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Your search keyword '"Choi, Joon-hun"' showing total 8 results
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8. Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1 H -imidazoles as ALK5 inhibitors.

Author

Park MS, Park HJ, An YJ, Choi JH, Cha G, Lee HJ, Park SJ, Dewang PM, and Kim DK

Subjects
Caco-2 Cells, Cell Line, Dose-Response Relationship, Drug, Humans, Imidazoles chemical synthesis, Imidazoles chemistry, Models, Molecular, Molecular Structure, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors chemistry, Receptor, Transforming Growth Factor-beta Type I metabolism, Structure-Activity Relationship, Imidazoles pharmacology, Protein Kinase Inhibitors pharmacology, Receptor, Transforming Growth Factor-beta Type I antagonists & inhibitors
Abstract

A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1 H -imidazoles, 7a-c , 11a-h , and 16a-h has been synthesised and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Incorporation of a quinoxalin-6-yl moiety and a methylene linker at the 4- and 2-position of the imidazole ring, respectively, and a m- CONH 2 substituent in the phenyl ring generated a highly potent and selective ALK5 inhibitor 11e . Docking model of ALK5 in complex with 11e showed that it fitted well in the ATP-binding pocket with favourable interactions.

Published
2020
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