Assay ID | Title | Year | Journal | Article |
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. |
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. |
AID1797850 | HDAC Enzyme Activity Assay from Article 10.1021/jm701079h: \\Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.\\ | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1346090 | Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2
| Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
AID1346077 | Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2
| Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
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. |
AID1346134 | Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2
| Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
AID1346082 | Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2
| Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
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. |
AID385685 | Inhibition of flag-tagged HDAC4 by pull-down assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
| Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases. |
AID1548274 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay | | | |
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. |
AID1853065 | Inhibition of HDAC1-CoREST-LSD1 (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
| A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras. |
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. |
AID664385 | Inhibition of SIRT1 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
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. |
AID1467233 | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 5 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated 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. |
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. |
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. |
AID1732162 | Cytotoxicity against human HCT-116 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. |
AID392619 | Cytotoxicity against human DU145 cells by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). |
AID1556404 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 1 to 5 uM incubated for 24 hrs by MTS assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
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. |
AID1846961 | Antiproliferative activity against human YCC-11 cells assessed as inhibition of cell viability | | | |
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. |
AID1596058 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1280296 | Inhibition of KDAC6 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method | 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. |
AID650218 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by flow cytometry (Rvb = 9.5 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1596055 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1454687 | Drug uptake in iv dosed rat brain after 90 mins by PET imaging method 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). |
AID1401926 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G0/G1 phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 80.65%) | 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. |
AID1881854 | Inhibition of HDAC2 (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | NO-HDAC dual inhibitors. |
AID328798 | Inhibition of HDAC5 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. |
AID488273 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID610086 | Inhibition of HDAC by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors. |
AID1548305 | 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 in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 9.1%) | | | |
AID1596042 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1706071 | Increase in LPS/IFNgamma-induced IL6 mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). |
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. |
AID650211 | Toxicity in human HCT116 cells xenografted in BALB/c- nu.nu mouse assessed as relative body weight change at 45 mg/kg, po administered every alternate days for 14 days measured up to day 16 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID316899 | Inhibition of HDAC6 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
AID1873471 | Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
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. |
AID1737666 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at subG1 phase at 16 uM for 48 hrs by PI staining based flow cytometry analysis | | | |
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. |
AID1401910 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%) | 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. |
AID1596049 | Inhibition of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1853066 | Inhibition of HDAC2-CoREST-LSD1 (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
| A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras. |
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. |
AID1586083 | Inhibition of human HDAC8 using RHKAcKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
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. |
AID1873427 | Inhibition of HDAC3 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr | 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. |
AID525011 | Inhibition of HDAC 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. |
AID777593 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-16-1# at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
AID1401900 | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 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. |
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. |
AID488363 | Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as reduction of tumor mass at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 16 measured on day 18 relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1847014 | Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as body weight loss at 100 mg/kg, ip administered for 14 days | | | |
AID664040 | Growth inhibition of human HCT116 cells after 2 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1235133 | Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors. |
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. |
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. |
AID777572 | Modulation of mouse C2C12 cell proliferation at 0.1 uM after 72 hrs | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
AID664041 | Growth inhibition of human U251 cells after 2 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1466381 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 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. |
AID670717 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity. |
AID316887 | Antiproliferative activity against human MKN45 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1596057 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID664380 | Inhibition of HDAC3 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1596062 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1578491 | Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac 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. |
AID1596034 | Inhibition of human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1466388 | Antiproliferative activity against HEL cells after 48 hrs by MTT assay | 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. |
AID1401917 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%) | 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. |
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. |
AID1901175 | 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 up to 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. |
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. |
AID519591 | Selectivity index, ratio of IC50 for human WI38 cells 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. |
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. |
AID777594 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-589 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
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. |
AID1917926 | Inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease. |
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. |
AID1401923 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G0/G1 phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 80.65%) | 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. |
AID360095 | Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1915581 | Cytotoxicity against human DU-145 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1380964 | Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM 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. |
AID1873439 | Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1847021 | Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in liver at 5 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based analys | | | |
AID1424833 | Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors. |
AID1293874 | Inhibition of HDAC in human HeLa nuclear extract using fluor de lys as substrate after 10 to 15 mins by spectrofluorometry | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID316892 | Inhibition of HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
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. |
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. |
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. |
AID1308513 | Inhibition of recombinant HDAC1 (unknown origin) using of Fluor-de-Lys substrate incubated for 10 mins by fluorimetric 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. |
AID1737645 | Inhibition of human recombinant HDAC2 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1401892 | Antiproliferative activity against human A375 cells at 8 uM after 72 hrs by CCK-8 assay relative to control | 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. |
AID1453362 | Inhibition of class 2 HDAC in HEL cells using Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID201624 | Compound was tested for antiproliferative activity against human SK-BR-3 cancer cell lines | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
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. |
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. |
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. |
AID1453364 | Inhibition of HDAC2 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
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. |
AID1706072 | Increase in LPS/IFNgamma-induced TNFalpha mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). |
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. |
AID519593 | Selectivity index, ratio of IC50 for human WI38 cells 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. |
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. |
AID1401897 | Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 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. |
AID1586067 | Growth inhibition of human KB cells after 48 hrs by SRB assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1466395 | Antitumor activity against human U937 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg/day administered via oral gavage for 13 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. |
AID1732172 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as sub-G1 phase at 8 uM incubated for 72 hrs by PI staining based flow cytometry analysis (Rvb = 0.8 %) | 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. |
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. |
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. |
AID316925 | Inhibition of human HepG2 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1454688 | Half life in human at 6 mg/m2, po | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
AID1740019 | Inhibition of recombinant human HDAC6 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
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. |
AID1596039 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
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. |
AID1467242 | 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 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. |
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. |
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. |
AID364648 | Inhibition of human recombinant HDAC by fluorimetric assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents. |
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. |
AID1548735 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by | 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. |
AID1474454 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID1548293 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%) | | | |
AID1474462 | Cytotoxicity against HUVEC after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID488366 | Cell cycle arrest in human HCT116 cells assessed as accumulation at subG1 phase at 10 uM after 48 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID488368 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
AID1466380 | Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 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. |
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. |
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%) | | | |
AID1401912 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%) | 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. |
AID1548734 | Inhibition of recombinant human HDAC5 using Boc-Lys (trifluoroacetyl)-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. |
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. |
AID1474456 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
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. |
AID1732201 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as increase in accumulation of G1 phase at 4 uM incubated for 24 hrs by PI staining based flow cytometry analysis | 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. |
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. |
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. |
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. |
AID1846955 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based MTT assay | | | |
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. |
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. |
AID1541441 | Inhibition of human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells at 10 uM ZMAL as substrate incubated for 90 mins by fluorescence assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. |
AID316896 | Inhibition of human HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
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. |
AID1876491 | Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression. |
AID664039 | Inhibition of HDAC1 using Fluor de Lys as substrate by fluorescence analysis | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID777606 | Induction of NO release in human HaCaT cells at 10 uM after 1 to 5 hrs by DAF-2D-based FACS analysis relative to DMSO-treated control | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1888470 | Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability at 100 uM incubated for 5 days | 2022 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 55 | Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat. |
AID421212 | Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Recent advances in the development of polyamine analogues as antitumor agents. |
AID50586 | Inhibitory concentration against colon HCT116 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1181316 | Induction of granulocytic differentiation in human U937 cells assessed as increase in CD11c expression at 5 uM after 48 hrs by 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. |
AID1453363 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID670718 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity. |
AID1873449 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as apparent inhibition constant using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme for 0.5 to 2 hrs followed by s | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID364642 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents. |
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. |
AID488276 | Inhibition of HDAC6 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1873440 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluoresc | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
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. |
AID316936 | Inhibition of HDAC7 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
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. |
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. |
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. |
AID1737641 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | | | |
AID519592 | Selectivity index, ratio of IC50 for breast 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. |
AID1556408 | Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of iNOS gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
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. |
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. |
AID1879900 | Inhibition of HDAC1 in human MV4-11 cells assessed as accumulation of acetylated histone H3 at 5 uM measured by immunoblotting method | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
AID1732165 | Inhibition of HDAC3 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence 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. |
AID1453359 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID650229 | Inhibition of HDAC1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1846954 | Inhibition of recombinant HDAC3 (unknown origin) at 1 uM relative to control | | | |
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. |
AID1453366 | Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
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. |
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. |
AID488360 | Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as reduction of tumor growth at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 16 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1873444 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
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%) | | | |
AID1467243 | 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 after 30 mins in presence of 0.2 uM S | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
| Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
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). |
AID1846980 | Selectivity index, ratio of IC50 for Inhibition of full length N-terminal GST-tagged human recombinant HDAC7 (501 to 952 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate to IC50 for inhibition of full length recombinant | | | |
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. |
AID1876490 | Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression. |
AID717813 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 7.81 x 10'-6 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. |
AID102521 | Inhibitory concentration against lung H446 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID488369 | Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 24 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
AID1401924 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%) | 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. |
AID316888 | Inhibition of HDAC from human SNU16 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1846974 | Inhibition of full length N-terminal GST-tagged human recombinant HDAC6 (1 to 1215 residues) expressed in Baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 | | | |
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. |
AID1732209 | Cytotoxicity against human A549 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. |
AID519590 | Toxicity in breast fibroblasts | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1737665 | Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP-1 level incubated for 24 hrs by Western blot analysis | | | |
AID488370 | Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
AID1846976 | Inhibition of full length C-terminal his-tagged human recombinant HDAC8 (142 to 143 residues) expressed in baculovirus in Sf9 insect cells using Ac-Leu-Gly-Lys (Tfa)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after | | | |
AID1548297 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%) | | | |
AID1596044 | Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
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. |
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. |
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. |
AID764214 | Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID650224 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at SubG1 phase at 10 uM after 24 hrs by flow cytometry (Rvb = 5.7 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1596075 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1732158 | Cytotoxicity against human MDA-MB-231 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. |
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. |
AID1732164 | Inhibition of HDAC2 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence 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. |
AID1732169 | Antiproliferative activity against HDACi-resistant human YCC3/7 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. |
AID777591 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-661 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
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. |
AID1401925 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%) | 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. |
AID1548292 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%) | | | |
AID610087 | Anticancer activity against human HCT116 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors. |
AID43458 | Inhibitory concentration against breast MCF-7 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1401899 | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 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. |
AID1691036 | Antiproliferative activity against human KB7D cells incubated for 48 hrs by SRB assay | | | |
AID161227 | Inhibitory concentration against prostate DU145 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID764213 | Inhibition of human recombinant HDAC4 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
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. |
AID1586069 | Growth inhibition of human MKN45 cells after 48 hrs by SRB assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
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. |
AID496803 | Inhibition of human HDAC3 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1596040 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1293872 | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID1881855 | Inhibition of HDAC3 (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | NO-HDAC dual inhibitors. |
AID1873438 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1556409 | Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of IL-10 gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
AID1596068 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
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. |
AID1401894 | Antiproliferative activity against human HeLa cells at 8 uM after 72 hrs by CCK-8 assay relative to control | 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. |
AID1453361 | Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
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. |
AID364641 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents. |
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. |
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. |
AID1737655 | Cytotoxicity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | | | |
AID1737664 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G1 phase at 4 uM for 24 hrs in presence of nocodazole by PI staining based flow cytometry analysis | | | |
AID1474452 | Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC in human HCT116 cells | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID1596053 | Inhibition of cell migration in human SMMC7721 cells at 0.5 uM measured after 48 hrs by microscopic analysis | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
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. |
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. |
AID269160 | Antitumor activity against human HCT116 cells xenografted in mouse at 20 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors. |
AID1691034 | Antiproliferative activity against human KB cells incubated for 48 hrs by SRB assay | | | |
AID1732207 | Cytotoxicity against human NCI-H661 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. |
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. |
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. |
AID1548294 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%) | | | |
AID1474460 | Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID650226 | Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1732161 | Cytotoxicity against human DLD-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. |
AID316931 | Inhibition of HDAC3 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1901167 | Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM measured after 24 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. |
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. |
AID1691035 | Antiproliferative activity against human KB-VIN cells incubated for 48 hrs by SRB assay | | | |
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. |
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. |
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. |
AID1596060 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1737667 | Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-3 level incubated for 24 hrs by Western blot analysis | | | |
AID1474459 | Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID1596043 | Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID525005 | Inhibition of HDAC7 in Fdelta508 CFTR-expressing human CFBE41o- monolayers assessed as increase in short circuit currents at 0.5 uM | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID8302 | Compound was tested for antiproliferative activity against human A549 cancer cell lines using MTT assay | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID1235135 | Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors. |
AID1737639 | Cytotoxicity against human HDACi-sensitive YCC-11 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay | | | |
AID385431 | Inhibition of TNF-alpha-induced tissue factor activity in HUVEC at 30 uM preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
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. |
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%) | | | |
AID1578487 | Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 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. |
AID1453360 | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID1235134 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors. |
AID316941 | Inhibition of HDAC9 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1479828 | Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 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. |
AID44724 | Inhibitory concentration against bladder T24 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1691040 | Inhibition of human recombinant HDAC8 using RHKAcKAc-AMC as substrate measured after 60 mins by fluorescence assay | | | |
AID50591 | Inhibitory concentration against colon SW48 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1401908 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%) | 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. |
AID1732167 | Inhibition of HDAC10 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence 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. |
AID777588 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-126# at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1293873 | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
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. |
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. |
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. |
AID1873446 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence b | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID90348 | Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1). | 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. |
AID1596063 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1732202 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as increase in accumulation of G2/M phase at 2.5 uM incubated for 24 hrs by PI staining based flow cytometry analysis | 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. |
AID1454683 | Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in motivation to consume alcohol at 500 uM, icv administered twice 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). |
AID1446910 | Inhibition of Schistosoma mansoni KDAC8 at 30 uM 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. |
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%) | | | |
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. |
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. |
AID1596051 | Selectivity ratio of IC50 for human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) 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%) | | | |
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). |
AID1294934 | Inhibition of HDAC in human HeLa nuclear extract using Boc-acetyl-lysine-AMC as substrate incubated for 30 mins in dark by microplate reader analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1737651 | Inhibition of human recombinant HDAC7 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1556400 | Inhibition of human recombinant C-terminal FLAG-tagged HDAC2 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
AID1737653 | Inhibition of human recombinant HDAC10 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1873450 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as apparent inhibition constant using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme for 0.5 to 2 hrs followed by substrate addition and measured after 30 mins | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID650213 | Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as suppression of tumor growth at 45 mg/kg, po administered every alternate days for 14 days measured up to day 16 relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1873448 | Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
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. |
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. |
AID488361 | Toxicity in human HCT116 cells xenografted BALB/c nu/nu mouse assessed increase of running behavior at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 16 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1548295 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%) | | | |
AID1915555 | Inhibition of human recombinant HDAC1 (unknown origin) using MAZ1600 as substrate preincubated for 3 hrs followed by substrate addition by multilabel plate reader method | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
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. |
AID488365 | Cell cycle arrest in human HCT116 cells assessed as accumulation at subG1 phase at 10 uM after 24 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1548278 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells at 100 nM in presence of bortezomib incubated for 24 hrs by TUNEL assay | | | |
AID525026 | Inhibition of HDAC 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. |
AID1453356 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID1530562 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition at 10 uM after 48 hrs by SYBR green1 staining based flow cytometry relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID90837 | Inhibitory concentration ratio against HDAC6/HDAC1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID777596 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-663B at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1401928 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%) | 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. |
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. |
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. |
AID777599 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-193b# at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID551597 | Inhibition of HDAC3 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy. |
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. |
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. |
AID324957 | Inhibition of HDAC6 in HEK293 cells 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. |
AID303014 | Inhibition of human recombinant HDAC1 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. |
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. |
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%) | | | |
AID650225 | Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
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. |
AID1821968 | Antiproliferative activity against human YCC-11 cells assessed as cell growth inhibition | | | |
AID1737648 | Inhibition of human recombinant HDAC3 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1740016 | Inhibition of recombinant human HDAC4 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1901176 | 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 up to 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. |
AID620534 | Reactivation of MeCp2 mutant expression in human GM11272 cells after 6 days 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. |
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. |
AID488362 | Toxicity in human HCT116 cells xenografted BALB/c nu/nu mouse assessed weight loss at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1401915 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%) | 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. |
AID1821969 | Antiproliferative activity against human YCC3/7 cells assessed as cell growth inhibition | | | |
AID1401909 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%) | 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. |
AID717814 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 3.91 x 10'-6 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. |
AID1401916 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%) | 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. |
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. |
AID1882460 | Displacement of [3H]-acetylated histones from HDAC1 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method | 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. |
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. |
AID1466412 | Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis | 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. |
AID1737649 | Inhibition of human recombinant HDAC4 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1454685 | Lipophilicity, log D of the compound at pH 7.4 | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
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. |
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. |
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. |
AID1454682 | Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in operant alcohol self-administration at 500 uM, icv administered twice 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). |
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. |
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. |
AID1453367 | Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC1 (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID1917928 | Inhibition of HDAC3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease. |
AID488367 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1732196 | Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in p21 expression at 4 uM incubated for 24 hrs by Western blot analysis | 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. |
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. |
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. |
AID1737646 | Inhibition of human recombinant HDAC6 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
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. |
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. |
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. |
AID1586082 | Inhibition of human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1846958 | Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based CCK-8 assay | | | |
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). |
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. |
AID1293875 | Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
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. |
AID1586078 | Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1401898 | Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 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. |
AID1873442 | Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1280295 | Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method | 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. |
AID1847001 | Induction of apoptosis in mouse B16-F10 cells assessed as early apoptotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 1.68 %) | | | |
AID777595 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-766 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID488274 | Inhibition of HDAC2 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
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. |
AID1596077 | Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1596050 | Inhibition of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS Green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence me | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1466390 | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay | 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. |
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. |
AID1732160 | Cytotoxicity against human HeLa 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. |
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. |
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. |
AID1732166 | Inhibition of HDAC8 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence 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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID610090 | Anticancer activity against human A2780 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors. |
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. |
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. |
AID1764296 | Inhibition of HDAC6 in human CAL-27 cells assessed as accumulation of acetylated alpha-tubulin 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. |
AID1847002 | Induction of apoptosis in mouse B16-F10 cells assessed as late apoptotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 0.00 %) | | | |
AID1596048 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1466408 | Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis | 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. |
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. |
AID1847000 | Induction of apoptosis in mouse B16-F10 cells assessed as viable cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 98.3 %) | | | |
AID1879890 | Inhibition of recombinant human HDAC1 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
AID777600 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-21# at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1466413 | Toxicity in BALB/c nude mouse xenografted with human U937 cells assessed as body weight loss at 100 mg/kg/day administered via oral gavage for 13 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. |
AID364644 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents. |
AID777590 | Effect on HDAC in human HaCaT cells assessed as upregulation of miR-1227 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
AID1548296 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%) | | | |
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. |
AID1888465 | Anti-androgenic activity at androgen receptor (unknown origin) expressed in HEK293 cells by BRET assay | 2022 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 55 | Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat. |
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. |
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. |
AID80683 | In vitro antiproliferative activity against human cancer cell line HCT116 using MTT assay | 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. |
AID1586085 | Inhibition of human HDAC10 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1466393 | Antiproliferative activity against human ES2 cells after 48 hrs by MTT assay | 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. |
AID385692 | Inhibition of HDAC4 catalytic domain expressed in HEK293 cells upto 10,000 nM by Biomol assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
| Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases. |
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. |
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. |
AID610088 | Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors. |
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. |
AID764212 | Inhibition of human recombinant HDAC6 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1453365 | Inhibition of HDAC3 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID1556401 | Inhibition of human recombinant C-terminal His-tagged HDAC3/NCOR2 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
AID1901146 | Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID519589 | Toxicity in human WI38 cells | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1737644 | Inhibition of human recombinant HDAC1 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1294943 | Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1917927 | Inhibition of HDAC2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease. |
AID777598 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-935 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
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. |
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. |
AID1403468 | Cytotoxicity against human HaCaT cells assessed as increase in dead cells 0.1 to 100 uM after 72 hrs by Trypan Blue-based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. |
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. |
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. |
AID1847023 | Cardiotoxicity in C57BL/6 mouse ssessed as shortening of QTc level by ECG analysis | | | |
AID1548732 | Inhibition of recombinant full length human C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluoresce | 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. |
AID1873472 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1474453 | Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
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. |
AID1578490 | Inhibition of recombinant human HDAC9 (604-1066 residues) 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. |
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). |
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. |
AID1737663 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as reduction in population between G1 to G2/M phases at 4 uM for 24 hrs by PI staining based flow cytometry analysis | | | |
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. |
AID1530563 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID1846997 | Induction of cell cycle arrest in mouse B16-F10 cells assessed as accumulation of cells in G2/M phase at 100 nM measured after 48 hrs by PI/RNaseA staining based flow cytometry analysis (Rvb= 5.76%) | | | |
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. |
AID1548892 | Induction of apoptosis in human MV4-11 cells harboring wild type p53/FLT3-ITD mutant assessed as cleavage of pro-caspase 3 at 1000 to 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. |
AID385436 | Inhibition of LPS-induced tissue factor activity in HUVEC at 30 uM preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
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. |
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. |
AID1596069 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1847015 | Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as reduction in tumor weight at 10 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone | | | |
AID1401913 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%) | 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. |
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. |
AID1737642 | Cytotoxicity in human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
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. |
AID1691039 | Inhibition of human recombinant HDAC3/NCOR2 using RHKKAc-AMC as substrate measured after 60 mins by fluorescence assay | | | |
AID1401918 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%) | 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. |
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. |
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. |
AID1401927 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%) | 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. |
AID1732168 | Antiproliferative activity against HDACi-sensitive human YCC-11 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. |
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. |
AID1596052 | Selectivity ratio of IC50 for human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1737656 | Cytotoxicity against human KG -1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | | | |
AID650221 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by flow cytometry (Rvb = 81.9 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID78450 | Tested for antiproliferative activity against HCT116 colorectal human carcinoma cell using WST-1 assay | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group. |
AID1466401 | Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 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. |
AID316891 | Inhibition of HDAC | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1882459 | Displacement of [3H]-acetylated histones HDAC6 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method | 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. |
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. |
AID650230 | Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID73169 | Inhibitory concentration against normal fibroblast MRHF cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1846962 | Antiproliferative activity against human YCC3/7 cells assessed as inhibition of cell viability | | | |
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. |
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. |
AID650227 | Solubility of the compound in 10 % DMSO/Water | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID316895 | Inhibition of human MCF7 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID664379 | Inhibition of HDAC1 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase 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). |
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). |
AID90349 | Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID1873441 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1881853 | Inhibition of HDAC1 (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | NO-HDAC dual inhibitors. |
AID1740014 | Inhibition of recombinant human HDAC3 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
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 | | | |
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. |
AID1308514 | Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement 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. |
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. |
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. |
AID1403469 | Cytotoxicity against mouse C2C12 cells assessed as increase in dead cells 0.5 to 10 uM after 72 hrs by Trypan Blue-based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. |
AID1596080 | Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1556399 | Inhibition of human recombinant C-terminal His/FLAG-tagged HDAC1 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
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. |
AID1403455 | Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. |
AID1453357 | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
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. |
AID1474455 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
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. |
AID1691038 | Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected insect cells using RHKKAc-AMC as substrate measured after 60 mins by fluorescence assay | | | |
AID1737647 | Inhibition of human recombinant HDAC8 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
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. |
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. |
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. |
AID1596072 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1596041 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1901166 | Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM measured after 24 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. |
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. |
AID1479838 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
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. |
AID1737657 | Cytotoxicity against human THP-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay | | | |
AID1596033 | Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1474461 | Inhibition of HDAC1 (unknown origin) using deacetylase fluorogenic substrate pretreated for 5 mins followed by substrate addition after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
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. |
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. |
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. |
AID1403456 | Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. |
AID1578485 | Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac 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. |
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. |
AID328828 | Antitumor activity against human HCT116 cells xenografted BALB/c mouse assessed as tumor growth inhibition at 60 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. |
AID1846971 | Inhibition of recombinant HDAC1 (unknown origin) at 1 uM | | | |
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. |
AID93030 | Effect on induced hyperacetylation of histones in whole cells | 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. |
AID664382 | Inhibition of HDAC4 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1401922 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 0.125 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%) | 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. |
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. |
AID1556406 | Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of TNF-alpha gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
AID1401911 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%) | 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. |
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. |
AID1873480 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as inhibition constant of EI complex in the first binding step using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate in the presence of inosi | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1732159 | Cytotoxicity against human MDA-MB-468 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. |
AID1596047 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1466410 | Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis | 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. |
AID488357 | Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
AID1454684 | Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in relapse phenomenon after period of abstinence at 500 uM, icv administered twice 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). |
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. |
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. |
AID1401890 | Antiproliferative activity against human MGC803 cells at 8 uM after 72 hrs by CCK-8 assay relative to control | 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. |
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. |
AID1380965 | Inhibition of HDAC6 in human HeLa cells assessed as increase in intracellular acetyl-tubulin levels at 1 uM 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. |
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. |
AID316934 | Inhibition of HDAC4 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
AID1293876 | Inhibition of HDAC in human HeLa nuclear extract assessed as accumulation of acetylated histone H3 after 24 hrs by western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID1873443 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
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. |
AID1873437 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based ass | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1596067 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1706069 | Increase in LPS/IFNgamma-induced IL-10 mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). |
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. |
AID1740018 | Inhibition of recombinant human HDAC9 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1408543 | Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches. |
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. |
AID1879896 | Inhibition of recombinant human HDAC8 using H2N-Arg- His-Lys(Ac)-Lys(Ac)-AMC as substrate incubated for 90 mins and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
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. |
AID1873447 | Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID777605 | Inhibition of HDAC activity in human HaCaT cell lysate at 1 to 50 uM after 1 hr by colorimetry | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1737662 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as reduction in population at S phase at 4 uM for 24 hrs by PI staining based flow cytometry analysis | | | |
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. |
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. |
AID1401893 | Antiproliferative activity against human HeLa cells at 2 uM after 72 hrs by CCK-8 assay relative to control | 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. |
AID777592 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-744# at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1737652 | Inhibition of human recombinant HDAC9 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1474463 | Therapeutic index, ratio of IC50 for HUVEC to IC50 for human HCT116 cells | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID1740012 | Inhibition of recombinant human HDAC1 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1846975 | Inhibition of full length N-terminal GST-tagged human recombinant HDAC7 (501 to 952 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins | | | |
AID1847020 | Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in liver at 10 mg/kg, ip administered for 14 days by H and E staining based analysis | | | |
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. |
AID1454689 | Half life in human at 2 mg/m2 dosed twice a week | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
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. |
AID488358 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
AID496802 | Inhibition of human HDAC2 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
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. |
AID650217 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by flow cytometry (Rvb = 5.4 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
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. |
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. |
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%) | | | |
AID717815 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 1.95 x 10'-6 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. |
AID1846970 | Inhibition of recombinant HDAC3 (unknown origin) at 1 uM | | | |
AID1454686 | Drug uptake in iv dosed baboon brain after 90 mins by PET imaging method 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). |
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. |
AID1915537 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1847017 | Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in kidney at 10 mg/kg, ip administered for 14 days by H and E staining based analysis | | | |
AID1453355 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
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. |
AID316920 | Antitumor activity against human HCT116 cells xenografted in nude mouse model at 20 mg/kg, ip | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID43462 | Inhibitory concentration against breast MDA-MB-231 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID650220 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 24 hrs by flow cytometry (Rvb = 10.6 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1846973 | Inhibition of recombinant HDAC3 (unknown origin) using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins | | | |
AID551596 | Inhibition of HDAC2 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy. |
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. |
AID1691037 | Inhibition of recombinant human full-length C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | | | |
AID420319 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAH 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. |
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. |
AID1556405 | Inhibition of HDAC1 in LPS/IFNgamma-stimulated mouse RAW blue cells assessed as upregulation of NFkappaB transcriptional activity by measuring increase in SEAP activity at 1 to 2.5 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
AID1596070 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1586084 | Inhibition of human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID316903 | Inhibition of human HCT116 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID488372 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
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. |
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%) | | | |
AID269168 | Antitumor activity against human SW48 cells xenografted in mouse at 20 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors. |
AID1474451 | Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC in human A2780 cells | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID1901145 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorimetry | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
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. |
AID1846972 | Inhibition of full length recombinant human HDAC1 (1 to 482 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins | | | |
AID1740013 | Inhibition of recombinant human HDAC2 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
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. |
AID421211 | Antitumor activity against mouse ML1 cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Recent advances in the development of polyamine analogues as antitumor agents. |
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. |
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. |
AID551595 | Inhibition of HDAC1 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy. |
AID1548303 | 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 in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 42%) | | | |
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. |
AID1596071 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1424827 | Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors. |
AID1847034 | In vivo inhibition of HDAC in tumor of mouse B16-F10 cells xenografted in C57BL/6 mouse assessed as increase in acetylated histone-H3 expression by H and E staining based immunohistochemistry method | | | |
AID324951 | Inhibition of HDAC4 H976Y mutant 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. |
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. |
AID1467241 | 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 in presence of 0.2 uM SAHA by f | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
| Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. |
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. |
AID1548733 | Inhibition of recombinant human HDAC4 using Boc-Lys (trifluoroacetyl)-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. |
AID1732163 | Inhibition of HDAC1 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence 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. |
AID1847024 | Cardiotoxicity in C57BL/6 mouse ssessed as shortening of QTc level in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by ECG analysis | | | |
AID1578486 | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac 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. |
AID1586079 | Inhibition of human HDAC3 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
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. |
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. |
AID496801 | Inhibition of human HDAC1 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
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. |
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. |
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%) | | | |
AID1401914 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%) | 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. |
AID1846959 | Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell viability measured for 48 hrs in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by microplate reader based MTT assay | | | |
AID1596038 | Antiproliferative activity against human HeLa cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID316898 | Inhibition of HDAC2 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
AID70208 | Inhibitory concentration against normal epithelial HMEC cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
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. |
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. |
AID1596066 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID717811 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-5 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. |
AID1596065 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1879893 | Inhibition of recombinant human HDAC6 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
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. |
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. |
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. |
AID1479842 | Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID670719 | Inhibition of HDAC1 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity. |
AID1847035 | In vivo inhibition of HDAC in tumor of mouse B16-F10 cells xenografted in C57BL/6 mouse assessed as increase in acetylated histone-H3 expression in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based immunohistoch | | | |
AID1876492 | Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression. |
AID488359 | Solubility in 10% DMSO-water | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
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. |
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. |
AID1901147 | Inhibition of recombinant human full-length C-terminal Flag-His6-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases 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. |
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. |
AID1596059 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID1737650 | Inhibition of human recombinant HDAC5 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | | | |
AID1479843 | Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
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. |
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. |
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. |
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. |
AID1401891 | Antiproliferative activity against human A375 cells at 2 uM after 72 hrs by CCK-8 assay relative to control | 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. |
AID1706070 | Increase in LPS/IFNgamma-induced iNOS mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). |
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. |
AID717812 | Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 1.56 x 10'-5 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. |
AID1403454 | Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors. |
AID328831 | Toxicity against human HCT116 cells xenografted BALB/c mouse assessed as body weight loss at 25 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. |
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. |
AID650228 | Inhibition of HDAC2 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1846956 | Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based MTT assay | | | |
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. |
AID1853011 | Inhibition of HDAC3-SMRT (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
| A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras. |
AID1847013 | Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as tumor growth inhibition at 10 mg/kg, ip administered for 14 days | | | |
AID670720 | Inhibition of HDAC2 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity. |
AID1691061 | Induction of apoptosis in human KB7D cells assessed as increase in activated gammaH2AX expression at 5 uM measured after 24 hrs by Western blot analysis | | | |
AID102520 | Inhibitory concentration against lung A549 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1881857 | Vasodilating activity in rat aorta in presence of ODQ | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | NO-HDAC dual inhibitors. |
AID1737640 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | | | |
AID488371 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by flow cytometry analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1873428 | Inhibition of HDAC2 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr | 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. |
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. |
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. |
AID488275 | Inhibition of HDAC3 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1596045 | Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) 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. |
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. |
AID303015 | Inhibition of human recombinant HDAC2 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. |
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. |
AID316927 | Inhibition of human CCD1059SK cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1586081 | Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID316893 | Inhibition of HDAC8 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1596074 | Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
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. |
AID1882461 | Displacement of [3H]-acetylated histones from HDAC3 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method | 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. |
AID764209 | Partition coefficient, log D of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID488364 | Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
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. |
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. |
AID1737668 | Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-8 level incubated for 24 hrs by Western blot analysis | | | |
AID1548275 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay | | | |
AID1873473 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescen | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1873429 | Mixed-type inhibition of HDAC3 (unknown origin) at 3.90625 to 62.5 nM by Lineweaver-Burk plot 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. |
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. |
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. |
AID316926 | Inhibition of human SW620 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
AID777589 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-941 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1401896 | Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 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. |
AID1596073 | Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1479845 | Induction of apoptosis in human PBMC at 5 uM after 24 hrs by Annexin V/propidium iodide staining-based flow cytometric method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
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. |
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. |
AID1556407 | Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of IL-6 gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages. |
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. |
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. |
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. |
AID316943 | Inhibition of human HDAC1 assessed as histone H4 acetylation in cell based assay | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID488277 | Inhibition of HDAC8 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1915580 | Cytotoxicity against human K562 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1474457 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
AID316935 | Inhibition of HDAC5 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
AID1280294 | Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method | 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. |
AID1847037 | Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as tumor growth inhibition at 10 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone | | | |
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. |
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. |
AID1596036 | Antiproliferative activity against human A375 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID269169 | Antitumor activity against human A549 cells xenografted in mouse at 20 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors. |
AID1578488 | Inhibition of recombinant full length human HDAC5 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. |
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). |
AID1737643 | Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
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. |
AID1586077 | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
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. |
AID1578489 | Inhibition of recombinant full length human HDAC7 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. |
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%) | | | |
AID1732171 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as sub-G1 phase at 4 uM incubated for 72 hrs by PI staining based flow cytometry analysis (Rvb = 0.8 %) | 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. |
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. |
AID106868 | Compound was tested for antiproliferative activity against human MKN45 cancer cell lines | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
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. |
AID1873426 | Inhibition of HDAC1 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr | 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. |
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. |
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. |
AID1740017 | Inhibition of recombinant human HDAC7 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1596061 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID764208 | Intrinsic aqueous solubility of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
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. |
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. |
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. |
AID610089 | Anticancer activity against human DU145 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors. |
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. |
AID650222 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by flow cytometry (Rvb = 74.2 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1596046 | Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID316922 | Antitumor activity against human SW48 cells xenografted in nude mouse model at 20 mg/kg, ip | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
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. |
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. |
AID650223 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at SubG1 phase at 10 uM after 48 hrs by flow cytometry (Rvb = 2.3 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
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. |
AID385686 | Inhibition of flag-tagged HDAC4 by Biomol assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
| Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases. |
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. |
AID1466403 | Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as relative tumor increment ratio at 50 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. |
AID1847003 | Induction of apoptosis in mouse B16-F10 cells assessed as necrotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 0.012 %) | | | |
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. |
AID1466397 | Antitumor activity against human U937 cells xenografted in BALB/c nude mouse assessed as relative tumor increment ratio at 50 mg/kg/day administered via oral gavage for 13 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. |
AID420322 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 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. |
AID1846957 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based CCK-8 assay | | | |
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). |
AID1873479 | Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme and inositol hexa phosphate for 2 hrs followed by substrate addition an | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1453358 | Antiproliferative activity against HEL cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. |
AID777597 | Effect on HDAC in human HaCaT cells assessed as downregulation of miR-629 at 10 uM after 1 hr by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1466392 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 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. |
AID360094 | Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1548299 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%) | | | |
AID385691 | Inhibition of flag-tagged HDAC4 expressed in HEK293 cells upto 10,000 nM by Biomol assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
| Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases. |
AID1454739 | Lipophilicity, log P of the compound at pH 7.4 | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
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. |
AID90666 | Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1) | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID316918 | Antitumor activity against human A549 cells xenografted in nude mouse model at 20 mg/kg, ip | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID519594 | Selectivity index, ratio of IC50 for breast 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. |
AID1732208 | Cytotoxicity against human NCI-H1299 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. |
AID90529 | Inhibitory concentration against histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID1466399 | Toxicity in BALB/c nude mouse xenografted with human U937 cells assessed as body weight at 50 mg/kg/day administered via oral gavage for 13 days (Rvb = 25.39 +/- 1.18 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. |
AID1401895 | Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 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. |
AID1548736 | Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs b | 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. |
AID1586080 | Inhibition of human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1881856 | Vasodilating activity in rat aorta | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | NO-HDAC dual inhibitors. |
AID1401889 | Antiproliferative activity against human MGC803 cells at 2 uM after 72 hrs by CCK-8 assay relative to control | 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. |
AID1466389 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 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. |
AID1466404 | Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as body weight at 50 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. |
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%) | | | |
AID1596037 | Antiproliferative activity against human HeLa cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
AID650219 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by flow cytometry (Rvb = 10.4 %) | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1401919 | Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%) | 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. |
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. |
AID1474458 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents. |
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. |
AID1235132 | Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by fluorogenic substrate addition measured after 30 mins by microplate reader analysis | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors. |
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 | | | |
AID1873445 | Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
| Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity. |
AID1401921 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 0.125 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%) | 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. |
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. |
AID777601 | Induction of HDAC4 nuclear shuttling in human HaCaT cells at 10 uM after 1 hr by immunofluorescence method relative to DMSO-treated control | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor. |
AID1596035 | Antiproliferative activity against human A375 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1847012 | Upregulation of AC-H3 in mouse B16-F10 cells incubated for 12 hrs by Western blot analysis | | | |
AID1466391 | Antiproliferative activity against human U266 cells after 48 hrs by MTT assay | 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. |
AID1548298 | Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%) | | | |
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. |
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. |
AID664384 | Inhibition of HDAC10 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1548304 | 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 in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 46%) | | | |
AID1596056 | Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (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. |
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. |
AID1586068 | Growth inhibition of human A549 cells after 48 hrs by SRB assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1280297 | Inhibition of KDAC8 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method | 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. |
AID664381 | Inhibition of HDAC8 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID90208 | Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives. |
AID664383 | Inhibition of HDAC6 | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. |
AID1737654 | Cytotoxicity against human HDACi-sensitive YCC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay | | | |
AID1740015 | Inhibition of recombinant human HDAC8 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
AID1847018 | Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in kidney at 5 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based analy | | | |
AID1596064 | Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%) | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors. |
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. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |