Structure Based Design and Syntheses of Amino-1H-pyrazole Amide Derivatives as Selective Raf Kinase Inhibitors in Melanoma Cells

Title
Structure Based Design and Syntheses of Amino-1H-pyrazole Amide Derivatives as Selective Raf Kinase Inhibitors in Melanoma Cells
Authors
김미현김민정유하나김환유경호심태보하정미
Keywords
Aminopyrazole amide; Antiproliferative activity; Melanoma cell line; Kinase inhibitor; Kinase selectivity
Issue Date
2011-03
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 19, NO 6, 1915-1923
Abstract
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 them, N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl) 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.
URI
http://pubs.kist.re.kr/handle/201004/40817
ISSN
0968-0896
Appears in Collections:
KIST Publication > Article
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