Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors
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 quinoxal
An, Young Jae,Cha, Geunyoung,Choi, Joon Hun,Dewang, Purushottam M.,Kim, Dae-Kee,Lee, Hwa Jeong,Park, Hyun-Ju,Park, Myoung-Soon,Park, So-Jung
p. 702 - 712
(2020/03/23)
2-PYRIDYL SUBSTITUTED IMIDAZOLES AS ALK5 AND/OR ALK4 INHIBITORS
This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifi
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Page/Page column 20-21; 33
(2008/06/13)
2-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors
Compounds of the formula: wherein R1, R2, R3, A1 and A2 are as defined herein, which are used advantageously in inhibiting the TGF-β and/or activin signaling pathway in mammals.
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Page/Page column 8
(2008/06/13)
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