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

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

  • J Med Chem. 2005 Sep 8;48(18):5644-7. doi: 10.1021/jm050408c.
Lara S Kallander 1,  Qing Lu,  Wenfang Chen,  Thaddeus Tomaszek,  Guang Yang,  David Tew,  Thomas D Meek,  Glenn A Hofmann,  Christina K Schulz-Pritchard,  Ward W Smith,  Cheryl A Janson,  M Dominic Ryan,  Gui-Feng Zhang,  Kyung O Johanson,  Robert B Kirkpatrick,  Thau F Ho,  Paul W Fisher,  Michael R Mattern,  Randall K Johnson,  Michael J Hansbury,  James D Winkler,  Keith W Ward,  Daniel F Veber,  Scott K Thompson
Affiliations

Affiliation

  • 1 GlaxoSmithKline Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA. [email protected]
PMID: 16134930 DOI: 10.1021/jm050408c
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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