Design, synthesis and biological evaluation of novel HDAC inhibitors: sulphur-containing zinc binding groups

作     者：Wenwen Cheng Dongmei Zhang Qiang Zheng Zhongjun Li Xiangbao Meng 程文文;张冬梅;郑强;李中军;孟祥豹

作者机构：State Key Laboratory of Natural and Biomimetic DrugsSchool of Pharmaceutical SciencesPeking University Health Science CenterBeijing100191China Shandong Institute for Food and Drug ControlJinan250101China 

基　　金：National Natural Science Foundation of China(Grant No.81573272) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2019年第28卷第6期

页      码：408-421页

摘      要：Zinc binding group(ZBG)is the crucial moiety in the chemical structure of any HDAC *** the present study,a series of sulphur-containing ZBG were designed and synthesized in the novel HDAC inhibitors to replace the classical ZBGs of SAHA and BML-210,hydroxamic acids and benzamides,*** HDAC inhibitory activity and the structure-activity relationships of these molecules were analyzed.A sulphur-rich group,diethylcarbamo(dithioperoxo)thioate,was finally identified as a novel potent *** all the synthesized compounds,4 d was much more potent compared with BML-210,and it showed similar inhibitory effect of SAHA against HDAC isoforms 1 and ***,it was chosen as a lead compound.

主 题 词：Histone deacetylase inhibitor Zinc binding group Anticancer 

学科分类：1007[医学-药学类] 1006[医学-中西医结合类] 100706[100706] 100701[100701] 10[医学] 100602[100602] 

核心收录：

D　O　I：10.5246/jcps.2019.06.040

馆 藏 号：203688923...