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

GS Sheppard, J Wang, M Kawai, NY BaMaung…

Index: Sheppard, George S.; Wang, Jieyi; Kawai, Megumi; BaMaung, Nwe Y.; Craig, Richard A.; Erickson, Scott A.; Lynch, Linda; Patel, Jyoti; Yang, Fan; Searle, Xenia B.; Lou, Pingping; Park, Chang; Kim, Ki H.; Henkin, Jack; Lesniewski, Richard Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 4 p. 865 - 868

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Citation Number: 43

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 ...