Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors

被引：56

作者：

Guan, Peng ^{[1
]}

Sun, Feng'e ^{[1
]}

Hou, Xuben ^{[1
]}

Wang, Feng ^{[1
]}

Yi, Fan ^{[2
]}

Xu, Wenfang ^{[1
]}

Fang, Hao ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharm, Minist Educ, Dept Med Chem,Key Lab Chem Biol, Jinan 250012, Shandong, Peoples R China

[2] Shandong Univ, Sch Med, Dept Pharmacol, Jinan 250012, Shandong, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 12期

关键词：

1,3,4-Thiadiazole; Histone deacetylase inhibitors; Anticancer; ANTITUMOR ACTIVITIES;

D O I：

10.1016/j.bmc.2012.04.032

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Histone deacetylase (HDAC) inhibitors have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. In the present study, a series of 1,3,4-thiadiazole based hydroxamic acids were developed as potent HDAC inhibitors. Some of them showed good inhibitory activity in HDAC enzyme assay and potent growth inhibition in some tumor cell lines. Among them, compound 6i (IC50 = 0.089 mu M), exhibited better inhibitory effect compared with SAHA (IC50 = 0.15 mu M). (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3865 / 3872

页数：8

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