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

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 wi...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (4), p.865-868
Hauptverfasser: SHEPPARD, George S, JIEYI WANG, PINGPING LOU, CHANG PARK, KIM, Ki H, HENKIN, Jack, LESNIEWSKI, Richard, KAWAI, Megumi, BAMAUNG, Nwe Y, CRAIG, Richard A, ERICKSON, Scott A, LYNCH, Linda, PATEL, Jyoti, FAN YANG, SEARLE, Xenia B
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Sprache:eng
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Zusammenfassung: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).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.12.031