Design, synthesis and activity study of aminopeptidase N targeted 3-amino-2-hydroxy-4-phenyl-butanoic acid derivatives

Laizhong Chen; Jiajia Mou; Yingying Xu; Hao Fang; Wenfang Xu

doi:10.5582/ddt.2011.v5.2.61

Brief Report

Design, synthesis and activity study of aminopeptidase N targeted 3-amino-2-hydroxy-4-phenyl-butanoic acid derivatives

Laizhong Chen, Jiajia Mou, Yingying Xu, Hao Fang, Wenfang Xu

著者情報

キーワード: AHPA derivatives, synthesis, inhibitors, aminopeptidase N

ジャーナルフリー

2011 年 5 巻 2 号 p. 61-65

DOI https://doi.org/10.5582/ddt.2011.v5.2.61

詳細

抄録

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.

責任著者(Corresponding author)

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