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Non-oxime pyrazole based inhibitors of B-Raf kinase |
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| Authors: | Newhouse Bradley J Hansen Joshua D Grina Jonas Welch Mike Topalov George Littman Nicole Callejo Michele Martinson Matthew Galbraith Sarah Laird Ellen R Brandhuber Barbara J Vigers Guy Morales Tony Woessner Rich Randolph Nikole Lyssikatos Joseph Olivero Alan |
| Affiliation: | a Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, United States b Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080-4990, United States |
| Abstract: | The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a selective and potent B-Raf inhibitor. |
| Keywords: | B-Raf Oxime Pyrazole |
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