A novel amino-benzosuberone derivative is a picomolar inhibitor of mammalian aminopeptidase N/CD13

C Maiereanu, C Schmitt, N Schifano-Faux…

Index: Maiereanu, Carmen; Schmitt, Celine; Schifano-Faux, Nadge; Le Nouen, Didier; Defoin, Albert; Tarnus, Celine Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5716 - 5733

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Citation Number: 17

Abstract

A new class of low molecular weight, highly potent and selective non peptidic inhibitors of aminopeptidase N (APN/CD13) is described. We report the synthesis and in vitro evaluation of racemic substituted analogues of 7-amino-benzocyclohepten-6-one 1a. We investigated various substitutions on the aromatic ring with phenyl and halogen groups. In vitro kinetic studies revealed that these compounds are among the most effective APN/CD13 inhibitors ...