| Literature DB >> 15012983 |
George S Sheppard1, 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.
Abstract
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).Entities:
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Year: 2004 PMID： 15012983 DOI： 10.1016/j.bmcl.2003.12.031
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823