Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.

Basic Information

ID: ALA1155370

Journal: Bioorg Med Chem Lett

Title: Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.

Authors: Lee J, Kim H, Yu H, Chung JY, Oh CH, Yoo KH, Sim T, Hah JM.

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.

CiteXplore: 20149658

DOI: 10.1016/j.bmcl.2010.01.064

Patent ID: