Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors

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• 作者：Peng Guan^a ; Feng&rsquo ; e Sun^a ; Xuben Hou^a ; Feng Wang^a ; Fan Yi^b ; Wenfang Xu^a ; Hao Fang^a ; ^{haofangcn@sdu.edu.cn}
• 关键词：RSAWOPMPUVTZGX-OUKQBFOZSA-N ; JFFSLVSLBFEXJJ-UHFFFAOYSA-N ; FATZGTRPEGZRDM-UHFFFAOYSA-N ; LFGPNCCYHIZERK-UHFFFAOYSA-N ; FKZSXARZQYLGIT-VOTSOKGWSA-N ; YRBLXLBAXMDAHJ-UHFFFAOYSA-N ; IZNCFULXCFWHRB-RMKNXTFCSA-N ; RNWKHWGZJUKVGU-UHFFFAOYSA-N ; QYQXQKQVCNIZPK-UHFFFAOY
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 June, 2012
• 卷：20
• 期：12
• 页码：3865-3872
• 文件大小：2255 K

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 (IC₅₀ = 0.089 渭M), exhibited better inhibitory effect compared with SAHA (IC₅₀ = 0.15 渭M).