1197376-59-2Relevant academic research and scientific papers
Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors
Bode, Christiane M.,Boezio, Alessandro A.,Albrecht, Brian K.,Bellon, Steven F.,Berry, Loren,Broome, Martin A.,Choquette, Deborah,Dussault, Isabelle,Lewis, Richard T.,Lin, Min-Hwa Jasmine,Rex, Karen,Whittington, Douglas A.,Yang, Yajing,Harmange, Jean-Christophe
, p. 4089 - 4093 (2012/07/03)
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.
