期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 12, 页码 5754-5762出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.08.013
关键词
1,3,4-Triarylpyrazole; Melanoma; Diarylurea; Diarylamide; B-RAF kinase; ERK kinase
资金
- Korea Institute of Science and Technology (KIST)
- National Research Council of Science & Technology (NST), Republic of Korea [2E2236] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
- National Research Foundation of Korea [핵C6A3404] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Synthesis of a new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold is described. Their in vitro antiproliferative activities against 9 human melanoma cell lines were tested. Compounds 12, 13, 15, and 21-23 showed the highest potency against A375P melanoma cell line. In addition, compounds 10-15 and 19-24 showed high potency over the NCl 8 tested melanoma cell-lines panel. The IC50 values for compound 23 were 0.36 mu M and 0.84 mu M over LOX IMVI and M14 cell lines, respectively. Compounds 21 and 23 showed high, dose-dependent inhibition of ERK kinase. Virtual screening was carried out through docking of compound 21 into the domain of V600E-B-RAF and the binding mode was studied. (C) 2011 Elsevier Masson SAS. All rights reserved.
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