Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase

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• 作者：Brian K. Albrecht ; Jean-Christophe Harmange ; David Bauer ; Loren Berry ; Christiane Bode ; Alessandro A. Boezio ; April Chen ; Deborah Choquette ; Isabelle Dussault ; Cary Fridrich ; Satoko Hirai ; Doug Hoffma
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：May 22, 2008
• 年：2008
• 卷：51
• 期：10
• 页码：2879 - 2882
• 全文大小：728K
• 年卷期：v.51,no.10(May 22, 2008)
• ISSN：1520-4804

文摘

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.