Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase
Journal of Medicinal Chemistry2008Vol. 51(10), pp. 2879–2882
Citations Over TimeTop 10% of 2008 papers
Brian K. Albrecht, Jean-Christophe Harmange, David Bauer, Loren Berry, Christiane Bode, Alessandro A. Boezio, April Chen, Deborah M. Choquette, Isabelle Dussault, Cary Fridrich, Satoko Hirai, Doug Hoffman, Jay F. Larrow, Paula Kaplan‐Lefko, Jasmine Lin, Julia Lohman, Alexander Long, Jodi Moriguchi, Anne O’Connor, Michele Potashman, Monica Reese, Karen Rex, Aaron Siegmund, Kavita Shah, Roman Shimanovich, Stephanie K. Springer, Yohannes Teffera, Yajing Yang, Yihong Zhang, Steven F. Bellon
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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