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


  • 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.

published proceedings

  • J Med Chem

altmetric score

  • 9

author list (cited authors)

  • Kallander, L. S., Lu, Q., Chen, W., Tomaszek, T., Yang, G., Tew, D., ... Thompson, S. K.

citation count

  • 145

complete list of authors

  • Kallander, Lara S||Lu, Qing||Chen, Wenfang||Tomaszek, Thaddeus||Yang, Guang||Tew, David||Meek, Thomas D||Hofmann, Glenn A||Schulz-Pritchard, Christina K||Smith, Ward W||Janson, Cheryl A||Ryan, M Dominic||Zhang, Gui-Feng||Johanson, Kyung O||Kirkpatrick, Robert B||Ho, Thau F||Fisher, Paul W||Mattern, Michael R||Johnson, Randall K||Hansbury, Michael J||Winkler, James D||Ward, Keith W||Veber, Daniel F||Thompson, Scott K

publication date

  • September 2005