Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells
- Authors
- Kim, Mi-hyun; Kim, Minjung; Yu, Hana; Kim, Hwan; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung-Mi
- Issue Date
- Mar-2011
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Aminopyrazole amide; Antiproliferative activity; Melanoma cell line; Kinase inhibitor; Kinase selectivity
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.19, no.6, pp.1915 - 1923
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 19
- Number
- 6
- Start Page
- 1915
- End Page
- 1923
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/38204
- DOI
- 10.1016/j.bmc.2011.01.067
- ISSN
- 0968-0896
- 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.
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