Structure Based Design and Syntheses of Amino-1H-pyrazole Amide Derivatives as Selective Raf Kinase Inhibitors in Melanoma Cells
- Structure Based Design and Syntheses of Amino-1H-pyrazole Amide Derivatives as Selective Raf Kinase Inhibitors in Melanoma Cells
- 김미현; 김민정; 유하나; 김환; 유경호; 심태보; 하정미
- Aminopyrazole amide; Antiproliferative activity; Melanoma cell line; Kinase inhibitor; Kinase selectivity
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 19, NO 6, 1915-1923
- The synthesis of a novel series of N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl amide derivatives
6a–o, 7a–s and their antiproliferative activities against A375P melanoma cell line were described. Most
compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among
ureido)-2-methylbenzamide 7c exhibited potent activities (GI50 = 0.27 lM). Especially, 7c was found to
be a potent and selective B-Raf V600E and C-Raf inhibitor (IC50 = 0.26 μM, IC50 = 0.11 μM, respectively),
showing a possibility as melanoma therapeutics.
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