标题:Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
作者:Zhang Y;Feng J;Liu C;Zhang L;Jiao J;Fang H;Su L;Zhang X;Zhang J;Li M;Wang B;Xu W
作者机构:[Zhang, Y] Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, China;[ Feng, J] Department of Medicin 更多
通讯作者:Xu, WF
通讯作者地址:[Xu, WF]Shandong Univ, Sch Pharm, Dept Med Chem, Jinan 250012, Shandong, Peoples R China.
来源:Bioorganic and medicinal chemistry
出版年:2010
卷:18
期:5
页码:1761-1772
DOI:10.1016/j.bmc.2010.01.060
关键词:1,2,3,4-Tetrahydroisoquinoline-3-carboxylic acid derivatives; Histone; deacetylases; Inhibitor; Synthesis
摘要:Histone deacetylases (HDACs) are enzymes involved in tumor genesis and development. Herein, we report a novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as HDACs inhibitors. The preliminary biological screening showed that most of our compounds exhibited potent inhibitory activity against HDACs. Within this series, five compounds, 13a (IC(50)=0.58+/-0.10 microM), 7d (IC(50)=1.00+/-0.16 microM), 8l (IC(50)=1.06+/-0.14 microM), 7i (IC(50)=1.17+/-0.19 microM) and 7a (IC(50)=1.29+/-0.15 microM) possessed better HDACs inhibitory activity than Vorinostat (IC(50)=1.48+/-0.20 microM). So these five compounds could be used as novel lead compounds for further design of HDACs inhibitors. The anti-proliferative activities of a few compounds and the structure-activity relationships are also briefly discussed.
收录类别:SCOPUS;SCIE
WOS核心被引频次:43
Scopus被引频次:43
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-77249167010&doi=10.1016%2fj.bmc.2010.01.060&partnerID=40&md5=7fe209df165a666b28f9fdaf953c64b6
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