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Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
Authors
Kim D.-K.Jang Y.Ho S.L.Park H.-J.Yoo J.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2007
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 50, no. 13, pp. 3143 - 3147
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 4(5)-(6-alkylpyridin-2-yl)imidazoles 13a-p, 17a, and 17b have been synthesized and evaluated for ALK5 inhibitory activity in an enzyme assay and in cell-based luciferase reporter assays. The quinoxalinyl analogue 13e inhibited ALK5 phosphorylation with an IC 50 of 0.012 μM and showed more than 90% inhibition at 0.05 μM in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct. The binding mode of 13e generated by flexible docking studies shows that 13e fits well into the active site cavity of ALK5 by forming several tight interactions. © 2007 American Chemical Society.
DOI
10.1021/jm070129k
Appears in Collections:
약학대학 > 약학과 > Journal papers
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