期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 12, 页码 3805-3808出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.039
关键词
1,4-Dihydropyrazolo[4,3-d]imidazole; phenyl derivatives; Antiproliferative activity; Melanoma cell line; Selectivity
资金
- 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 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC50 = 0.56-0.86 mu M). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics. (C) 2010 Elsevier Ltd. All rights reserved.
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