2. Academic Validation
  3. 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
PMID: 18426196 DOI: 10.1021/jm800043g
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.

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