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  • Title: Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
    Author: Gopalsamy A, Ciszewski G, Shi M, Berger D, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.
    Journal: Bioorg Med Chem Lett; 2009 Dec 15; 19(24):6890-2. PubMed ID: 19884006.
    Abstract:
    Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.
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