Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors

被引：33

作者：

Tan, Qiu ^{[1
]}

Zhang, Zhitao ^{[1
]}

Hui, Jie ^{[1
]}

Zhao, Yu ^{[1
]}

Zhu, Li ^{[1
]}

机构：

[1] Nantong Univ, Inst Naut Med, Nantong 226001, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Thieno[3,2-d]pyrimidines; HDAC; Synthesize; Anti-proliferative; HISTONE-DEACETYLASE INHIBITORS; MOLECULAR-MECHANISMS; HYDROXAMIC ACID; CANCER CELLS; DESIGN; APOPTOSIS;

D O I：

10.1016/j.bmc.2013.11.021

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：

A series of thieno[3,2-d]pyrimidines bearing a hydroxamic acid moiety as novel HDAC inhibitors were designed and synthesized. The structures of the new synthesized compounds were confirmed using IR, H-1, C-13 NMR spectrum. Compounds 11-13 showed potent inhibitory activities against HDACs with IC50 values at 0.38, 0.49 and 0.61 mu M. Most of target compounds displayed strong anti-proliferative activity by a MTT assay on three human cancer cell lines including HCT-116, MCF-7 and HeLa. Compound 11, having potent inhibitory activities against HDACs, induced apoptosis and G2/M cell cycle arrest in HCT-116 cell line. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：358 / 365

页数：8

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