期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 2, 页码 568-576出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.03.024
关键词
Transforming growth factor-beta (TGF-beta); ALK5 inhibitors; Fibrosis; Cancer
资金
- Ministry of Commerce, Industry and Energy, Korea [MI-0310-43-0001, MI-0310-43-0002]
A series of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles (15a-1) 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]benzenesulfonamide (15b) and 4-[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]benzene-sulfonamide (15c) showed more than 90% inhibition at 0.5 mu M in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, but inhibited p38 alpha MAP kinase activity only 11 and 8% at a concentration of 10 mu M, respectively. (C) 2008 Elsevier Masson SAS. All rights reserved.
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