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

✍ Scribed by Alex J. Buckmelter; Li Ren; Ellen R. Laird; Bryson Rast; Greg Miknis; Steve Wenglowsky; Stephen Schlachter; Mike Welch; Eugene Tarlton; Jonas Grina; Joseph Lyssikatos; Barbara J. Brandhuber; Tony Morales; Nikole Randolph; Guy Vigers; Matthew Martinson; Michele Callejo

Book ID: 104005220
Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 886 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.12.039

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✦ Synopsis

Virtual and high-throughput screening identified imidazo[1,2-a]pyrazines as inhibitors of B-Raf. We describe the rationale, SAR, and evolution of the initial hits to a series of furo[2,3-c]pyridine indanone oximes as highly potent and selective inhibitors of B-Raf.

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