Amino-benzosuberone: A novel warhead for selective inhibition of human aminopeptidase-N/CD13

…, M Al-Lakkis-Wehbe, A Orsini, A Defoin, P Pale…

Index: Albrecht, Sebastien; Al-Lakkis-Wehbe, Mira; Orsini, Alban; Defoin, Albert; Pale, Patrick; Salomon, Emmanuel; Tarnus, Celine; Weibel, Jean-Marc Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 4 p. 1434 - 1449

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Citation Number: 15

Abstract

This paper describes the design and synthesis of compounds belonging to a novel class of highly selective mammalian CD13 inhibitors. Racemic homologues of 3-amino-2-tetralone 1 were synthesised and evaluated for their ability to selectively inhibit the membrane-bound, zinc-dependent aminopeptidase-N/CD13 (EC 3.4. 11.2). Some of these novel non-peptidic compounds are potent, competitive inhibitors of the mammalian enzyme, with Ki values in ...