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ID: ALA1154789
Journal: Eur J Med Chem
Title: Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Design, chemistry and activity evaluation. Part I.
Authors: Li Q, Fang H, Wang X, Hu L, Xu W.
Abstract: A series of aminopeptidase inhibitors with cyclic-imide scaffold are described. The biological characterization for the piperidinedione analogues revealed that most compounds displayed high inhibitory activity against APN. Among which 4l and 6 showed potent inhibition against APN with the IC(50) value of 5.2 microM and 3.1 microM, respectively. In addition, 6 also displayed good activity in HL-60 cell assay and in vivo anti-metastasis assay. This interesting activity profile may also guide the design of new, specific inhibitors of target mammalian aminopeptidases with 'one-zinc' active site.
CiteXplore: 19683842