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ID: ALA1146676

Journal: Bioorg Med Chem Lett

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

Authors: Sheppard GS, Wang J, Kawai M, BaMaung NY, Craig RA, Erickson SA, Lynch L, Patel J, Yang F, Searle XB, Lou P, Park C, Kim KH, Henkin J, Lesniewski R.

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).

CiteXplore: 15012983

DOI: 10.1016/j.bmcl.2003.12.031