Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy
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- 作者：Chao-Jun Gong1 ; An-Hui Gao1 ; Yang-Ming Zhang ; Ming-Bo Su ; Fei Chen ; Li Sheng ; Yu-Bo Zhou ; Jing-Ya Li ; Jia Li ; jli@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author ; Fa-Jun Nan ; fjnan@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Bisthiazole ; Histone deacetylases ; ZBG ; Trifluoromethyl ketones
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：13 April 2016
- 年：2016
- 卷：112
- 期：Complete
- 页码：81-90
- 全文大小：1402 K
文摘
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Bisthiazole-based HDACi with different ZBGs were designed and synthesized.
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Bisthiazole compounds with trifluoromethyl ketone as ZBG showed improved efficacy.
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The most potent compound 7 displayed an IC50 value of 20–30 nM against HDACs.
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Compound 7 displayed potent antiproliferative activity against several cancer cell lines.