(E)-3-(3-Bromo-4-hydroxyphenyl)-N-(3-(hydroxyamino)-3-oxopropyl)-2-(hydroxyimino)propanamide

ID: ALA2047684

Max Phase: Preclinical

Molecular Formula: C12H14BrN3O5

Molecular Weight: 360.16

Molecule Type: Small molecule

Names and Identifiers

Canonical SMILES:  O=C(CCNC(=O)/C(Cc1ccc(O)c(Br)c1)=N/O)NO

Standard InChI:  InChI=1S/C12H14BrN3O5/c13-8-5-7(1-2-10(8)17)6-9(15-20)12(19)14-4-3-11(18)16-21/h1-2,5,17,20-21H,3-4,6H2,(H,14,19)(H,16,18)/b15-9+

Standard InChI Key:  OFVVEEGKXCCFDK-OQLLNIDSSA-N

Molfile:  

     RDKit          2D

 21 21  0  0  0  0  0  0  0  0999 V2000
   26.2941   -1.4590    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   25.5748   -1.0566    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   24.8613   -1.4750    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   26.3039   -2.2840    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   27.0034   -1.0406    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   25.5649   -0.2316    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   24.8456    0.1749    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   27.7226   -1.4388    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   28.4320   -1.0204    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   29.1513   -1.4269    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   29.1613   -2.2519    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   29.8607   -1.0085    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   30.5730   -1.4189    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   24.1462   -1.0726    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   23.4368   -1.4911    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   22.7175   -1.0887    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   22.7077   -0.2637    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   23.4170    0.1589    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   24.1404   -0.2477    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   21.9884    0.1428    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   22.0082   -1.5071    0.0000 Br  0  0  0  0  0  0  0  0  0  0  0  0
  1  2  1  0
  2  3  1  0
  1  4  2  0
  1  5  1  0
  6  7  1  0
  2  6  2  0
  8  9  1  0
  9 10  1  0
 10 11  2  0
 12 13  1  0
 10 12  1  0
  5  8  1  0
 14 15  1  0
 15 16  2  0
 16 17  1  0
 17 18  2  0
 18 19  1  0
 14 19  2  0
 17 20  1  0
 16 21  1  0
  3 14  1  0
M  END

Alternative Forms

1. Parent:

   

   ALA2047684

   ---

Molecule Features

Natural Product: No

Oral: No

Chemical Probe: No

Parenteral: No

Molecule Type: Small molecule

Topical: No

First In Class: No

Black Box: No

Chirality: No

Availability: No

Prodrug: No

Calculated Properties

Molecular Weight: 360.16

Molecular Weight (Monoisotopic): 359.0117

AlogP: 0.54

#Rotatable Bonds: 6

Polar Surface Area: 131.25

Molecular Species: NEUTRAL

HBA: 6

HBD: 5

#RO5 Violations: ┄

HBA (Lipinski): 8

HBD (Lipinski): 5

#RO5 Violations (Lipinski): ┄

CX Acidic pKa: 7.93

CX Basic pKa: ┄

CX LogP: 0.70

CX LogD: 0.58

Aromatic Rings: 1

Heavy Atoms: 21

QED Weighted: 0.22

Np Likeness Score: 0.26

References

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27. Santo, Loredana L and 18 more authors.  2012-03-15  Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.  [PMID:22262760]

28. Fredenhagen, Andreas A and 9 more authors.  2012-05  Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589).  [PMID:22344701]

29. Lai, Mei-Jung and 11 more authors.  2012-04-26  Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.  [PMID:22439863]

30. Bergman, Joel A JA and 5 more authors.  2012-11-26  Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.  [PMID:23009203]

31. Wong, Jason C JC and 38 more authors.  2012-10-25  Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.  [PMID:23061376]

32. Choi, Sun Ea and Pflum, Mary Kay H.  2012-12-01  The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.  [PMID:23089527]

33. Suzuki, Takayoshi T and 13 more authors.  2012-11-26  Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries.  [PMID:23116147]

34. Zhang, Yingjie and 5 more authors.  2013-02-14  Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with Indole-Containing Cap Group.  [PMID:23493449]

35. Patil, Vishal; Sodji, Quaovi H; Kornacki, James R; Mrksich, Milan and Oyelere, Adegboyega K.  2013-05-09  3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.  [PMID:23547652]

36. Guerrant, William and 5 more authors.  2013-06-01  Dual-acting histone deacetylase-topoisomerase I inhibitors.  [PMID:23622981]

37. Kalin, Jay H JH and Bergman, Joel A JA.  2013-08-22  Development and therapeutic implications of selective histone deacetylase 6 inhibitors.  [PMID:23627282]

38. Gryder, Berkley E BE and 9 more authors.  2013-07-25  Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.  [PMID:23786452]

39. Yu, Chao-Wu CW, Chang, Pei-Teh PT, Hsin, Ling-Wei LW and Chern, Ji-Wang JW.  2013-09-12  Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.  [PMID:23905680]

40. Wang, Cheng; Flemming, Creston J and Cheng, Yi-Qiang.  2012-08-01  Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264.  [PMID:23997923]

41. Ko, Kristin S; Steffey, Michael E; Brandvold, Kristoffer R and Soellner, Matthew B.  2013-08-08  Development of a chimeric c-Src kinase and HDAC inhibitor.  [PMID:24015327]

42. Seo, Young Jun and 8 more authors.  2013-12-15  Radionuclide labeling and evaluation of candidate radioligands for PET imaging of histone deacetylase in the brain.  [PMID:24210501]

43. Bürli, Roland W RW and 29 more authors.  2013-12-27  Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.  [PMID:24261862]

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46. Li, Xiaoyang and 8 more authors.  2014-04-24  Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.  [PMID:24694055]

47. Cincinelli, Raffaella R and 6 more authors.  2014-05-22  Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.  [PMID:24742384]

48. Lee, Hsueh-Yun HY and 13 more authors.  2014-05-22  Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells.  [PMID:24766560]

49. Valente, Sergio S and 12 more authors.  2014-07-24  1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.  [PMID:24972008]

50. Tang, Guozhi G and 15 more authors.  2014-10-09  Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors.  [PMID:25238284]

51. Sodji, Quaovi H QH, Kornacki, James R JR, McDonald, John F JF, Mrksich, Milan M and Oyelere, Adegboyega K AK.  2015  Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.  [PMID:25899338]

52. Duan, Wenwen and 8 more authors.  2015-05-28  Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor.  [PMID:25906087]

53. Daniel, Kevin B and 6 more authors.  2015-06-11  Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release.  [PMID:25974739]

54. Tang, Chu and 7 more authors.  2015-06-11  Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.  [PMID:25993269]

55. Clausen, Dane J and 5 more authors.  2015-08-01  Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.  [PMID:26054247]

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57. Yao, Yiwu Y and 7 more authors.  2015-10-08  Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.  [PMID:26331334]

58. Yang, Zhuang Z and 14 more authors.  2016-02-25  Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.  [PMID:26443078]

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63. Cincinelli, Raffaella R and 10 more authors.  2016-04-13  Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.  [PMID:26890116]

64. Heimburg, Tino T and 14 more authors.  2016-03-24  Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.  [PMID:26937828]

65. Yoo, Jakyung J and 10 more authors.  2016-06-30  Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.  [PMID:27060764]

66. Ellis, Jonathan D JD and 8 more authors.  2016-08  Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation.  [PMID:27222932]

67. Wagner, Florence F FF and 17 more authors.  2016-09-15  Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.  [PMID:27377864]

68. Rabal, Obdulia O and 15 more authors.  2016-10-13  Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.  [PMID:27606546]

69. Zwick, Vincent V and 8 more authors.  2016-10-15  Synthesis of a selective HDAC6 inhibitor active in neuroblasts.  [PMID:27650925]

70. Jadhavar, Pradeep S PS and 20 more authors.  2016-11-01  Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.  [PMID:27717544]

71. McClure, Jesse J and 5 more authors.  2016-11-10  Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.  [PMID:27754681]

72. Almaliti, Jehad and 7 more authors.  2016-12-08  Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue.  [PMID:27809521]

73. Lee, Hsueh-Yun HY and 12 more authors.  2017-01-05  3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.  [PMID:27886544]

74. Huang, Pengyu P and 7 more authors.  2017-01-10  Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.  [PMID:27926524]

75. Raji, Idris and 9 more authors.  2017-02-01  Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.  [PMID:28057407]

76. Raji, Idris I, Ahluwalia, Kabir K and Oyelere, Adegboyega K AK.  2017-02-15  Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.  [PMID:28131715]

77. Negmeldin, Ahmed T AT, Padige, Geetha G, Bieliauskas, Anton V AV and Pflum, Mary Kay H MK.  2017-03-09  Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.  [PMID:28337317]

78. Li, Xiaoyang X and 12 more authors.  2017-07-07  Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.  [PMID:28415009]

79. Kim, Bumki and 7 more authors.  2017-06-15  Synthesis and biological evaluation of largazole zinc-binding group analogs.  [PMID:28416100]

80. Yuan, Zigao Z and 9 more authors.  2017-07-07  Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.  [PMID:28419930]

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82. Gao, Shuai and 8 more authors.  2017-06-15  Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.  [PMID:28511906]

83. Stenzel, Katharina K and 13 more authors.  2017-07-13  Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.  [PMID:28581289]

84. Yuan, Zigao Z and 9 more authors.  2017-08-01  Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.  [PMID:28601509]

85. Negmeldin, Ahmed T and Pflum, Mary Kay H.  2017-08-01  The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.  [PMID:28648461]

86. Lai, Jiun-I JI and 7 more authors.  2017-08-01  Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.  [PMID:28648462]

87. Shao, Mingfeng M and 10 more authors.  2017-09-01  Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.  [PMID:28765013]

88. Hsieh, Hao-Yu HY and 5 more authors.  2017-11-10  Targeting breast cancer stem cells by novel HDAC3-selective inhibitors.  [PMID:28923385]

89. Duan, Ying-Chao YC and 9 more authors.  2017-11-10  Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.  [PMID:28987602]

90. Tavares, Maurício T MT and 7 more authors.  2017-10-12  Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.  [PMID:29057046]

91. Zhang, Yingjie; Yan, Jin and Yao, Tso-Pang.  2017-12-01  Discovery of a fluorescent probe with HDAC6 selective inhibition.  [PMID:29102179]

92. Wang, Xiu-Xiu XX, Wan, Ren-Zhong RZ and Liu, Zhao-Peng ZP.  2018-01-01  Recent advances in the discovery of potent and selective HDAC6 inhibitors.  [PMID:29133060]

93. Negmeldin, Ahmed T AT, Knoff, Joseph R JR and Pflum, Mary Kay H MKH.  2018-01-01  The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.  [PMID:29150330]

94. Chao, Shi-Wei SW and 9 more authors.  2018-01-01  Discovery of aliphatic-chain hydroxamates containing indole derivatives with potent class I histone deacetylase inhibitory activities.  [PMID:29223096]

95. Lee, Hsueh-Yun HY and 8 more authors.  2018-02-08  (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo.  [PMID:29304284]

96. Chen, Dizhong D, Soh, Chang Kai CK, Goh, Wei Huang WH and Wang, Haishan H.  2018-02-22  Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.  [PMID:29360358]

97. Li, Xiaoyang X and 7 more authors.  2018-03-22  Class I HDAC Inhibitors Display Different Antitumor Mechanism in Leukemia and Prostatic Cancer Cells Depending on Their p53 Status.  [PMID:29499113]

98. Li, Yongtao Y and 13 more authors.  2018-04-12  Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.  [PMID:29518312]

99. Rabal, Obdulia O and 15 more authors.  2018-04-25  Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.  [PMID:29549837]

100. Ojha, Ritu R and 10 more authors.  2018-04-25  1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.  [PMID:29567459]

101. Sellmer, Andreas A and 13 more authors.  2018-04-26  Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.  [PMID:29589441]

102. Zang, Jie J and 7 more authors.  2018-06-28  Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.  [PMID:29787262]

103. Huang, Yahui Y and 5 more authors.  2018-07-26  Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.  [PMID:29940115]

104. Lee, Hsueh-Yun HY and 11 more authors.  2018-08-23  5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.  [PMID:30028616]

105. Porter, Nicholas J and 6 more authors.  2018-09-13  Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.  [PMID:30118224]

106. Chu-Farseeva, Yu-Yi YY and 6 more authors.  2018-10-05  Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.  [PMID:30243158]

107. Diedrich, Daniela D and 14 more authors.  2018-10-05  One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.  [PMID:30245402]

108. Bhatia, Sanil S and 10 more authors.  2018-11-21  Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.  [PMID:30365892]

109. Bouchut, Anne A and 16 more authors.  2019-01-01  Identification of novel quinazoline derivatives as potent antiplasmodial agents.  [PMID:30366254]

110. Lai, Mei-Jung MJ and 11 more authors.  2019-01-15  1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.  [PMID:30476825]

111. Zhou, Ruolan R and 10 more authors.  2019-02-01  Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.  [PMID:30594434]

112. Song, Yoojin Y, Lim, Jiah J and Seo, Young Ho YH.  2019-02-15  A novel class of anthraquinone-based HDAC6 inhibitors.  [PMID:30597327]

113. Chen, Yong Y and 10 more authors.  2019-02-14  Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy.  [PMID:30629434]

114. Vögerl, Katharina and 15 more authors.  2019-02-14  Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.  [PMID:30645113]

115. Ling, Yong Y and 11 more authors.  2019-04-15  β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma.  [PMID:30851694]

116. Ling, Yong Y and 12 more authors.  2019-06-28  Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.  [PMID:31120744]

117. Yang, Zhuang Z and 10 more authors.  2019-09-15  Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.  [PMID:31177073]

118. Cao, Fangyuan F and 5 more authors.  2019-09-01  Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.  [PMID:31181405]

119. Bouchet, Samuel S and 8 more authors.  2019-06-13  Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.  [PMID:31223439]

120. Nam, Gibeom G and 7 more authors.  2019-08-01  Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.  [PMID:31235266]

121. Liu, Ruiqi R and 8 more authors.  2019-07-09  Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.  [PMID:31306905]

122. Reßing, Nina N and 9 more authors.  2019-07-01  Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.  [PMID:31391882]

123. Liang, Tao T, Hou, Xuben X, Zhou, Yi Y, Yang, Xinying X and Fang, Hao H.  2019-08-08  Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.  [PMID:31413795]

124. Shen, Sida S and 12 more authors.  2019-08-15  Discovery of a New Isoxazole-3-hydroxamate Based Histone Deacetylase 6 Inhibitor SS-208 with Anti-tumor Activity in Syngeneic Melanoma Mouse Models.  [PMID:31414801]

125. Brindisi, Margherita M and 5 more authors.  2019-08-27  Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.  [PMID:31415174]

126. Wan, Yichao; Li, Yuanhua; Yan, Chunxing; Yan, Mi and Tang, Zilong.  2019-12-01  Indole: A privileged scaffold for the design of anti-cancer agents.  [PMID:31536895]

127. Soumyanarayanan, Uttara and 8 more authors.  2019-12-15  Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.  [PMID:31627059]

128. Krieger, Viktoria and 10 more authors.  2019-12-26  Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.  [PMID:31762274]

129. Wu, Ying and 6 more authors.  2020-01-09  Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide.  [PMID:31938461]

130. Ojha, Ritu and 14 more authors.  2020-03-15  Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.  [PMID:32058238]

131. Wu, Bocheng and 5 more authors.  2020-03-15  Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.  [PMID:32061484]

132. Osko, Jeremy D and Christianson, David W.  2020-04-15  Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.  [PMID:32067866]

133. Tseng, Hui-Ju and 13 more authors.  2020-04-15  Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.  [PMID:32151835]

134. Pan, Zhaoping and 9 more authors.  2020-04-09  Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells.  [PMID:32153186]

135. Nepali, Kunal and 7 more authors.  2020-06-15  Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors.  [PMID:32325365]

136. Han, Guiyan and 5 more authors.  2020-05-28  Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.  [PMID:32347094]

137. Tng, Jiahui and 6 more authors.  2020-06-11  Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.  [PMID:32383881]

138. Romanelli, Annalisa and 14 more authors.  2020-05-14  Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.  [PMID:32435414]

139. Ghazy, Ehab and 12 more authors.  2020-08-15  Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.  [PMID:32497960]

140. Gawel, Justyna M and 14 more authors.  2020-09-01  PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.  [PMID:32615502]

141. Huang, Ying and 6 more authors.  2020-09-01  The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.  [PMID:32773090]

142. Yao, Dahong and 6 more authors.  2020-11-01  Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.  [PMID:32791401]

143. Reßing, Nina and 11 more authors.  2020-09-24  Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.  [PMID:32803970]

144. Noonepalle, Satish and 12 more authors.  2020-09-24  Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.  [PMID:32815366]

145. Wei, Mingming and 14 more authors.  2020-11-15  Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.  [PMID:32823005]

146. Cao, Fangyuan and 5 more authors.  2020-12-15  Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).  [PMID:32971411]

147. Gu, Xiaoke and 9 more authors.  2020-12-15  Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.  [PMID:33132117]

148. Relitti, Nicola and 17 more authors.  2021-02-15  Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation.  [PMID:33199154]

149. Mehndiratta, Samir and Liou, Jing-Ping.  2020-09-01  Histone lysine specific demethylase 1 inhibitors.  [PMID:33479691]

150. Bao, Yu and 8 more authors.  2021-01-14  Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group.  [PMID:33488962]

151. Zhao, Lei and 9 more authors.  2021-03-05  Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFRT790M mutant cell lines.  [PMID:33493830]

152. Singh, Arshdeep and 8 more authors.  2021-02-06  CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.  [PMID:33588178]

153. Rabal, Obdulia and 16 more authors.  2021-03-04  Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo Efficacy in Multiple Myeloma.  [PMID:33661013]

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