title: Design, synthesis and activity study of aminopeptidase N targeted 3-amino-2-hydroxy-4-phenyl-butanoic acid derivatives.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, China.
authors.forename: L Z
authors.initials: LZ
authors.lastname: Chen
authors.forename: J J
authors.initials: JJ
authors.lastname: Mou
authors.forename: Y Y
authors.initials: YY
authors.lastname: Xu
authors.forename: H
authors.initials: H
authors.lastname: Fang
authors.forename: W F
authors.initials: WF
authors.lastname: Xu