Discovery and Initial SAR of Pyrimidin-4-yl-1H-imidazole derivatives with Antiproliferative activity against Melanoma cell lines

Title
Discovery and Initial SAR of Pyrimidin-4-yl-1H-imidazole derivatives with Antiproliferative activity against Melanoma cell lines
Authors
이정헌김환유하나정재윤오창현유경호심태보하정미
Keywords
Pyrimidin-4-yl-1H-imidazol-2-yl; derivatives; Antiproliferative activity; Melanoma cell line; BRAF; CRAF; Selectivity
Issue Date
2010-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, NO 5, 1573-1577
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 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.
URI
http://pubs.kist.re.kr/handle/201004/37580
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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