标题: Design, synthesis and activity study of aminopeptidase N targeted 3-amino-2-hydroxy-4-phenyl-butanoic acid derivatives.
作者: Chen, L Z; Mou, J J; Xu, Y Y; Fang, H; Xu, W F
作者机构:[ Chen, L Z; Chen LZ] Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, China.;[ Mou, J J; Mou JJ];[ Xu, Y 更多
来源: Drug discoveries & therapeutics
出版年:2011
卷: 5
期: 2
DOI: 422 [pii]
摘要: A series of (2RS,3S)-3-amino-2-hydroxy-4-phenyl-butanoic acids (AHPA) derivatives (MA0-MA7) were synthesized. The in vitro aminopeptidase N (APN) enzyme and cell proliferation assay of target compounds were investigated. The results showed that most compounds displayed potent inhibitory activities against APN, compound MA0 showed even better inhibitory effects than bestatin on both enzyme activity and HL60 cell proliferation. The FlexX docking result showed the mode of binding between MA0 and APN.
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资源类型:期刊论文
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