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Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-β type1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-β type1 receptor kinase inhibitors
Authors
Kim D.-K.Choi J.H.An Y.J.Lee H.S.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 18, no. 6, pp. 2122 - 2127
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 5-(pyridin-2-yl)thiazoles (14a-l and 15a-l) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-[[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl ]benzamide (15i) and 3-[[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl] benzamide (15k) showed more than 95% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luciferase reporter construct. © 2008 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2008.01.084
Appears in Collections:
약학대학 > 약학과 > Journal papers
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