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

被引：6

作者：

Chen, Laizhong ^{[1
]}

Mou, Jiajia ^{[1
]}

Xu, Yingying ^{[1
]}

Fang, Hao ^{[1
]}

Xu, Wenfang ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharm, Dept Med Chem, 44 Wenhuaxi Rd, Jinan 250012, Shandong, Peoples R China

来源：

DRUG DISCOVERIES AND THERAPEUTICS | 2011年 / 5卷 / 02期

基金：

国家高技术研究发展计划(863计划); 中国国家自然科学基金;

关键词：

AHPA derivatives; synthesis; inhibitors; aminopeptidase N;

D O I：

10.5582/ddt.2011.v5.2.61

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of (2RS, 3S)-3-amino2-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.

引用

页码：61 / 65

页数：5

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