1256349-67-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors
Chen, Xin,Zhao, Shuang,Li, Hongmei,Wang, Xin,Geng, Aixin,Cui, Hao,Lu, Tao,Chen, Yadong,Zhu, Yong
, p. 110 - 122 (2019)
Histone deacetylases (HDACs) as appealing targets for the treatment of many diseases has been studied extensively and its use in cancer care is the most important. Here, we developed a series of novel derivatives containing isoindolinone skeleton. Twelve compounds demonstrated nanomolar IC50 values against HDAC1, and the best compounds were 5a (65.6 nM), 5b (65.1 nM) and 13a (57.9 nM). In vitro, 5a and 5b also showed potent antiproliferative activities against several cancer cell lines, in particular 5b, which behaved better than approved drug chidamide. Morever, enzyme inhibition and western blot assay established 5b to be a selective inhibitor for HDAC1-3. Molecular docking was performed to rationalize the high potency of isoindolinones. Additionally, 5b had more appropriate drug metabolism in human liver microsome (HLM) compared with chidamide and moderate pharmacokinetics properties. These results indicated that 5b was worthy of further biological studies.
NAPHTHALENE CARBOXAMIDE DERIVATIVES AS INHIBITORS OF PROTEIN KINASE AND HISTONE DEACETYLASE, PREPARATION METHODS AND USES THEREOF
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Page/Page column 18, (2012/04/23)
The naphthalene carboxamide derivatives, the preparation methods and the uses thereof are provided. The structure thereof is shown as the formula (I), wherein the definitions of R1, R2, R3, R4 and Z are the same
Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors
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Page/Page column 15, (2010/12/29)
Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatm
