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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1573-7. doi: 10.1016/j.bmcl.2010.01.064. Epub 2010 Jan 21.

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

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1
Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.

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.

PMID:
20149658
DOI:
10.1016/j.bmcl.2010.01.064
[Indexed for MEDLINE]

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