Abstract
A series of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles 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 and 4-[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]benzenesulfonamide showed more than 90% inhibition at 0.5 microM in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, but inhibited p38alpha MAP kinase activity only 11 and 8% at a concentration of 10 microM, respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzenesulfonamides
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Cell Line
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Receptor, Transforming Growth Factor-beta Type I
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Receptors, Transforming Growth Factor beta / antagonists & inhibitors*
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Structure-Activity Relationship
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Sulfonamides
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors
Substances
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Imidazoles
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Protein Kinase Inhibitors
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Receptors, Transforming Growth Factor beta
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Sulfonamides
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Protein Serine-Threonine Kinases
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p38 Mitogen-Activated Protein Kinases
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Receptor, Transforming Growth Factor-beta Type I
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TGFBR1 protein, human