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Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1)

文献类型：期刊论文

作者Ma, Lei1,2; Yang, Zhengyi1; Li, Chenjing1; Zhu, Zhiyuan1; Shen, Xu1; Hu, Lihong1,2
刊名JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
出版日期2011-10
卷号26期号:5页码:643-648
关键词Alzheimer's disease BACE1 chalcone SAR Glycyrrhiza uralensis
ISSN号1475-6366
DOI10.3109/14756366.2010.543420
文献子类Article
英文摘要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).
WOS关键词AMYLOID PRECURSOR PROTEIN ; HUMAN BRAIN ; ALZHEIMERS-DISEASE ; POTENT INHIBITORS ; MICE
资助项目Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09102-022] ; Chinese National High-tech RD Program[2007AA02Z147] ; National Natural Science Foundation of China[90713046] ; National Natural Science Foundation of China[30772638] ; National Natural Science Foundation of China[30925040] ; CAS Foundation[KSCX2-YW-R-179] ; China 111 Project[B07023]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000294864300004
出版者INFORMA HEALTHCARE
源URL[http://119.78.100.183/handle/2S10ELR8/278380]  
专题上海中药现代化研究中心
通讯作者Hu, Lihong
作者单位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
推荐引用方式
GB/T 7714		 Ma, Lei,Yang, Zhengyi,Li, Chenjing,et al. Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1)[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2011,26(5):643-648.
APA Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,&Hu, Lihong.(2011).Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1).JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,26(5),643-648.
MLA Ma, Lei,et al."Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1)".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 26.5(2011):643-648.

入库方式： OAI收割

来源：上海药物研究所

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