文献类型：期刊文献

英文题名：Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)

作者：Ma, Lei[1,2];Yang, Zhengyi[1];Li, Chenjing[1];Zhu, Zhiyuan[1];Shen, Xu[1];Hu, Lihong[1,2]

机构：[1]Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China;[2]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2011

卷号：26

期号：5

起止页码：643

外文期刊名：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000294864300004)】；

基金：This work was supported by the Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" (grants 2009ZX09301-001, 2009ZX09102-022), the Chinese National High-Tech R&D Program (grants 2007AA02Z147), the National Natural Science Foundation of China (grants 90713046, 30772638, 30925040), CAS Foundation (grant KSCX2-YW-R-179) and China 111 Project (B07023).

语种：英文

外文关键词：Alzheimer's disease; BACE1; chalcone; SAR; Glycyrrhiza uralensis

摘要：According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of beta-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A- and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC(50) = 0.27 mu M).