Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.

Teresa E Williams,Sharadha Subramanian,Joelle Verhagen,Christopher M McBride,Abran Costales,Leonard Sung,William Antonios-McCrea,Maureen McKenna,Alicia K Louie,Savithri Ramurthy,Barry Levine,Cynthia M Shafer,Timothy Machajewski,Paul A Renhowe,Brent A Appleton,Payman Amiri, James Chou,Darrin Stuart,Kimberly Aardalen,Daniel Poon

ACS medicinal chemistry letters（2015）

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摘要

Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent cancers. We report the development of imidazo-benzimidazoles as potent B-RAF inhibitors. Robust in vivo efficacy coupled with correlating pharmacokinetic/pharmacodynamic (PKPD) and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials.

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关键词

B-RAF,MAP,VEGF,serine/threonine kinases,tyrosine kinases

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