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
- Author
- 하정미
- Keywords
- Aminopyrazole amide; Antiproliferative activity; Melanoma cell line; Kinase inhibitor; Kinase selectivity
- Issue Date
- 2011-03
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v. 19, NO. 6, Page. 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 (GI(50) = 0.27 mu M). Especially, 7c was found to be a potent and selective B-Raf V600E and C-Raf inhibitor (IC50 = 0.26 mu M, IC50 = 0.11 mu M, respectively), showing a possibility as melanoma therapeutics. (C) 2011 Elsevier Ltd. All rights reserved.
- URI
- https://www.sciencedirect.com/science/article/pii/S0968089611000964?via%3Dihubhttps://repository.hanyang.ac.kr/handle/20.500.11754/186144
- ISSN
- 0968-0896;1464-3391
- DOI
- 10.1016/j.bmc.2011.01.067
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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