The discovery of furo [2, 3-c] pyridine-based indanone oximes as potent and selective B-Raf inhibitors

…, E Tarlton, J Grina, J Lyssikatos, BJ Brandhuber…

Index: Buckmelter, Alex J.; Ren, Li; Laird, Ellen R.; Rast, Bryson; Miknis, Greg; Wenglowsky, Steve; Schlachter, Stephen; Welch, Mike; Tarlton, Eugene; Grina, Jonas; Lyssikatos, Joseph; Brandhuber, Barbara J.; Morales, Tony; Randolph, Nikole; Vigers, Guy; Martinson, Matthew; Callejo, Michele Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 4 p. 1248 - 1252

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Citation Number: 16

Abstract

The Ras/Raf/MEK/ERK signal transduction pathway is critical to the survival, growth, and proliferation of cells and has been implicated in several human cancers. B-Raf is a serine-threonine kinase in this pathway that has been shown to have a much higher basal kinase activity relative to either of its isoforms (A-Raf or C-Raf), and recently has been reported to be frequently mutated in various human cancers. Activating B-Raf mutations, most notably V600E (formerly termed ...