Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors

被引：6

作者：

Zhang, Qingwei

Lu, Bingliu

Li, Jianqi ^{[1
]}

机构：

[1] Shanghai Inst Pharmaceut Ind, Novel Technol Ctr Pharmaceut Chem, Shanghai 201203, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 14期

基金：

中国国家自然科学基金;

关键词：

Chidamide derivatives; HDACs inhibitors; Anticancer activity; Molecular docking; HISTONE DEACETYLASE INHIBITOR; CANCER; EXPRESSION;

D O I：

10.1016/j.bmcl.2017.05.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and biological evaluation of a variety of 4-piperazinyl-containing Chidamide derivatives is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below micromolar range, and inhibited proliferation of several human cancer cells, not possessing toxicity to human normal cells and hERG K+ ion channels. Compound 9g, proved to be the most potent and efficacious derivative in this series, was orally active in an HCT116 xenograft model in vivo. (C) 2017 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3162 / 3166

页数：5

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