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Design, Synthesis and Activity Study of Aminopeptidase N Targeted AHPA Derivatives

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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.

This study was published online in Drug Discoveries and Therapeutics and is free to access.