期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 11, 页码 2843-2855出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.04.013
关键词
Receptor tyrosine kinase; c-Met; 4-(2-Fluorophenoxy)quinoline derivatives; 4-Oxo-1,4-dihydrocinnoline-3-carboxamide
A series of novel 4-(2-fluorophenoxy)quinoline derivatives containing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and six typical cancer cell lines (A549, H460, HT-29, MKN-45, U87MG and SMMC-7721). All the prepared compounds showed moderate to excellent antiproliferative activity, and the analysis of their structure-activity relationships indicated that 2-chloro or 2-trifluoromethyl substituted phenyl group on the 1-position of cinnoline ring was more favorable for antitumor activity. In this study, a promising compound 33, with a c-Met IC50 value of 0.59 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor. (C) 2013 Elsevier Ltd. All rights reserved.
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