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Bioorg Med Chem Lett. 2012 Jun 15;22(12):4089-93. doi: 10.1016/j.bmcl.2012.04.072. Epub 2012 Apr 25.

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

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  • 1Amgen Inc., 360 Binney St., Cambridge, MA 02142, USA.


Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of a structurally diverse series of carbon-linked quinoline triazolopyridinones, which demonstrates nanomolar inhibition of c-Met kinase activity. This novel series of inhibitors exhibits favorable pharmacokinetics as well as potent inhibition of HGF-mediated c-Met phosphorylation in a mouse liver pharmacodynamic model.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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