1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A Novel Type II Raf kinase inhibitors
- 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A Novel Type II Raf kinase inhibitors
- 유하나; 정윤경; 김환; 이정헌; 오창현; 유경호; 심태보; 하정미
- 1,4-Dihydropyrazolo[4,3-d]imidazole; phenyl derivatives; Antiproliferative activity; Melanoma cell line; Selectivity
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 20, NO 12, 3805-3808
- 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.
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