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
收藏
页码：358 / 365
页数：8
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