Brief Report
Design, synthesis and activity study of aminopeptidase N targeted 3-amino-2-hydroxy-4-phenyl-butanoic acid derivatives
2011 Volume 5 Issue 2 Pages 61-65
Details
2011 Volume 5 Issue 2 Pages 61-65
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.
