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Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors.
- Source :
-
Journal of Enzyme Inhibition & Medicinal Chemistry . Dec2020, Vol. 35 Issue 1, p702-712. 11p. - Publication Year :
- 2020
-
Abstract
- A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-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-CONH2 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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *MOLECULAR models
*IMIDAZOLES
*MOIETIES (Chemistry)
Subjects
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 35
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 147176757
- Full Text :
- https://doi.org/10.1080/14756366.2020.1734799