期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 17, 页码 5246-5260出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.06.026
关键词
c-Met; Kinase inhibitor; Anti-tumor; Quinoline; Semicarbazone
资金
- National ST Major Project [2011ZX09102-001-006]
- National Natural Science Foundation of China (NSFC) [21002065]
A novel series of N-1-(3-fluoro-4-(6,7-disubstituted-quinolin-4-yloxy)phenyl)-N-4-arylidenesemicarbazide derivatives were synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against A549, HT-29, MKN-45 and MDA-MB-231 cancer cell lines in vitro. Several potent compounds were further evaluated against three other cancer cell lines (U87MG, NCI-H460 and SMMC7721). Most of compounds tested exhibited moderate to excellent activity. The studies of SARs identified the most promising compound 28 (c-Met IC50 = 1.4 nM) as a c-Met kinase inhibitor. In this study, a promising compound 28 was identified, which displayed 2.1-, 3.3-, 48.4- and 3.6-fold increase against A549, HT-29, U87MG and NCI-H460 cell lines, respectively, compared with that of Foretinib. (C) 2013 Elsevier Ltd. All rights reserved.
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