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Polyamine deacetylase HDAC10
A polyamine deacetylase HDAC10 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q969S8]
Synonyms
EC 3.5.1.48;
EC 3.5.1.62;
Histone deacetylase 10;
HD10
Research
Bioassay Publications (239)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.42) | 18.2507 |
| 2000's | 54 (22.59) | 29.6817 |
| 2010's | 140 (58.58) | 24.3611 |
| 2020's | 44 (18.41) | 2.80 |
Compounds (76)
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) | Ki | 136.0000 | 1 | 1 |
| celecoxib | Homo sapiens (human) | IC50 | 1.6370 | 1 | 1 |
| ci 994 | Homo sapiens (human) | IC50 | 3.0525 | 4 | 4 |
| clioquinol | Homo sapiens (human) | IC50 | 71.0857 | 1 | 14 |
| valproic acid | Homo sapiens (human) | IC50 | 4,117.5000 | 2 | 2 |
| valproic acid | Homo sapiens (human) | Ki | 564.0000 | 1 | 1 |
| fluconazole | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | Homo sapiens (human) | IC50 | 0.8330 | 2 | 2 |
| entinostat | Homo sapiens (human) | IC50 | 6.7189 | 25 | 34 |
| 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 |
| scriptaid | Homo sapiens (human) | IC50 | 0.4300 | 2 | 2 |
| 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 | 1.5771 | 190 | 200 |
| vorinostat | Homo sapiens (human) | Ki | 0.6550 | 4 | 4 |
| acetylcysteine | Homo sapiens (human) | IC50 | 3,160.0000 | 1 | 1 |
| camptothecin | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| osajin | Homo sapiens (human) | IC50 | 6.5300 | 1 | 1 |
| lapatinib | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| n-hydroxy-2,2-diphenylacetamide | Homo sapiens (human) | IC50 | 27.3000 | 2 | 2 |
| 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 | 0.3266 | 47 | 67 |
| trichostatin a | Homo sapiens (human) | Ki | 0.1719 | 3 | 3 |
| 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 |
| 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 |
| ex 527 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sodium butyrate | Homo sapiens (human) | IC50 | 360.0000 | 3 | 3 |
| 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 | 18.5000 | 1 | 1 |
| romidepsin | Homo sapiens (human) | IC50 | 0.0646 | 6 | 6 |
| 3',4'-dihydroxyaurone | Homo sapiens (human) | IC50 | 8.2000 | 1 | 1 |
| psammaplin a | Homo sapiens (human) | IC50 | 0.0270 | 2 | 2 |
| trichostatin c | Homo sapiens (human) | IC50 | 23.6300 | 1 | 1 |
| laq824 | Homo sapiens (human) | IC50 | 0.0309 | 5 | 5 |
| indigo carmine | Homo sapiens (human) | IC50 | 321.6200 | 2 | 2 |
| tanespimycin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| tubacin | Homo sapiens (human) | IC50 | 3.7100 | 4 | 4 |
| tubacin | Homo sapiens (human) | Ki | 0.3737 | 1 | 1 |
| (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 | 0.0140 | 7 | 7 |
| belinostat | Homo sapiens (human) | IC50 | 0.0357 | 5 | 5 |
| belinostat | Homo sapiens (human) | Ki | 0.0590 | 1 | 1 |
| sk-7041 | Homo sapiens (human) | IC50 | 0.1720 | 1 | 1 |
| panobinostat | Homo sapiens (human) | IC50 | 0.0070 | 10 | 10 |
| panobinostat | Homo sapiens (human) | Ki | 0.0180 | 2 | 2 |
| hdac-42 | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| 4-acetamido-N-(2-amino-5-thiophen-2-ylphenyl)benzamide | Homo sapiens (human) | IC50 | 6.1642 | 3 | 12 |
| n1-(2-aminophenyl)-n7-phenylheptanediamide | Homo sapiens (human) | IC50 | 78.0000 | 1 | 1 |
| bml 210 | Homo sapiens (human) | IC50 | 91.4000 | 5 | 5 |
| n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide | Homo sapiens (human) | IC50 | 0.8145 | 4 | 4 |
| givinostat | Homo sapiens (human) | IC50 | 0.3310 | 1 | 1 |
| methyl 3,5-di-o-caffeoyl quinate | Homo sapiens (human) | IC50 | 6.2900 | 2 | 2 |
| r 306465 | Homo sapiens (human) | IC50 | 0.0052 | 2 | 2 |
| quisinostat | Homo sapiens (human) | IC50 | 0.0082 | 7 | 7 |
| quisinostat | Homo sapiens (human) | Ki | 0.0022 | 2 | 2 |
| abexinostat | Homo sapiens (human) | IC50 | 0.0213 | 3 | 3 |
| abexinostat | Homo sapiens (human) | Ki | 0.0499 | 3 | 8 |
| chidamide | Homo sapiens (human) | IC50 | 1.9255 | 4 | 3 |
| hc toxin | Homo sapiens (human) | IC50 | 0.4300 | 1 | 1 |
| azumamide e | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| cnf 2024 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| pci 34051 | Homo sapiens (human) | IC50 | 29.4015 | 7 | 7 |
| cudc 101 | Homo sapiens (human) | IC50 | 0.1815 | 9 | 6 |
| largazole | Homo sapiens (human) | IC50 | 2.2100 | 1 | 1 |
| N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]-oxomethyl]-5-isoxazolyl]phenyl]carbamic acid tert-butyl ester | Homo sapiens (human) | IC50 | 0.3128 | 4 | 4 |
| 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 | 23.4558 | 13 | 13 |
| pracinostat | Homo sapiens (human) | IC50 | 1.2388 | 4 | 4 |
| pracinostat | Homo sapiens (human) | Ki | 0.0230 | 1 | 1 |
| acy-1215 | Homo sapiens (human) | IC50 | 2.9762 | 4 | 4 |
| cudc-907 | Homo sapiens (human) | IC50 | 0.0036 | 7 | 7 |
| 4-((1-butyl-3-phenylureido)methyl)-n-hydroxybenzamide | Homo sapiens (human) | IC50 | 3.9353 | 4 | 4 |
| osimertinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| santacruzamate a | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bufexamac | Homo sapiens (human) | Kd | 12.3000 | 1 | 1 |
| ci 994 | Homo sapiens (human) | EC50 | 3.8100 | 1 | 1 |
| entinostat | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| vorinostat | Homo sapiens (human) | EC50 | 3.4300 | 6 | 6 |
| belinostat | Homo sapiens (human) | EC50 | 0.0300 | 1 | 1 |
| kd 5170 | Homo sapiens (human) | EC50 | 0.0450 | 1 | 1 |
Drugs with Other Measurements
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
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
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
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
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
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]European journal of medicinal chemistry, , Jun-15, Volume: 196, 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
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
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
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
Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 53, 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
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
Recent advances in the development of polyamine analogues as antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
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
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
(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
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
[no title available],
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 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
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 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
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 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
Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 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
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
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
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
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
Environment-sensitive fluorescent inhibitors of histone deacetylase.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 30, Issue:11, 2020
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 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
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
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
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
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
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
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
A novel class of anthraquinone-based HDAC6 inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 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
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
[no title available]Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 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 Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.ACS medicinal chemistry letters, , Aug-08, Volume: 10, Issue:8, 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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
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
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
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
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
Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 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
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
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
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
Development of ACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 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
Development of a chimeric c-Src kinase and HDAC inhibitor.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 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
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
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
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
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 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
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
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
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
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
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
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
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
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 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
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 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
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
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
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
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
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
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
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:5, 2009
Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.European journal of medicinal chemistry, , Volume: 44, Issue:3, 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
Alpha-mercaptoketone based histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 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
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
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
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
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
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
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 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
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from Journal of natural products, , 09-24, Volume: 84, Issue:9, 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
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
1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
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
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
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
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
Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.European journal of medicinal chemistry, , May-22, Volume: 79, 2014
Aurones as histone deacetylase inhibitors: identification of key features.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
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
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
Structure-based optimization of click-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:8, 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
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
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Synthesis and biological activity of cyclotetrapeptide analogues of the natural HDAC inhibitor FR235222.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 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
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
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
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
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
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
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
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
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 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
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
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
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
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
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
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
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
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
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
Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases.ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
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
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.Bioorganic & medicinal chemistry, , 04-15, Volume: 27, Issue:8, 2019
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.ACS medicinal chemistry letters, , Feb-08, Volume: 9, Issue:2, 2018
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
Histone deacetylase inhibitors: from bench to clinic.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
[no title available]Journal of medicinal chemistry, , 01-13, Volume: 65, Issue:1, 2022
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
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 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
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
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
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
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
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
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 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
Indole: A privileged scaffold for the design of anti-cancer agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 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
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
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
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
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 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
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
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
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
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
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
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],
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 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
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
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
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
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],
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
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
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
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
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
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 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
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
Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Discovery of a fluorescent probe with HDAC6 selective inhibition.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
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
Development and therapeutic implications of selective histone deacetylase 6 inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 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 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
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
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
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
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
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 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
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
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
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|
| 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] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| deacetylase activity | molecular function | Catalysis of the hydrolysis of an acetyl group or groups from a substrate molecule. [GOC:jl] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| 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 deacetylase binding | molecular function | Binding to histone deacetylase. [GOC:jl] |
| acetylputrescine deacetylase activity | molecular function | Catalysis of the reaction: N-acetylputrescine + H2O = acetate + putrescine. [EC:3.5.1.62, RHEA:23412] |
| acetylspermidine deacetylase activity | molecular function | Catalysis of the reaction: N(8)-acetylspermidine + H2O = acetate + spermidine. [EC:3.5.1.48, RHEA:23928] |
Located In
This protein is located in 5 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] |
| 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] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| histone deacetylase complex | cellular component | A protein complex that possesses histone deacetylase activity. [GOC:mah] |
Involved In
This protein is involved in 11 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] |
| DNA repair | biological process | The process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486] |
| chromatin organization | biological process | The assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| macroautophagy | biological process | The autophagic process that proceeds via the formation of an autophagosome. [PMID:24366339] |
| positive regulation of mismatch repair | biological process | Any process that activates or increases the frequency, rate or extent of mismatch repair. [GOC:vk] |
| homologous recombination | biological process | A DNA recombination process that results in the exchange of an equal amount of genetic material between highly homologous DNA molecules. [GOC:mah, PMID:11139492, PMID:17304215] |
| 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] |
| polyamine deacetylation | biological process | The modification of acetylpolyamine by the removal of acetyl groups. [PMID:28516954] |
| spermidine deacetylation | biological process | The modification of acetylspermadine by the removal of acetyl groups. [PMID:28516954] |
| epigenetic regulation of gene expression | biological process | A process that modulates the frequency, rate or extent of gene expression through chromatin remodeling either by modifying higher order chromatin fiber structure, nucleosomal histones, or cytosine methylation of DNA. Once established, this regulation may be maintained over many cell divisions. It can also be heritable in the absence of the instigating signal. [PMID:10521337, PMID:11498582, PMID:22243696, PMID:34414474] |