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

Autor: Kallander, L. S., Lu, Q., Chen, W., Tomaszek, T., Yang, G., Tew, D., Meek, T. D., Hofmann, G. A., Schulz-Pritchard, C. K., Smith, W. W., Janson, C. A., Ryan, M. D., Zhang, G.-F., Johanson, K. O., Kirkpatrick, R. B., Ho, T. F., Fisher, P. W., Mattern, M. R., Johnson, R. K., Hansbury, M. J., Winkler, J. D., Ward, K. W., Veber, D. F., Thompson, S. K.
Zdroj: Journal of Medicinal Chemistry; September 2005, Vol. 48 Issue: 18 p5644-5647, 4p
Abstrakt: 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.
Databáze: Supplemental Index