Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles as inhibitors of transforming growth factor-β type I receptor (ALK5) |
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| Authors: | Changbin Guo Chong Zhang Xingzhou Li Wei Li Zhongliang Xu Liangliang Bao Yue Ding Lili Wang Song Li |
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| Institution: | 1. Department of Chemistry, Capital Normal University, Beijing 100048, China;2. Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China |
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| Abstract: | A series of 2-(6-methylpyridin-2-yl)-1H-imidazoles were synthesized and evaluated for ALK5 inhibitory activity in cell-based luciferase reporter assays. The compound 4-(((1-(benzod]1,3]dioxol-5-yl)-2-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)methyl)amino)benzenesulfonamide (27a) exhibited slightly higher inhibition (IC50 = 0.24 μM) than SB431542 (IC50 = 0.35 μM), a well known potent ALK5 inhibitor. The binding mode of 27a generated by flexible docking study shows that it fits well into the site cavity of ALK5 by forming several tight interactions. |
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| Keywords: | ALK5 Kinase inhibitor Imidazole derivatives |
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