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Bioorg Med Chem Lett. 2004 Feb 23;14(4):865-8.

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

Author information

1
Abbott Laboratories, Global Pharmaceutical Research and Development, Cancer Research, 100 Abbott Park Road, Abbott Park, IL 60064, USA. george.sheppard@abbott.com

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).

PMID:
15012983
DOI:
10.1016/j.bmcl.2003.12.031
[Indexed for MEDLINE]

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