3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2

George S. Sheppard*, Jieyi Wang, Megumi Kawai, Nwe Y. BaMaung, Richard A. Craig, Scott A. Erickson, Linda Lynch, Jyoti Patel, Fan Yang, Xenia B. Searle, Pingping Lou, Chang Park, Ki H. Kim, Jack Henkin, Richard Lesniewski

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    47 Scopus citations


    Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).

    Original languageEnglish (US)
    Pages (from-to)865-868
    Number of pages4
    JournalBioorganic and Medicinal Chemistry Letters
    Issue number4
    StatePublished - Feb 23 2004

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry


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