Bioorganic & medicinal chemistry letters

Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors

X Hu, J Zhu, S Srivathsan, D Pei

文献索引：Hu, Xubo; Zhu, Jinge; Srivathsan, Sumant; Pei, Dehua Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 1 p. 77 - 79

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被引用次数: 33

摘要

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 Ki value of 2.5 μM and> 20-fold selectivity toward E. coli MAP.