Design, Synthesis and Biological Evaluation of Novel Selective Thiol-based Histone Deacetylase（HDAC） Ⅵ Inhibitors Bearing Indeno[1,2-c]pyrazole or Benzoindazole Scaffold

作     者：XU Qihao YU Shujia CAI Yijun YANG Jinyu ZHAO Linxiang LIU Dan 

作者机构：Key Laboratory of Structure-based Drug Design and Discovery Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 P.. 1~ China 

基　　金：Supported by the National Natural Science Foundation of China(No.81473086) and the Natural Science Foundation of Liaoning Province  China(No.2015020728 -301 ) 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2018年第34卷第1期

页      码：75-83页

摘      要：A series of thiol-based mdeno[1,2-c]pyrazoles and benzoindazole compounds was designed and synthesized according to the structural specificity of his-tone deacetylase VI（HDAC6） and the structural characteristics of HDAC inhibitors. The inhibitory activities of the target compounds against HDAC6 and HDAC1 were screened by fluorescence analysis. Most of the target compounds showed moderate inhibitory activity against HDAC6（IC50=44-598 nmol/L）. Among them, compound A-4 displayed the highest selectivity against HDAC6 and similar inhibitory activity（IC50=44 nmol/L） to that of the positive drug SAHA（IC50=41 nmol/L） against HDAC6.

主 题 词：Histone deacetylase Ⅵ(HDAC6) selective inhibitor, Indeno[1,2-c]pyrazole compound Benzoindazole compound Antitumor 

学科分类：0710[理学-生物科学类] 081901[081901] 0819[工学-海洋工程类] 07[理学] 08[工学] 09[农学] 

核心收录：

D　O　I：10.1007/s40242-018-7239-6

馆 藏 号：203284449...