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Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
Authors
Kim D.-K.Jung S.H.Lee H.S.Dewang P.M.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2009
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 44, no. 2, pp. 568 - 576
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles (15a-l) have been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 4-[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]b enzenesulfonamide (15b) and 4-[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]be nzenesulfonamide (15c) showed more than 90% inhibition at 0.5 μM in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, but inhibited p38α MAP kinase activity only 11 and 8% at a concentration of 10 μM, respectively. © 2008 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2008.03.024
Appears in Collections:
약학대학 > 약학과 > Journal papers
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