4-Aryl-1,2,3-triazole: A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo
Journal of Medicinal Chemistry2005Vol. 48(18), pp. 5644–5647
Citations Over TimeTop 12% of 2005 papers
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
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.
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