标题:Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors
作者:Guan,P.;Sun,F.;Hou,X.;Wang,F.;Yi,F.;Xu,W.;Fang,H.
作者机构:[Guan, P] Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, China;[ Sun, F] Department of Medicinal 更多
通讯作者:Fang, H
通讯作者地址:[Fang, H]Shandong Univ, Sch Pharm, Minist Educ, Dept Med Chem,Key Lab Chem Biol, Jinan 250012, Shandong, Peoples R China.
来源:Bioorganic and medicinal chemistry
出版年:2012
卷:20
期:12
页码:3865-3872
DOI:10.1016/j.bmc.2012.04.032
关键词:1;3;4-Thiadiazole;Anticancer;Histone deacetylase inhibitors
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 (IC 50 = 0.089 μM), exhibited better inhibitory effect compared with SAHA (IC 50 = 0.15 μM).
收录类别:SCOPUS;SCIE
WOS核心被引频次:34
Scopus被引频次:34
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84861579581&doi=10.1016%2fj.bmc.2012.04.032&partnerID=40&md5=24812316c6709e3366848fab8fcf3c2f
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