期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 14, 页码 4228-4232出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.05.032
关键词
TGF-beta; ALK5 inhibitor; Cell-based luciferase reporter assays
资金
- Ministry of Commerce, Industry and Energy, Korea [10027900]
- Korea Institute of Industrial Technology(KITECH) [10027900] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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 mu M in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luc reporter construct, respectively. (C) 2010 Elsevier Ltd. All rights reserved.
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