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Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer

文献类型：期刊论文

作者Chen, Danqi1; Shen, Aijun2; Fang, Guanghua1; Liu, Hongchun2; Zhang, Minmin2; Tang, Shuai2; Xiong, Bing1; Ma, Lanping1; Geng, Meiyu2; Shen, Jingkang1
刊名ACTA PHARMACEUTICA SINICA B
出版日期2016-01
卷号6期号:1页码:93-99
关键词Histone deacetylases inhibitor Anticancer Tetrahydroisoquinoline Structure-activity relationship
ISSN号2211-3835
DOI10.1016/j.apsb.2015.11.002
文献子类Article
英文摘要Histone acetylation is a critical process in the regulation of chromatin structure and gene expression. Histone deacetylases (HDACs) remove the acetyl group, leading to chromatin condensation and transcriptional repression. HDAC inhibitors are considered a new class of anticancer agents and have been shown to alter gene transcription and exert antitumor effects. This paper describes our work on the structural determination and structure-activity relationship (SAR) optimization of tetrahydroisoquinoline compounds as HDAC inhibitors. These compounds were tested for their ability to inhibit HDAC 1, 3, 6 and for their ability to inhibit the proliferation of a panel of cancer cell lines. Among these, compound 82 showed the greatest inhibitory activity toward HDAC 1, 3, 6 and strongly inhibited growth of the cancer cell lines, with results clearly superior to those of the reference compound, vorinostat (SAHA). Compound 82 increased the acetylation of histones H3, H4 and tubulin in a concentration-dependent manner, suggesting that it is a broad inhibitor of HDACs. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
WOS关键词SOLID TUMORS ; DISCOVERY ; DESIGN
资助项目National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program' of China[2014ZX09507002] ; National Marine '863' Project[2013AA092902]
WOS研究方向Pharmacology & Pharmacy
语种英语
CSCD记录号CSCD:5625142
WOS记录号WOS:000371987700010
出版者INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
源URL[http://119.78.100.183/handle/2S10ELR8/276240]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
药理学第一研究室
通讯作者Ma, Lanping; Geng, Meiyu; Shen, Jingkang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Chen, Danqi,Shen, Aijun,Fang, Guanghua,et al. Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer[J]. ACTA PHARMACEUTICA SINICA B,2016,6(1):93-99.
APA Chen, Danqi.,Shen, Aijun.,Fang, Guanghua.,Liu, Hongchun.,Zhang, Minmin.,...&Shen, Jingkang.(2016).Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer.ACTA PHARMACEUTICA SINICA B,6(1),93-99.
MLA Chen, Danqi,et al."Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer".ACTA PHARMACEUTICA SINICA B 6.1(2016):93-99.

入库方式： OAI收割

来源：上海药物研究所

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