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ID: ALA1146714

Journal: Bioorg Med Chem Lett

Title: Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors.

Authors: Hu X, Zhu J, Srivathsan S, Pei D.

Abstract: A new class of methionine aminopeptidase (MetAP) inhibitors, which contain an internal hydroxamate (N-acyl-N-alkylhydroxylamine) core as the metal-chelating group, has been designed, synthesized, and tested. The compounds exhibited reversible, competitive inhibition against Escherichia coli MetAP as well as human MetAP-1 and MetAP-2. The most potent inhibitor had a K(i) value of 2.5 microM and >20-fold selectivity toward E. coli MAP.

CiteXplore: 14684302

DOI: 10.1016/j.bmcl.2003.10.031