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. 2008 May 22;51(10):2879-82.
doi: 10.1021/jm800043g. Epub 2008 Apr 22.

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

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

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

Brian K Albrecht et al. J Med Chem. .

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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