期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 5, 页码 1573-1577出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.064
关键词
Pyrimidin-4-yl-1H-imidazol-2-yl derivatives; Antiproliferative activity; Melanoma cell line; BRAF; CRAF; Selectivity
资金
- Korea Institute of Science and Technology (KIST)
- Ministry of Education, Science and Technology [2009-0087992]
- National Research Foundation of Korea [2009-0087992] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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 (IC50 = 0.62 and 4.49 mu M, respectively) and turned out to be a selective and potent CRAF inhibitor. (C) 2010 Elsevier Ltd. All rights reserved.
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