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Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5- (quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5- (quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors
Authors
Li F.Park Y.Hah J.-M.Ryu J.-S.
Ewha Authors
류재상
SCOPUS Author ID
류재상scopus
Issue Date
2013
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 23, no. 4, pp. 1083 - 1086
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles has been synthesized and evaluated for their ALK5 inhibitory activity. The 1-(6-methylpyridin-2-yl)-1,2,3-triazoles were assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition. Following this, quinoxaline was introduced through Pd-catalyzed direct arylation. The synthesized 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles revealed significant selectivity differences with respect to p38α MAP kinase. In particular, 12k showed 80.8% ALK5 inhibitory activity at a concentration of 10 μM and IC50 value of 4.69 μM, but did not show p38α MAP kinase inhibitory activity (-1.94% inhibition at a concentration of 10 μM). © 2012 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2012.12.008
Appears in Collections:
약학대학 > 약학과 > Journal papers
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