Target Validation Information
Target ID T65755
Target Name Histone deacetylase
Target Type
Successful
Drug Potency against Target ITF2357 Drug Info IC50 = 7.5~16 nM [552589]
Sodium butyrate Drug Info IC50 = 1000 nM [552717]
Chlamydocin Drug Info IC50 = 1.3 nM [552324]
PDX-101 Drug Info IC50 = 27 nM [536272]
M-carboxycinnamic acid bishydroxamide Drug Info IC50 = 1000 nM [536272]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [527439]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [527439]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 7700 nM [527980]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [527500]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info IC50 = 340 nM [527439]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [527691]
ST-5732 Drug Info IC50 = 18000 nM [530067]
AN-9 Drug Info IC50 = 1000 nM [536272]
2,2-bis(4-chlorophenyl)-N-hydroxyacetamide Drug Info IC50 = 1400 nM [530327]
N-(5-Hydroxycarbamoyl-pentyl)-4-methoxy-benzamide Drug Info IC50 = 140 nM [525643]
NVP-LAQ824 Drug Info IC50 = 32 nM [535748]
PDX-101 Drug Info Pki = 8.5 [552854]
SNDX-275 Drug Info IC50 = 300 nM [536272]
NVP-LAQ824 Drug Info IC50 = 1 nM [536272]
Tacedinaline Drug Info Ki = 550 nM [530700]
Pyroxamide Drug Info IC50 = 1 uM [536272]
Panobinostat Drug Info IC50 = 1 nM [536272]
AR-42 Drug Info IC50 = 16 nM [552511]
SK-7068 Drug Info IC50 = 1 nM [536272]
Valproic Acid Drug Info IC50 = 1mM [536272]
N-hydroxy-9,10-dihydroanthracene-9-carboxamide Drug Info IC50 = 1460 nM [530327]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [527691]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [526922]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1750 nM [530704]
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 56 nM [530704]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 15500 nM [527980]
N-hydroxy-2,2-diphenylpropanamide Drug Info IC50 = 1200 nM [530327]
N-hydroxy-2,2-diphenylacetamide Drug Info IC50 = 140 nM [530327]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [527500]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide Drug Info IC50 = 137 nM [530704]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 2263 nM [530704]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1346 nM [530704]
N-Hydroxy-N'-(2-methylphenyl)octanediamide Drug Info IC50 = 1348 nM [530704]
2,2-bis(3-fluorophenyl)-N-hydroxyacetamide Drug Info IC50 = 90 nM [530327]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 4989 nM [530704]
N-Hydroxy-N'-(3-methylphenyl)octanediamide Drug Info IC50 = 58 nM [530704]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [527691]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [526871]
SB-623 Drug Info IC50 < 10 nM [536272]
ST-2986 Drug Info IC50 = 5480 nM [530016]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [526266]
8-Oxo-8-phenyl-octanoic acid Drug Info IC50 = 270 nM [526266]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 9400 nM [527980]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [527439]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info IC50 = 3600 nM [526922]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 110 nM [527691]
MGCD-0103 Drug Info IC50 = 100 nM [552548]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [526922]
Phenylbutyrate Drug Info IC50 = 44 nM [527691]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [526871]
Scriptaid Drug Info pKi = 6.65 [552671]
Romidepsin Drug Info IC50 = 36~47 nM [536363]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [529333]
N-(4-aminobiphenyl-3-yl)nicotinamide Drug Info IC50 = 11350 nM [529767]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [527691]
PSAMMAPLIN A Drug Info IC50 = 4 nM [526878]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [527439]
4-Phenylbutyrohydroxamic acid Drug Info Ki = 16000 nM [530700]
ST-2987 Drug Info IC50 = 790 nM [530016]
N-(2-aminophenyl)nicotinamide Drug Info IC50 = 3640 nM [529767]
N-(2-aminophenyl)-4-methoxybenzamide Drug Info IC50 = 1400 nM [529104]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [527439]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [527691]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Drug Info IC50 = 7300 nM [529767]
8-Mercapto-octanoic acid phenylamide Drug Info IC50 = 1500 nM [527439]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [527691]
N-hydroxy-9H-xanthene-9-carboxamide Drug Info IC50 = 110 nM [530327]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [527439]
2,2-bis(4-fluorophenyl)-N-hydroxyacetamide Drug Info IC50 = 280 nM [530327]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [526266]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info IC50 = 6700 nM [526878]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info IC50 = 568 nM [526266]
Octanedioic acid hydroxyamide pyridin-4-ylamide Drug Info IC50 = 306 nM [526266]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 1100 nM [526871]
Tacedinaline Drug Info IC50 = 1000 nM [536272]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [526871]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Drug Info IC50 = 2600 nM [526878]
ST-3050 Drug Info IC50 = 3060 nM [530016]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1556 nM [526266]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1100 nM [530704]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [527439]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [527691]
Octanedioic acid hydroxyamide pyridin-2-ylamide Drug Info IC50 = 248 nM [526266]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info IC50 = 2580 nM [527056]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [526871]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide Drug Info IC50 = 7 nM [530106]
SB-639 Drug Info IC50 < 10 nM [552485]
N-(5-Hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 900 nM [525643]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [527058]
SK-7041 Drug Info IC50 = 1 nM [536272]
Octanedioic acid bis-hydroxyamide Drug Info Ki = 9500 nM [530700]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [527439]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 35 nM [530704]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [527439]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 30 nM [530704]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 240 nM [530704]
N-Hydroxy-N'-(4-methylphenyl)octanediamide Drug Info IC50 = 114 nM [530704]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [529333]
HC-Toxin Drug Info IC50 = 30 nM [552451]
Depudecin Drug Info IC50 = 1000 nM [536272]
Oxamflatin Drug Info IC50 = 1000 nM [536272]
Action against Disease Model ITF2357 The clonogenic activity of JAK2V617F mutated cells was inhibited by low concentrations of ITF2357 (IC50 0.001-0.01 mu M) [552763] Drug Info
Valproic Acid Valproic acid is widely used to treat epilepsy and bipolar disorder and is also a potent teratogen, but its mechanisms of action in any of these settings are unknown. We report that valproic acid activates Wntdependent gene expression, similar to lithi uM, the mainstay of therapy for bipolar disorder. Valproic acid, however, acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC(50) for HDAC1 = 0.4 mm). At therapeutic levels, valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells. Valproic acid, like trichostatin A, also activates transcription from diverse exogenous and endogenous promoters. Furthermore, valproic acid and trichostatin A have remarkably similar teratogenic effects in vertebrate embryos, while non-teratogenic analogues of valproic acid do not inhibit histone deacetylase and do not activate transcription. Based on these observations, we propose that inhibition of histone deacetylase provides a mechanism for valproic acid-induced birth defects and could also explain the efficacy of valproic acid in the treatment of bipolar disorder. [552262] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Recent studies have revealed key roles for histone deacetylases (HDACs) in the control of pathological cardiac growth. Class II HDACs associate with the MEF2 transcription factor, and other factors, to maintain normal cardiac size and function. Stress signals lead to the phosphorylation of class II HDACs and their export from the nucleus to the cytoplasm, with consequent activation of genes involved in cardiac growth. HDAC knockout mice are hypersensitive to stress signalling and develop massively enlarged hearts in response to various pathological stress stimuli due to an inability to counteract pathological signalling to MEF2. Strategies for normalizing gene expression in the failing heart by regulating HDAC phosphorylation and function represent potentially powerful therapeutic approaches. [552589]
References
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Ref 552717Scriptaid and suberoylanilide hydroxamic acid are histone deacetylase inhibitors with potent anti-Toxoplasma gondii activity in vitro. J Parasitol. 2007 Jun;93(3):694-700.
Ref 552324Inhibition of histone deacetylases by chlamydocin induces apoptosis and proteasome-mediated degradation of survivin. J Pharmacol Exp Ther. 2003 Feb;304(2):881-8.
Ref 552763The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F). Leukemia. 2008 Apr;22(4):740-7. Epub 2007 Dec 13.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527980J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
Ref 527500Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 530067Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3. Epub 2009 Mar 26.Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.
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Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 525643J Med Chem. 1999 Nov 4;42(22):4669-79.Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.
Ref 535748NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. Epub 2003 Jun 19.
Ref 5528545-HT1A receptor, an old target for new therapeutic agents. Curr Top Med Chem. 2008;8(12):1024-34.
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Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 530700Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 552511Novel HDAC inhibitors with radiosensitizing properties. Radiat Res. 2005 May;163(5):488-93.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 526922J Med Chem. 2004 Jan 15;47(2):467-74.Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 527980J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 527500Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 526871Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
Ref 552262Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 2001 Sep 28;276(39):36734-41. Epub 2001 Jul 25.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 530016Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. Epub 2009 Feb 12.N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC)inhibitors.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 527980J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 526922J Med Chem. 2004 Jan 15;47(2):467-74.Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 552548Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). Curr Top Med Chem. 2005;5(9):869-84.
Ref 526922J Med Chem. 2004 Jan 15;47(2):467-74.Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 526871Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
Ref 552671Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes. Curr Top Med Chem. 2007;7(2):163-86.
Ref 536363HDACs, histone deacetylation and gene transcription: from molecular biology to cancer therapeutics. Cell Res. 2007 Mar;17(3):195-211.
Ref 529333Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7. Epub 2008 Feb 8.New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity.
Ref 529767Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 526878J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 530700Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases.
Ref 530016Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. Epub 2009 Feb 12.N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC)inhibitors.
Ref 529767Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Ref 529104J Med Chem. 2007 Nov 15;50(23):5543-6. Epub 2007 Oct 17.Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 529767Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 530327Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. Epub 2009 Aug 7.Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 526878J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 526871Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 526871Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
Ref 526878J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors.
Ref 530016Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. Epub 2009 Feb 12.N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC)inhibitors.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 527691J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Ref 526266J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
Ref 527056Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81.Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.
Ref 526871Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
Ref 530106Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6. Epub 2009 Apr 20.Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
Ref 552485Histone deacetylase inhibitors. Eur J Med Chem. 2005 Jan;40(1):1-13.
Ref 525643J Med Chem. 1999 Nov 4;42(22):4669-79.Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.
Ref 527058Bioorg Med Chem Lett. 2004 May 17;14(10):2617-20.Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 530700Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
Ref 527439J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.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.
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