Portal de Periódicos da CAPES

4-Aryl-1,2,3-triazole: A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo

2005; American Chemical Society; Volume: 48; Issue: 18 Linguagem: Inglês

10.1021/jm050408c

1520-4804

Lara S. Kallander, Qing Lü, Wenfang Chen, Thaddeus A. Tomaszek, Guang Yang, David G. Tew, Thomas D. Meek, Glenn A. Hofmann, Christina K. Schulz-Pritchard, Ward W. Smith, Cheryl A. Janson, Margret Ryan, Guifeng Zhang, Kyung Johanson, Robert B. Kirkpatrick, Thau Ho, Paul W. Fisher, Michael R. Mattern, Randall K. Johnson, Michael Hansbury, James D. Winkler, Keith W. Ward, Daniel F. Veber, Scott K. Thompson,

Signaling Pathways in Disease

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.