Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1573-7. doi: 10.1016/j.bmcl.2010.01.064. Epub 2010 Jan 21.
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.
描述了一系列新型嘧啶-4-基-1H-咪唑-2-基衍生物 7、8、9 的合成及其对 A375P 人黑色素瘤细胞系和 WM3629 细胞系的抗增殖活性。与著名的 RAF 抑制剂索拉非尼相比，大多数化合物表现出优异的抗增殖活性。其中，7a 对这两种细胞系均表现出较强的活性（IC50 分别为 0.62 和 4.49μM），并且是一种选择性和有效的 CRAF 抑制剂。
