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J Med Chem. 2005 Sep 8;48(18):5644-7.

4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.

Author information

1
GlaxoSmithKline Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA. lara.s.kallander@gsk.com

Abstract

Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.

PMID:
16134930
DOI:
10.1021/jm050408c
[Indexed for MEDLINE]

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