Page last updated: 2024-08-07 17:21:11
Histone deacetylase 2
A histone deacetylase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92769]
Synonyms
HD2;
EC 3.5.1.98
Research
Bioassay Publications (410)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.24) | 18.2507 |
| 2000's | 72 (17.56) | 29.6817 |
| 2010's | 242 (59.02) | 24.3611 |
| 2020's | 95 (23.17) | 2.80 |
Compounds (96)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gamma-aminobutyric acid | Homo sapiens (human) | Ki | 8.1900 | 1 | 1 |
| butyric acid | Homo sapiens (human) | IC50 | 206.0000 | 2 | 2 |
| butyric acid | Homo sapiens (human) | Ki | 136.0000 | 1 | 1 |
| celecoxib | Homo sapiens (human) | IC50 | 1.6370 | 1 | 1 |
| ci 994 | Homo sapiens (human) | IC50 | 13.0657 | 14 | 24 |
| ci 994 | Homo sapiens (human) | Ki | 0.1188 | 2 | 4 |
| clioquinol | Homo sapiens (human) | IC50 | 71.0857 | 1 | 14 |
| valproic acid | Homo sapiens (human) | IC50 | 1,819.9480 | 5 | 5 |
| valproic acid | Homo sapiens (human) | Ki | 564.0000 | 1 | 1 |
| fluconazole | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| beta-thujaplicin | Homo sapiens (human) | Ki | 0.0154 | 1 | 1 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | Homo sapiens (human) | IC50 | 0.8330 | 2 | 2 |
| entinostat | Homo sapiens (human) | IC50 | 3.3769 | 54 | 72 |
| entinostat | Homo sapiens (human) | Ki | 0.1835 | 4 | 4 |
| 4-phenylbutyric acid | Homo sapiens (human) | IC50 | 65.0000 | 1 | 1 |
| 4-phenylbutyric acid | Homo sapiens (human) | Ki | 2.8000 | 1 | 1 |
| pomiferin | Homo sapiens (human) | IC50 | 1.0500 | 1 | 1 |
| pyroxamide | Homo sapiens (human) | IC50 | 5.1000 | 2 | 2 |
| pyroxamide | Homo sapiens (human) | Ki | 36.0000 | 1 | 1 |
| suberoyl bis-hydroxamic acid | Homo sapiens (human) | IC50 | 8.2300 | 1 | 1 |
| suberoyl bis-hydroxamic acid | Homo sapiens (human) | Ki | 0.0290 | 1 | 1 |
| scriptaid | Homo sapiens (human) | IC50 | 0.6300 | 2 | 2 |
| scriptaid | Homo sapiens (human) | Ki | 0.0022 | 1 | 1 |
| 4-phenylbutyric acid, sodium salt | Homo sapiens (human) | Ki | 6.3400 | 1 | 1 |
| fenofibrate | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| vorinostat | Homo sapiens (human) | IC50 | 1.9998 | 354 | 389 |
| vorinostat | Homo sapiens (human) | Ki | 0.3447 | 8 | 8 |
| benzohydroxamic acid | Homo sapiens (human) | IC50 | 7.9100 | 1 | 1 |
| acetylcysteine | Homo sapiens (human) | IC50 | 3,160.0000 | 1 | 1 |
| camptothecin | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| lovastatin | Homo sapiens (human) | IC50 | 25.9330 | 1 | 1 |
| atorvastatin | Homo sapiens (human) | IC50 | 22.5470 | 1 | 1 |
| bendamustine | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| ubenimex | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| osajin | Homo sapiens (human) | IC50 | 6.5300 | 1 | 1 |
| lapatinib | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| N-hydroxy-2-phenylacetamide | Homo sapiens (human) | IC50 | 33.3300 | 1 | 1 |
| n-hydroxy-2,2-diphenylacetamide | Homo sapiens (human) | IC50 | 20.4000 | 3 | 3 |
| bortezomib | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| trapoxin a | Homo sapiens (human) | IC50 | 0.0047 | 3 | 3 |
| e-z cinnamic acid | Homo sapiens (human) | Ki | 0.0082 | 1 | 1 |
| trichostatin a | Homo sapiens (human) | IC50 | 0.6401 | 67 | 87 |
| trichostatin a | Homo sapiens (human) | Ki | 0.0851 | 6 | 6 |
| caffeic acid | Homo sapiens (human) | IC50 | 2,540.0000 | 1 | 1 |
| caffeic acid | Homo sapiens (human) | Ki | 10.8400 | 1 | 1 |
| curcumin | Homo sapiens (human) | IC50 | 187.0000 | 1 | 1 |
| curcumin | Homo sapiens (human) | Ki | 97.6700 | 1 | 1 |
| chlorogenic acid | Homo sapiens (human) | IC50 | 258.3333 | 3 | 3 |
| chlorogenic acid | Homo sapiens (human) | Ki | 0.1350 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | IC50 | 10.0000 | 3 | 3 |
| desmethylanethol trithione | Homo sapiens (human) | IC50 | 0.4500 | 2 | 2 |
| 5-chloro-7-[(4-ethyl-1-piperazinyl)-(3-pyridinyl)methyl]-8-quinolinol | Homo sapiens (human) | IC50 | 25.1950 | 1 | 8 |
| ex 527 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sodium butyrate | Homo sapiens (human) | IC50 | 273.0000 | 4 | 4 |
| sodium butyrate | Homo sapiens (human) | Ki | 365.0000 | 1 | 1 |
| 5'-o-caffeoylquinic acid | Homo sapiens (human) | IC50 | 185.2000 | 2 | 2 |
| harmine | Homo sapiens (human) | IC50 | 10.0000 | 3 | 3 |
| aureusidin | Homo sapiens (human) | IC50 | 28.7000 | 2 | 2 |
| romidepsin | Homo sapiens (human) | IC50 | 0.8883 | 9 | 9 |
| romidepsin | Homo sapiens (human) | Ki | 0.0000 | 2 | 2 |
| cinnamoylhydroxamic acid | Homo sapiens (human) | IC50 | 0.4570 | 1 | 1 |
| 3',4'-dihydroxyaurone | Homo sapiens (human) | IC50 | 6.6500 | 2 | 2 |
| psammaplin a | Homo sapiens (human) | IC50 | 0.0290 | 3 | 3 |
| trichostatin c | Homo sapiens (human) | IC50 | 23.6300 | 1 | 1 |
| laq824 | Homo sapiens (human) | IC50 | 0.0506 | 9 | 12 |
| laq824 | Homo sapiens (human) | Ki | 0.0014 | 2 | 2 |
| indigo carmine | Homo sapiens (human) | IC50 | 321.6200 | 2 | 2 |
| tanespimycin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| pd 404182 | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| tubacin | Homo sapiens (human) | IC50 | 5.5187 | 8 | 8 |
| tubacin | Homo sapiens (human) | Ki | 0.6114 | 2 | 2 |
| (3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone | Homo sapiens (human) | IC50 | 0.0185 | 11 | 11 |
| (3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| belinostat | Homo sapiens (human) | IC50 | 0.2401 | 12 | 12 |
| belinostat | Homo sapiens (human) | Ki | 0.0079 | 3 | 3 |
| sk-7041 | Homo sapiens (human) | IC50 | 0.1720 | 1 | 1 |
| panobinostat | Homo sapiens (human) | IC50 | 0.2526 | 19 | 27 |
| panobinostat | Homo sapiens (human) | Ki | 0.0076 | 5 | 5 |
| hdac-42 | Homo sapiens (human) | IC50 | 0.1580 | 2 | 2 |
| 4-acetamido-N-(2-amino-5-thiophen-2-ylphenyl)benzamide | Homo sapiens (human) | IC50 | 5.9060 | 12 | 33 |
| 4-acetamido-N-(2-amino-5-thiophen-2-ylphenyl)benzamide | Homo sapiens (human) | Ki | 0.1258 | 2 | 4 |
| n1-(2-aminophenyl)-n7-phenylheptanediamide | Homo sapiens (human) | IC50 | 27.0600 | 3 | 3 |
| bml 210 | Homo sapiens (human) | IC50 | 45.3650 | 10 | 10 |
| n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide | Homo sapiens (human) | IC50 | 3.0441 | 9 | 9 |
| givinostat | Homo sapiens (human) | IC50 | 0.2930 | 1 | 1 |
| givinostat | Homo sapiens (human) | Ki | 0.0030 | 2 | 2 |
| mocetinostat | Homo sapiens (human) | IC50 | 3.5691 | 9 | 18 |
| mocetinostat | Homo sapiens (human) | Ki | 0.0324 | 1 | 1 |
| methyl 3,5-di-o-caffeoyl quinate | Homo sapiens (human) | IC50 | 6.2900 | 2 | 2 |
| r 306465 | Homo sapiens (human) | IC50 | 0.0075 | 2 | 2 |
| luotonin a | Homo sapiens (human) | IC50 | 6.4000 | 1 | 1 |
| quisinostat | Homo sapiens (human) | IC50 | 0.0018 | 9 | 9 |
| quisinostat | Homo sapiens (human) | Ki | 0.0155 | 2 | 2 |
| abexinostat | Homo sapiens (human) | IC50 | 0.0630 | 1 | 1 |
| abexinostat | Homo sapiens (human) | Ki | 0.0493 | 3 | 8 |
| chidamide | Homo sapiens (human) | IC50 | 1.6254 | 5 | 4 |
| hc toxin | Homo sapiens (human) | IC50 | 0.4300 | 1 | 1 |
| hc toxin | Homo sapiens (human) | Ki | 0.4700 | 1 | 1 |
| azumamide e | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| azumamide e | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
| cnf 2024 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| N-(2-aminophenyl)-2-pyrazinecarboxamide | Homo sapiens (human) | IC50 | 2.2810 | 2 | 2 |
| pci 34051 | Homo sapiens (human) | IC50 | 51.5714 | 7 | 7 |
| cudc 101 | Homo sapiens (human) | IC50 | 0.1566 | 7 | 4 |
| largazole | Homo sapiens (human) | IC50 | 0.8721 | 6 | 6 |
| N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]-oxomethyl]-5-isoxazolyl]phenyl]carbamic acid tert-butyl ester | Homo sapiens (human) | IC50 | 0.1317 | 3 | 3 |
| trichostatin rk | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| jq1 compound | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| tubastatin a | Homo sapiens (human) | IC50 | 18.6676 | 30 | 39 |
| tubastatin a | Homo sapiens (human) | Ki | 3.4500 | 2 | 2 |
| pracinostat | Homo sapiens (human) | IC50 | 0.2080 | 2 | 2 |
| pracinostat | Homo sapiens (human) | Ki | 0.0270 | 1 | 1 |
| acy-1215 | Homo sapiens (human) | IC50 | 0.1116 | 17 | 17 |
| acy-1215 | Homo sapiens (human) | Ki | 0.2040 | 1 | 1 |
| cudc-907 | Homo sapiens (human) | IC50 | 0.0052 | 8 | 8 |
| rgfp966 | Homo sapiens (human) | IC50 | 8.5667 | 3 | 3 |
| rg2833 | Homo sapiens (human) | IC50 | 1.2800 | 1 | 1 |
| mi-192 | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
| acy-738 | Homo sapiens (human) | IC50 | 0.1280 | 2 | 2 |
| 2-((1-(3-fluorophenyl)cyclohexyl)amino)-n-hydroxypyrimidine-5-carboxamide | Homo sapiens (human) | IC50 | 2.5700 | 1 | 1 |
| 4-((1-butyl-3-phenylureido)methyl)-n-hydroxybenzamide | Homo sapiens (human) | IC50 | 5.2590 | 4 | 4 |
| 4-((1-butyl-3-phenylureido)methyl)-n-hydroxybenzamide | Homo sapiens (human) | Ki | 1.2500 | 1 | 1 |
| osimertinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| santacruzamate a | Homo sapiens (human) | IC50 | 1.4000 | 3 | 5 |
Drugs with Activation Measurements
Drugs with Other Measurements
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.ACS medicinal chemistry letters, , Oct-08, Volume: 2, Issue:1, 2010
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Histone deacetylase 3 inhibitors in learning and memory processes with special emphasis on benzamides.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.ACS medicinal chemistry letters, , Jun-13, Volume: 10, Issue:6, 2019
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Design, synthesis and biological evaluation of novel hydroxamates and 2-aminobenzamides as potent histone deacetylase inhibitors and antitumor agents.European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.ACS chemical biology, , Feb-19, Volume: 11, Issue:2, 2016
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.Bioorganic & medicinal chemistry, , 12-15, Volume: 52, 2021
Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.ACS medicinal chemistry letters, , Oct-08, Volume: 2, Issue:1, 2010
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
NO-HDAC dual inhibitors.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.ACS medicinal chemistry letters, , May-12, Volume: 13, Issue:5, 2022
CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
[no title available]Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
[no title available]European journal of medicinal chemistry, , Jun-15, Volume: 196, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.Bioorganic & medicinal chemistry letters, , May-01, Volume: 26, Issue:9, 2016
Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 96, 2015
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.The Journal of biological chemistry, , Sep-13, Volume: 288, Issue:37, 2013
Discovery of the first histone deacetylase 6/8 dual inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
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.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.Nature chemical biology, , Volume: 6, Issue:1, 2010
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
On the inhibition of histone deacetylase 8.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Recent advances in the development of polyamine analogues as antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Heterocyclic ketones as inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Trifluoromethyl ketones as inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , Dec-02, Volume: 12, Issue:23, 2002
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
[no title available],
Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.ACS medicinal chemistry letters, , Oct-08, Volume: 2, Issue:1, 2010
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.Nature chemical biology, , Volume: 6, Issue:1, 2010
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 64, 2022
Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 72, 2022
Discovery of 2,5-diphenyl-1,3,4-thiadiazole derivatives as HDAC inhibitors with DNA binding affinity.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 65, Issue:24, 2022
Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 70, 2022
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
[no title available]Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
[no title available]Journal of medicinal chemistry, , 10-28, Volume: 64, Issue:20, 2021
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFREuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.Bioorganic & medicinal chemistry, , 07-15, Volume: 42, 2021
Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.ACS medicinal chemistry letters, , Apr-08, Volume: 12, Issue:4, 2021
Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Current status in the discovery of dual BET/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 38, 2021
Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.ACS medicinal chemistry letters, , Jul-09, Volume: 11, Issue:7, 2020
Environment-sensitive fluorescent inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 30, Issue:11, 2020
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 30, Issue:22, 2020
Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
[no title available]Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.Bioorganic & medicinal chemistry, , 04-15, Volume: 27, Issue:8, 2019
[no title available]Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.ACS medicinal chemistry letters, , Jun-13, Volume: 10, Issue:6, 2019
A fluorine scan on the ZnEuropean journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.ACS medicinal chemistry letters, , Aug-08, Volume: 10, Issue:8, 2019
A novel class of anthraquinone-based HDAC6 inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.Journal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.ACS medicinal chemistry letters, , Feb-08, Volume: 9, Issue:2, 2018
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.ACS medicinal chemistry letters, , Jan-11, Volume: 9, Issue:1, 2018
LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.ACS chemical biology, , 01-20, Volume: 12, Issue:1, 2017
Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of a fluorescent probe with HDAC6 selective inhibition.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Design, synthesis and biological evaluation of quinoline derivatives as HDAC class I inhibitors.European journal of medicinal chemistry, , Jun-16, Volume: 133, 2017
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.Journal of medicinal chemistry, , 10-12, Volume: 60, Issue:19, 2017
4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 27, Issue:18, 2017
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.ACS medicinal chemistry letters, , Mar-09, Volume: 8, Issue:3, 2017
Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.Bioorganic chemistry, , Volume: 71, 2017
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.ACS chemical biology, , Feb-19, Volume: 11, Issue:2, 2016
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.ACS medicinal chemistry letters, , Mar-12, Volume: 6, Issue:3, 2015
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 96, 2015
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Design, synthesis and preliminary evaluation of α-sulfonyl γ-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 22, Issue:11, 2014
Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives.Bioorganic & medicinal chemistry, , May-01, Volume: 22, Issue:9, 2014
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Design and synthesis of novel and highly-active pan-histone deacetylase (pan-HDAC) inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 22, Issue:14, 2014
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.European journal of medicinal chemistry, , May-22, Volume: 79, 2014
Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 22, Issue:5, 2014
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.Journal of natural products, , Jan-24, Volume: 77, Issue:1, 2014
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.Chemical biology & drug design, , Volume: 82, Issue:2, 2013
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.Journal of natural products, , Nov-22, Volume: 76, Issue:11, 2013
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Investigating the selectivity of metalloenzyme inhibitors.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Development of a chimeric c-Src kinase and HDAC inhibitor.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Dual-acting histone deacetylase-topoisomerase I inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
A cyclodextrin-capped histone deacetylase inhibitor.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.The Journal of biological chemistry, , Sep-13, Volume: 288, Issue:37, 2013
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.European journal of medicinal chemistry, , Volume: 66, 2013
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 64, 2013
Discovery of the first histone deacetylase 6/8 dual inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Development of ACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 2013
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 22, Issue:17, 2012
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.ACS medicinal chemistry letters, , Jun-14, Volume: 3, Issue:6, 2012
Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 22, Issue:15, 2012
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.ACS medicinal chemistry letters, , Jul-21, Volume: 2, Issue:9, 2011
In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Synthesis and evaluation of aliphatic-chain hydroxamates capped with osthole derivatives as histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Structure-based optimization of click-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:8, 2011
Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Discovery of histone deacetylase 8 selective inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.Journal of enzyme inhibition and medicinal chemistry, , Volume: 25, Issue:1, 2010
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.Nature chemical biology, , Volume: 6, Issue:1, 2010
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
On the inhibition of histone deacetylase 8.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
Design and synthesis of novel isoxazole-based HDAC inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.Bioorganic & medicinal chemistry, , Dec-15, Volume: 18, Issue:24, 2010
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:5, 2009
Non-peptide macrocyclic histone deacetylase inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:11, 2009
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.European journal of medicinal chemistry, , Volume: 44, Issue:3, 2009
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:5, 2009
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.Bioorganic & medicinal chemistry, , May-01, Volume: 16, Issue:9, 2008
Alpha-mercaptoketone based histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 2008
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 16, Issue:15, 2006
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Heterocyclic ketones as inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Trifluoromethyl ketones as inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , Dec-02, Volume: 12, Issue:23, 2002
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
[no title available],
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.Bioorganic & medicinal chemistry, , 11-15, Volume: 50, 2021
A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from Journal of natural products, , 09-24, Volume: 84, Issue:9, 2021
Synthesis and biological evaluation of 2-quinolineacrylamides.Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018
Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available]European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 26, Issue:20, 2016
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.Journal of natural products, , Dec-24, Volume: 78, Issue:12, 2015
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Aurones as histone deacetylase inhibitors: identification of key features.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.The Journal of biological chemistry, , Nov-22, Volume: 288, Issue:47, 2013
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.The Journal of biological chemistry, , Sep-13, Volume: 288, Issue:37, 2013
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
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.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study.European journal of medicinal chemistry, , Volume: 52, 2012
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 19, Issue:15, 2011
Structure-based optimization of click-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:8, 2011
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.Nature chemical biology, , Volume: 6, Issue:1, 2010
Inside HDAC with HDAC inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:6, 2010
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
On the inhibition of histone deacetylase 8.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Synthesis and biological activity of cyclotetrapeptide analogues of the natural HDAC inhibitor FR235222.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.Bioorganic & medicinal chemistry, , Dec-15, Volume: 18, Issue:24, 2010
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.Bioorganic & medicinal chemistry, , May-01, Volume: 16, Issue:9, 2008
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Design and synthesis of a potent histone deacetylase inhibitor.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Design and synthesis of phthalimide-type histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.Bioorganic & medicinal chemistry letters, , May-17, Volume: 14, Issue:10, 2004
Subtype selective substrates for histone deacetylases.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Heterocyclic ketones as inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 30, Issue:11, 2020
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.Journal of natural products, , Dec-24, Volume: 78, Issue:12, 2015
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.Bioorganic & medicinal chemistry letters, , May-01, Volume: 26, Issue:9, 2016
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.Bioorganic & medicinal chemistry, , 12-15, Volume: 52, 2021
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities.MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.ACS medicinal chemistry letters, , Aug-14, Volume: 5, Issue:8, 2014
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.European journal of medicinal chemistry, , Volume: 60, 2013
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.ACS medicinal chemistry letters, , Jun-14, Volume: 3, Issue:6, 2012
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.Journal of natural products, , Oct-28, Volume: 74, Issue:10, 2011
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
[no title available]ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Synthesis, biological evaluation and molecular modeling studies of psammaplin A and its analogs as potent histone deacetylases inhibitors and cytotoxic agents.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 26, Issue:17, 2016
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Quantitative measurement of intracellular HDAC1/2 drug occupancy using a MedChemComm, , Apr-01, Volume: 8, Issue:4, 2017
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
On the inhibition of histone deacetylase 8.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.ACS medicinal chemistry letters, , Jun-14, Volume: 3, Issue:6, 2012
Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases.ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
On the inhibition of histone deacetylase 8.Bioorganic & medicinal chemistry, , Jun-01, Volume: 18, Issue:11, 2010
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Histone deacetylase inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.ACS medicinal chemistry letters, , Apr-08, Volume: 12, Issue:4, 2021
HIV latency reversal agents: A potential path for functional cure?European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.Bioorganic & medicinal chemistry, , 04-15, Volume: 27, Issue:8, 2019
Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.ACS medicinal chemistry letters, , Feb-08, Volume: 9, Issue:2, 2018
4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Indole-3-ethylsulfamoylphenylacrylamides: potent histone deacetylase inhibitors with anti-inflammatory activity.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.ACS chemical biology, , Feb-19, Volume: 11, Issue:2, 2016
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Discovery of the first histone deacetylase 6/8 dual inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589).Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:5, 2012
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 2021
Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.ACS chemical biology, , 01-20, Volume: 12, Issue:1, 2017
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.ACS chemical biology, , Feb-19, Volume: 11, Issue:2, 2016
Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Mutagenesis studies of the 14 Å internal cavity of histone deacetylase 1: insights toward the acetate-escape hypothesis and selective inhibitor design.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.The Journal of biological chemistry, , Sep-13, Volume: 288, Issue:37, 2013
Discovery of the first histone deacetylase 6/8 dual inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Inside HDAC with HDAC inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:6, 2010
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Histone deacetylase 3 inhibitors in learning and memory processes with special emphasis on benzamides.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.Nature chemical biology, , Volume: 2, Issue:10, 2006
Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 70, 2022
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.Nature chemical biology, , Volume: 2, Issue:10, 2006
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.European journal of medicinal chemistry, , Jul-15, Volume: 198, 2020
Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Potent and Selective Inhibitors of Histone Deacetylase-3 Containing Chiral Oxazoline Capping Groups and a N-(2-Aminophenyl)-benzamide Binding Unit.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Chemical phylogenetics of histone deacetylases.Nature chemical biology, , Volume: 6, Issue:3, 2010
SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103).Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 19, Issue:19, 2009
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
[no title available]Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.European journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo.Molecular cancer therapeutics, , Volume: 5, Issue:5, 2006
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
[no title available],
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.ACS medicinal chemistry letters, , Aug-10, Volume: 8, Issue:8, 2017
Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
[no title available],
A fluorine scan on the ZnEuropean journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 23, Issue:21, 2013
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
[no title available]Journal of medicinal chemistry, , 10-28, Volume: 64, Issue:20, 2021
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Synthesis and biological evaluation of 2-quinolineacrylamides.Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Recent advances in the discovery of potent and selective HDAC6 inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.ACS chemical biology, , 01-20, Volume: 12, Issue:1, 2017
Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of a fluorescent probe with HDAC6 selective inhibition.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.ACS medicinal chemistry letters, , Mar-09, Volume: 8, Issue:3, 2017
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 26, Issue:20, 2016
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 23, Issue:16, 2015
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.European journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
(N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Recent advances in the discovery of potent and selective HDAC6 inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Designing multi-targeted agents: An emerging anticancer drug discovery paradigm.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
[no title available]ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.Journal of natural products, , Nov-22, Volume: 76, Issue:11, 2013
Enables
This protein enables 14 target(s):
| Target | Category | Definition |
|---|
| chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| histone deacetylase activity | molecular function | Catalysis of the reaction: histone N6-acetyl-L-lysine + H2O = histone L-lysine + acetate. This reaction represents the removal of an acetyl group from a histone, a class of proteins complexed to DNA in chromatin and chromosomes. [PMID:9893272, RHEA:58196] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| heat shock protein binding | molecular function | Binding to a heat shock protein, a protein synthesized or activated in response to heat shock. [GOC:mah, GOC:vw] |
| protein lysine deacetylase activity | molecular function | Catalysis of the reaction: H2O + N6-acetyl-L-lysyl-[protein] = acetate + L-lysyl-[protein]. [PMID:27296530, RHEA:58108] |
| histone binding | molecular function | Binding to a histone, any of a group of water-soluble proteins found in association with the DNA of eukaryotic or archaeal chromosomes. They are involved in the condensation and coiling of chromosomes during cell division and have also been implicated in gene regulation and DNA replication. They may be chemically modified (methylated, acetlyated and others) to regulate gene transcription. [GOC:jl, PMID:16209651, PMID:30212449, PMID:9305837] |
| histone deacetylase binding | molecular function | Binding to histone deacetylase. [GOC:jl] |
| NF-kappaB binding | molecular function | Binding to NF-kappaB, a transcription factor for eukaryotic RNA polymerase II promoters. [GOC:ai] |
| RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
| histone decrotonylase activity | molecular function | Catalysis of the reaction: H2O + N6-(2E)-butenoyl-L-lysyl-[histone] = (2E)-2-butenoate + L-lysyl-[histone]. [PMID:28497810] |
| protein de-2-hydroxyisobutyrylase activity | molecular function | Catalysis of the reaction: H2O + N6-(2-hydroxyisobutanoyl)-L-lysyl-[protein] = 2-hydroxy-2-methylpropanoate + L-lysyl-[protein]. [PMID:29192674] |
| promoter-specific chromatin binding | molecular function | Binding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| chromosome, telomeric region | cellular component | The end of a linear chromosome, required for the integrity and maintenance of the end. A chromosome telomere usually includes a region of telomerase-encoded repeats the length of which rarely exceeds 20 bp each and that permits the formation of a telomeric loop (T-loop). The telomeric repeat region is usually preceded by a sub-telomeric region that is gene-poor but rich in repetitive elements. Some telomeres only consist of the latter part (for eg. D. melanogaster telomeres). [GOC:elh] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 6 target(s):
| Target | Category | Definition |
|---|
| NuRD complex | cellular component | An approximately 2 MDa multi-subunit complex that exhibits ATP-dependent chromatin remodeling activity in addition to histone deacetylase (HDAC) activity, and has been shown to establish transcriptional repression of a number of target genes in vertebrates, invertebrates and fungi. Amongst its subunits, the NuRD complex contains histone deacetylases, histone binding proteins and Mi-2-like proteins. [PMID:10589671, PMID:11743021, PMID:17289569] |
| Sin3-type complex | cellular component | Any of a number of evolutionarily conserved histone deacetylase complexes (HDACs) containing a core consisting of a paired amphipathic helix motif protein (e.g. Sin3p in S. cerevisiae, Pst1 in S. pombe or Sin3A in mammals) at least one class I histone deacetylase (e.g. Rpd3p in S. cerevisiae, Clr6 in S. pombe, or HDAC1 and HDAC2 in mammals), and at least one WD40 repeat protein (e.g. Ume1p in S. cerevisiae, Prw1 in S. pombe, or RbAp46 and RbAp48 in mammals). These complexes also contain a variable number of other proteins that direct histone binding, DNA binding, or add other functionality to the complex. [PMID:15565322, PMID:18292778] |
| histone deacetylase complex | cellular component | A protein complex that possesses histone deacetylase activity. [GOC:mah] |
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
| ESC/E(Z) complex | cellular component | A multimeric protein complex that can methylate lysine-27 and lysine-9 residues of histone H3. In Drosophila the core subunits of the complex include ESC, E(Z), CAF1 (NURF-55) and SU(Z)12. In mammals the core subunits of the complex include EED, EZH2, SUZ12 and RBBP4. [GOC:bf, GOC:sp, PMID:12408863, PMID:12408864, PMID:20064375] |
Involved In
This protein is involved in 52 target(s):
| Target | Category | Definition |
|---|
| negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| response to amphetamine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef] |
| cardiac muscle hypertrophy | biological process | The enlargement or overgrowth of all or part of the heart muscle due to an increase in size of cardiac muscle cells without cell division. [GOC:mtg_heart] |
| chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| epidermal cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of an epidermal cell, any of the cells making up the epidermis. [GOC:dph, GOC:go_curators, GOC:mtg_sensu, GOC:sdb_2009, GOC:tb] |
| positive regulation of epithelial to mesenchymal transition | biological process | Any process that increases the rate, frequency, or extent of epithelial to mesenchymal transition. Epithelial to mesenchymal transition is where an epithelial cell loses apical/basolateral polarity, severs intercellular adhesive junctions, degrades basement membrane components and becomes a migratory mesenchymal cell. [GOC:BHF, GOC:dph, GOC:tb] |
| negative regulation of transcription by competitive promoter binding | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of DNA-dependent transcription using a mechanism that involves direct competition for interaction with a promoter binding site. [GOC:tb] |
| negative regulation of neuron projection development | biological process | Any process that decreases the rate, frequency or extent of neuron projection development. Neuron projection development is the process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:dph, GOC:tb] |
| dendrite development | biological process | The process whose specific outcome is the progression of the dendrite over time, from its formation to the mature structure. [GOC:aruk, GOC:bc, GOC:jl, ISBN:0198506732, PMID:22683681] |
| negative regulation of cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell migration. [GOC:go_curators] |
| negative regulation of transforming growth factor beta receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of any TGF-beta receptor signaling pathway. [GOC:mah] |
| response to caffeine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a caffeine stimulus. Caffeine is an alkaloid found in numerous plant species, where it acts as a natural pesticide that paralyzes and kills certain insects feeding upon them. [GOC:ef, GOC:mah] |
| heterochromatin formation | biological process | An epigenetic gene silencing mechanism in which chromatin is compacted into heterochromatin, resulting in a chromatin conformation refractory to transcription. This process starts with heterochromatin nucleation, its spreading, and ends with heterochromatin boundary formation. [PMID:25192661, PMID:33827924] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| positive regulation of interleukin-1 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-1 production. [GOC:mah] |
| positive regulation of tumor necrosis factor production | biological process | Any process that activates or increases the frequency, rate or extent of tumor necrosis factor production. [GO_REF:0000058, GOC:TermGenie, PMID:10891884, PMID:15560120] |
| circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
| positive regulation of collagen biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of collagen, any of a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. [GOC:mah] |
| cellular response to heat | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a heat stimulus, a temperature stimulus above the optimal temperature for that organism. [GOC:mah] |
| response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
| protein modification process | biological process | The covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl] |
| response to cocaine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| odontogenesis of dentin-containing tooth | biological process | The process whose specific outcome is the progression of a dentin-containing tooth over time, from its formation to the mature structure. A dentin-containing tooth is a hard, bony organ borne on the jaw or other bone of a vertebrate, and is composed mainly of dentin, a dense calcified substance, covered by a layer of enamel. [GOC:cjm, GOC:mah, GOC:mtg_sensu, PMID:10333884, PMID:15355794] |
| positive regulation of tyrosine phosphorylation of STAT protein | biological process | Any process that activates or increases the frequency, rate or extent of the introduction of a phosphate group to a tyrosine residue of a STAT (Signal Transducer and Activator of Transcription) protein. [GOC:jl, PMID:11426647] |
| regulation of cell fate specification | biological process | Any process that mediates the adoption of a specific fate by a cell. [GOC:go_curators] |
| embryonic digit morphogenesis | biological process | The process, occurring in the embryo, by which the anatomical structures of the digit are generated and organized. A digit is one of the terminal divisions of an appendage, such as a finger or toe. [GOC:bf, GOC:jl, UBERON:0002544] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| negative regulation of DNA-binding transcription factor activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:jl] |
| negative regulation of MHC class II biosynthetic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of MHC class II. [GOC:go_curators] |
| positive regulation of proteolysis | biological process | Any process that activates or increases the frequency, rate or extent of the hydrolysis of a peptide bond or bonds within a protein. [GOC:go_curators] |
| negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| behavioral response to ethanol | biological process | Any process that results in a change in the behavior of an organism as a result of an ethanol stimulus. [GOC:jid] |
| positive regulation of oligodendrocyte differentiation | biological process | Any process that activates or increases the frequency, rate or extent of oligodendrocyte differentiation. [GOC:vp, PMID:15139015] |
| response to hyperoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating increased oxygen tension. [GOC:kmv] |
| hair follicle placode formation | biological process | The developmental process in which a hair placode forms. An hair follicle placode is a thickening of the ectoderm that will give rise to the hair follicle bud. [GOC:dph, GOC:sdb_2009, GOC:tb] |
| negative regulation of dendritic spine development | biological process | Any process that decreases the rate, frequency, or extent of dendritic spine development, the process whose specific outcome is the progression of the dendritic spine over time, from its formation to the mature structure. [GOC:dph] |
| eyelid development in camera-type eye | biological process | The progression of the eyelid in a camera-type eye from its formation to the mature state. The eyelid is a membranous cover that helps protect and lubricate the eye. [GOC:dph, GOC:yaf] |
| fungiform papilla formation | biological process | The developmental process pertaining to the initial formation of a spongiform papilla from unspecified parts. The fungiform papilla is a mushroom-shaped papilla of the tongue. [GOC:dph] |
| cellular response to hydrogen peroxide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hydrogen peroxide (H2O2) stimulus. [CHEBI:16240, GOC:mah] |
| cellular response to retinoic acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a retinoic acid stimulus. [GOC:mah] |
| cellular response to transforming growth factor beta stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a transforming growth factor beta stimulus. [GOC:ecd, PMID:15451575] |
| positive regulation of male mating behavior | biological process | Any process that activates or increases the frequency, rate or extent of male mating behavior. [GOC:TermGenie, PMID:24089208] |
| negative regulation of stem cell population maintenance | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of stem cell population maintenance. [GOC:hjd, GOC:TermGenie, PMID:22969033] |
| positive regulation of stem cell population maintenance | biological process | Any process that activates or increases the frequency, rate or extent of stem cell population maintenance. [GOC:hjd, GOC:TermGenie, PMID:22969033] |
| cellular response to dopamine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a dopamine stimulus. [GO_REF:0000071, GOC:mr, GOC:TermGenie, PMID:11118945] |
| response to amyloid-beta | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
| regulation of stem cell differentiation | biological process | Any process that modulates the frequency, rate or extent of stem cell differentiation. [GOC:obol] |
| negative regulation of peptidyl-lysine acetylation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of peptidyl-lysine acetylation. [GOC:obol] |