标题:Design and Synthesis of a Tetrahydroisoquinoline-Based Hydroxamate Derivative (ZYJ-34v), An Oral Active Histone Deacetylase Inhibitor with Potent Antitumor Activity
作者:Zhang, Yingjie; Liu, Chunxi; Chou, C. James; Wang, Xuejian; Jia, Yuping; Xu, Wenfang
作者机构:[Zhang, Yingjie; Xu, Wenfang] Shandong Univ, Dept Med Chem, Sch Pharm, Jinan 250012, Shandong, Peoples R China.; [Liu, Chunxi] Shandong Univ, Sch Ph 更多
通讯作者:Xu, WF
通讯作者地址:[Xu, WF]Shandong Univ, Dept Med Chem, Sch Pharm, Jinan 250012, Shandong, Peoples R China.
来源:CHEMICAL BIOLOGY & DRUG DESIGN
出版年:2013
卷:82
期:2
页码:125-130
DOI:10.1111/cbdd.12144
关键词:antitumor; histone deacetylases; inhibitor; oral active;; tetrahydroisoquinoline; valproic acid
摘要:In our previous study, we developed a novel series of tetrahydroisoquinoline-based hydroxamic acid derivatives as histone deacetylase inhibitors (Bioorg Med Chem, 2010, 18, 1761-1772; J Med Chem, 2011, 54, 2823-2838), among which, compound ZYJ-34c (1) was identified and validated as the most potent one with marked in vitro and in vivo antitumor potency (J Med Chem, 2011, 54, 5532-5539.). Herein, further modification in 1 afforded another oral active analog ZYJ-34v (2) with simplified structure and lower molecular weight. Biological evaluation of compound 2 showed efficacious inhibition against histone deacetylase 1, 2, 3, and 6, which was confirmed by Western blot analysis results. Most importantly, compound 2 exhibited similar even more potent in vitro and in vivo antitumor activities relative to the approved histone deacetylase inhibitor SAHA.
收录类别:SCOPUS;SCIE
WOS核心被引频次:5
Scopus被引频次:5
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84880745811&doi=10.1111%2fcbdd.12144&partnerID=40&md5=caaaee4e7f5e913478ce3408d70e8083
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