1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A Novel Type II Raf kinase inhibitors

Title
1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A Novel Type II Raf kinase inhibitors
Authors
유하나정윤경김환이정헌오창현유경호심태보하정미
Keywords
1,4-Dihydropyrazolo[4,3-d]imidazole; phenyl derivatives; Antiproliferative activity; Melanoma cell line; Selectivity
Issue Date
2010-06
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, NO 12, 3805-3808
Abstract
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 μM). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics.
URI
http://pubs.kist.re.kr/handle/201004/37582
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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