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
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.
Kim, Dae-Kee,Jung, Sun Hee,Lee, Ho Soon,Dewang, Purushottam M.
experimental part
p. 568 - 576
(2009/09/27)
Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-β type1 receptor kinase inhibitors
A series of 5-(pyridin-2-yl)thiazoles (14a-l and 15a-l) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-[[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl ]b
Kim, Dae-Kee,Choi, Joon Hun,An, Young Jae,Lee, Ho Soon
p. 2122 - 2127
(2008/12/21)
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
A series of 4(5)-(6-alkylpyridin-2-yl)imidazoles 13a-p, 17a, and 17b have been synthesized and evaluated for ALK5 inhibitory activity in an enzyme assay and in cell-based luciferase reporter assays. The quinoxalinyl analogue 13e inhibited ALK5 phosphoryla
Kim, Dae-Kee,Jang, Yoojeung,Ho, Soon Lee,Park, Hyun-Ju,Yoo, Jakyung
p. 3143 - 3147
(2008/02/08)
Triarylimidazole derivatives as cytokine inhibitors
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are various substituent groups; and one of X1 and X2 is N or CR″, and the other is NR″ or CHR″ wherein R″
-
(2008/06/13)
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