1. Academic Validation
  2. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase

  • J Med Chem. 2008 May 22;51(10):2879-82. doi: 10.1021/jm800043g.
Brian K Albrecht 1 Jean-Christophe Harmange David Bauer Loren Berry Christiane Bode Alessandro A Boezio April Chen Deborah Choquette Isabelle Dussault Cary Fridrich Satoko Hirai Doug Hoffman Jay F Larrow Paula Kaplan-Lefko Jasmine Lin Julia Lohman Alexander M Long Jodi Moriguchi Anne O'Connor Michele H Potashman Monica Reese Karen Rex Aaron Siegmund Kavita Shah Roman Shimanovich Stephanie K Springer Yohannes Teffera Yajing Yang Yihong Zhang Steven F Bellon
Affiliations

Affiliation

  • 1 Amgen Inc., Cambridge, MA 02139, USA. brian.albrecht@amgen.com
Abstract

Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity.

Figures
Products