苯磺酰胺取代的4-(6-烷基吡啶-2-基)-5-(喹喔啉-6-基)咪唑作为转化生长因子-β1受体激酶抑制剂的合成及生物学评价
Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
作者信息
Kim Dae-Kee, Jung Sun Hee, Lee Ho Soon, Dewang Purushottam M
机构信息
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, South Korea.
出版信息
Eur J Med Chem. 2009 Feb;44(2):568-76. doi: 10.1016/j.ejmech.2008.03.024. Epub 2008 Apr 4.
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.
已经合成了一系列苯磺酰胺取代的4-(6-烷基吡啶-2-基)-5-(喹喔啉-6-基)咪唑，并在基于细胞的荧光素酶报告基因检测中评估了它们对ALK5的抑制活性。其中，4-[5-(6-甲基吡啶-2-基)-4-(喹喔啉-6-基)-1H-咪唑-2-基甲基]苯磺酰胺和4-[5-(6-乙基吡啶-2-基)-4-(喹喔啉-6-基)-1H-咪唑-2-基甲基]苯磺酰胺在使用p3TP-luc报告基因构建体瞬时转染的HaCaT细胞的荧光素酶报告基因检测中，在0.5 microM时显示出超过90%的抑制率，但在10 microM浓度下分别仅抑制p38α丝裂原活化蛋白激酶活性11%和8%。
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