标题:Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif
作者:Guan, Peng;Wang, Lei;Hou, Xuben;Wan, Yichao;Xu, Wenfang;Tang, Weiping;Fang, Hao
作者机构:[Guan, P] Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Shandong University, Jinan, Shandong, 250012, China;[ Wang, L] Depart 更多
通讯作者:Fang, H
通讯作者地址:[Fang, H]Shandong Univ, Key Lab Chem Biol, Dept Med Chem, Minist Educ,Sch Pharm, Jinan 250012, Shandong, Peoples R China.
来源:Bioorganic and medicinal chemistry
出版年:2014
卷:22
期:21
页码:5766-5775
DOI:10.1016/j.bmc.2014.09.039
关键词:1;3;4-Thiadiazole;Hydroxamic acid;Histone deacetylase inhibitor;Surface recognition motif;Antiproliferation
摘要:A series of 1,3,4-thiadiazole-containing hydroxamic acids, in accord with the common pharmacophore of histone deacetylase (HDAC) inhibitors (a Zn2+ binding moiety-a linker-a surface recognition motif), was identified as submicromolar HDAC inhibitors by our group. In this study, we continued our efforts to develop 1,3,4-thiadiazole bearing hydroxamate analogues by modifying the surface recognition motif. We found that 1,3,4-thiadiazoles having a heteroaromatic substituent showed better HDAC inhibitory activity in enzymatic assay and higher antiproliferative potency in cellular assay compared to SAHA. (C) 2014 Elsevier Ltd. All rights reserved.
收录类别:SCOPUS;SCIE
WOS核心被引频次:14
Scopus被引频次:14
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84908428873&doi=10.1016%2fj.bmc.2014.09.039&partnerID=40&md5=288ab41e24292d561acf40df1934d496
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