Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II

European Journal of Medicinal Chemistry
Qianbin LiWenfang Xu

Abstract

A novel class of potent aminopeptidase N inhibitors with 3-amino-cyclic-imide scaffold is described. The preliminary biological test revealed that all the compounds displayed high specific inhibitory activity against aminopeptidase N compared with previous work because of the existence of free amino group. Compounds containing hydroxamate group are more potent than carboxyl and ester derivatives. Compound 13f potentially inhibited APN activity with IC(50) value of 1.8 microM and displayed specific activity profiles in cells assay and in vivo anti-metastasis assay.

Citations

Dec 3, 2015·European Journal of Medicinal Chemistry·Chunhua MaYingjie Zhang
May 31, 2011·Expert Opinion on Therapeutic Patents·Li SuWenfang Xu
Apr 10, 2018·Journal of Medicinal Chemistry·Sk Abdul AminTarun Jha
Aug 11, 2017·Journal of the American Chemical Society·Noel Angel Espinosa-JalapaDavid Milstein

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