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Bioorg Med Chem Lett. 2012 May 15;22(10):3387-91. doi: 10.1016/j.bmcl.2012.04.015. Epub 2012 Apr 10.

The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.

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  • 1Array BioPharma, Inc., 3200 Walnut Street, Boulder, CO 80301, United States.


Herein we describe the discovery of a novel series of ATP competitive B-Raf inhibitors via structure based drug design (SBDD). These pyridopyrimidin-7-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 17, a potent, selective and orally available agent with excellent pharmacokinetic properties and robust tumor growth inhibition in xenograft studies.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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