced p53 Mutant Malignancies [NCT02042989] | Phase 1 | 68 participants (Actual) | Interventional | 2014-06-27 | Completed | ||
Phase II Study of Histone Deacetylase Inhibitor SAHA (Vorinostat) in Patients With Metastatic Thyroid Carcinoma [NCT00134043] | Phase 2 | 19 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
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 1 | 30 participants (Anticipated) | Interventional | 2017-03-17 | Recruiting | ||
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 1 | 3 participants (Actual) | Interventional | 2015-02-21 | Terminated(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 2 | 64 participants (Anticipated) | Interventional | 2023-12-01 | Not 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 2 | 55 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
Phase II Study of Suberoylanilide Hydroxamic Acid (SAHA) (NSC 701852) as Salvage Therapy in Metastatic Breast Cancer [NCT00132002] | Phase 2 | 14 participants (Actual) | Interventional | 2005-06-30 | Terminated(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 3 | 790 participants (Actual) | Interventional | 2017-03-29 | Active, not recruiting | ||
Vorinostat and Carboplatin or Vorinostat and Paclitaxel in Patients With Advanced Solid Tumors: A Pharmacokinetic and Pharmacodynamic Study [NCT01281176] | Phase 1 | 20 participants (Actual) | Interventional | 2011-02-09 | Active, not recruiting | ||
Phase II Study of Bevacizumab and Vorinostat for Recurrent WHO Grade IV Malignant Glioma Patients [NCT01738646] | Phase 2 | 48 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
Phase I/II Study of 5-azacitidine in Combination With Vorinostat in Patients With Relapsed or Refractory DLBCL [NCT01120834] | Phase 1/Phase 2 | 17 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
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 2 | 49 participants (Anticipated) | Interventional | 2020-02-04 | Recruiting | ||
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 2 | 2 participants (Actual) | Interventional | 2017-08-08 | Terminated(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 1 | 44 participants (Anticipated) | Interventional | 2017-09-28 | Recruiting | ||
A Phase I/II Study of Carfilzomib, Lenalidomide, Vorinostat, and Dexamethasone in Relapsed and/or Refractory Multiple Myeloma [NCT01297764] | Phase 1/Phase 2 | 17 participants (Actual) | Interventional | 2011-04-30 | Active, 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 2 | 112 participants (Actual) | Interventional | 2020-10-28 | Active, 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 2 | 29 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
Phase II Trial of Bortezomib and Vorinostat in Mantle Cell and Diffuse Large B-Cell Lymphomas [NCT00703664] | Phase 2 | 65 participants (Actual) | Interventional | 2008-07-09 | Completed | ||
Using Proton Magnetic Resonance Spectroscopy (MRS) to Predict Response of Vorinostat Treatment in Glioblastoma [NCT01342757] | 12 participants (Actual) | Interventional | 2010-12-31 | Completed | |||
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 3 | 754 participants (Actual) | Interventional | 2013-02-12 | Completed | ||
Decitabine and Vorinostat With CD3/CD19 Depleted Haploidentical Donor Natural Killer (NK) Cells for the Treatment of High Risk Myelodysplastic Syndromes (MDS) [NCT01593670] | Phase 2 | 9 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
A Phase 1 Study of Neoadjuvant Chemotherapy, Followed by Concurrent Chemoradiation With Gemcitabine, Sorafenib, and Vorinostat in Pancreatic Cancer [NCT02349867] | Phase 1 | 23 participants (Actual) | Interventional | 2015-01-29 | Completed | ||
Compassionate Use of Vorinostat (MK0683) for the Treatment of Patients With Advanced Cutaneous T-Cell Lymphoma [NCT00419367] | 0 participants | Expanded Access | No longer available | ||||
Pilot Trial of Vorinostat Plus Tacrolimus & Methotrexate to Prevent Graft Versus Host Disease Following Unrelated Donor Allogeneic Transplant [NCT01790568] | Phase 2 | 26 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
A Phase 2 Study of Vorinostat (NSC 701852) in Metastatic Uveal Melanoma [NCT01587352] | Phase 2 | 40 participants (Anticipated) | Interventional | 2012-04-20 | Active, 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 1 | 53 participants (Actual) | Interventional | 2016-02-23 | Completed | ||
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 2 | 114 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
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 1 | 72 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
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 2 | 135 participants (Anticipated) | Interventional | 2006-11-22 | Active, 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 1 | 18 participants (Actual) | Interventional | 2006-03-03 | Active, not recruiting | ||
A Phase I Study of Vorinostat (Suberoylanilide Hydroxamic Acid [SAHA]) in Combination With Temozolomide in Patients With Malignant Gliomas [NCT00268385] | Phase 1 | 83 participants (Actual) | Interventional | 2005-12-16 | Active, not recruiting | ||
A Pilot Study of Decitabine and Vorinostat With Chemotherapy for Relapsed ALL [NCT01483690] | Phase 1/Phase 2 | 23 participants (Actual) | Interventional | 2011-12-31 | Terminated(stopped due to Toxicity) | ||
HDAC Inhibitor Augmentation to Clozapine [NCT03263533] | Early Phase 1 | 0 participants (Actual) | Interventional | 2017-04-30 | Withdrawn(stopped due to PIs were unable to recruit any participants) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |