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Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
Authors
Dewang P.M.Kim D.-K.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 20, no. 14, pp. 4228 - 4232
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 2-pyridyl-substituted pyrazoles (16a-d, 17, 18, and 28a-e) and imidazoles (22 and 23) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-(3-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-pyrazole-1-carbothioamido)benzamide (28c) showed 96% and 93% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luc reporter construct, respectively. © 2010 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2010.05.032
Appears in Collections:
약학대학 > 약학과 > Journal papers
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