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Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors

Title
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors
Author
하정미
Keywords
4-arylamido 3-methyl isoxazoles; Antiproliferative activity; Hematopoietic cell line; Kinase inhibitor; Kinase selectivity; DESIGN; TARGET
Issue Date
2015-09
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 102, Page. 600-610
Abstract
A series of 4-arylamido 3-methyl isoxazoles were synthesized and evaluated for their antiproliferative activities against the A375P melanoma and U937 hematopoietic cell lines. Most compounds showed selective antiproliferative activity toward the U937 cell line and the activities were better than that of sorafenib, the reference standard. Derivatives were made as amide 5a-b, 6a-o and urea 7a-n, 8a-g with hydrophobic moieties, and one of the most potent inhibitor 6a, 5-methyl-N-(2-methyl-5-(3-(4-methylpiperazin-l-yl)-5-(trifluoromethyl)benzamido)pherwl)isoxazole-4-carboxamide was found to be very potent inhibitor of FMS kinase (GI(50) = 0.016 mu M, IC50 = 9.95 nM) with excellent selectivity profiles and is a promising candidate for further development in therapeutics for cancer. (C) 2015 Elsevier Masson SAS. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0223523415302154?via%3Dihubhttp://hdl.handle.net/20.500.11754/40270
ISSN
0223-5234; 1768-3254
DOI
10.1016/j.ejmech.2015.08.031
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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