2. Academic Validation
  3. Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy

Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy

  • Eur J Med Chem. 2016 Apr 13:112:81-90. doi: 10.1016/j.ejmech.2016.02.003.
Chao-Jun Gong 1,  An-Hui Gao 1,  Yang-Ming Zhang 1,  Ming-Bo Su 1,  Fei Chen 1,  Li Sheng 1,  Yu-Bo Zhou 1,  Jing-Ya Li 1,  Jia Li 2,  Fa-Jun Nan 3
Affiliations

Affiliations

  • 1 Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 189 Guoshoujing Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, PR China.
  • 2 Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 189 Guoshoujing Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, PR China. Electronic address: jli@simm.ac.cn.
  • 3 Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 189 Guoshoujing Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, PR China. Electronic address: fjnan@simm.ac.cn.
PMID: 26890114 DOI: 10.1016/j.ejmech.2016.02.003
Abstract

Histone deacetylases (HDACs) are a class of epigenetic modulators with complex functions in histone post-translational modifications and are well known targets for antineoplastic drugs. We have previously developed a series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors. In the present work, a new series of bisthiazole-based compounds with different zinc binding groups (ZBGs) have been designed and synthesized. Among them is compound 7, containing a trifluoromethyl ketone as the ZBG, which displays potent inhibitory activity towards human HDACs and improved antiproliferative activity in several Cancer cell lines.

Keywords

Bisthiazole; Histone deacetylases; Trifluoromethyl ketones; ZBG.

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