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

Authors
Lee, JunghunKim, HwanYu, HanaChung, Jae YoonOh, Chang-HyunYoo, Kyung HoSim, TaeboHah, Jung-Mi
Issue Date
Mar-2010
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Pyrimidin-4-yl-1H-imidazol-2-yl derivatives; Antiproliferative activity; Melanoma cell line; BRAF; CRAF; Selectivity
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.5, pp.1573 - 1577
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
20
Number
5
Start Page
1573
End Page
1577
URI
https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/39934
DOI
10.1016/j.bmcl.2010.01.064
ISSN
0960-894X
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 (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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