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  • Title: Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.
    Author: Blackburn C, Duffey MO, Gould AE, Kulkarni B, Liu JX, Menon S, Nagayoshi M, Vos TJ, Williams J.
    Journal: Bioorg Med Chem Lett; 2010 Aug 15; 20(16):4795-9. PubMed ID: 20630752.
    Abstract:
    A high throughput screen identified N-aroylpyrazoline 1 as a selective inhibitor of the V600E mutant of B-Raf kinase. Parallel synthesis of acyl, aroyl, and sulfonyl derivatives led to the identification of several potent inhibitors in both enzymatic and cellular (pERK) assays such as compound 42.
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