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  • Title: Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.
    Author: Lee J, Kim H, Yu H, Chung JY, Oh CH, Yoo KH, Sim T, Hah JM.
    Journal: Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1573-7. PubMed ID: 20149658.
    Abstract:
    The synthesis of a novel series of pyrimidin-4-yl-1H-imidazol-2-yl derivatives 7, 8, 9 and their antiproliferative activities against A375P human melanoma cell line and WM3629 cell line were described. Most compounds showed superior antiproliferative activities compared to Sorafenib, the well-known RAF inhibitor. Among them, 7a exhibited potent activities on both cell lines (IC(50)=0.62 and 4.49muM, respectively) and turned out to be a selective and potent CRAF inhibitor.
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