Kim, Mi-hyun Kim, Minjung Yu, Hana Kim, Hwan Yoo, Kyung Ho Sim, Taebo Hah, Jung-Mi 2024-01-20T17:31:14Z 2024-01-20T17:31:14Z 2021-09-02 2011-03-15 0968-0896 https://pubs.kist.re.kr/handle/201004/130534 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. English PERGAMON-ELSEVIER SCIENCE LTD BRAF MUTATIONS CRAF Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells Article 10.1016/j.bmc.2011.01.067 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.19, no.6, pp.1915 - 1923 BIOORGANIC & MEDICINAL CHEMISTRY 19 6 1915 1923 scie scopus 000288196900008 2-s2.0-79952453681 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article BRAF MUTATIONS CRAF Aminopyrazole amide Antiproliferative activity Melanoma cell line Kinase inhibitor Kinase selectivity