期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 3, 页码 254-259出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.12.063
关键词
Synthesis; 4-Phenoxypyridine derivatives; 1,8-Naphthyridinone; Antiproliferative activity; c-Met; Flt-3
资金
- National Natural Science Foundation of China (NSFC) [81660572]
- Natural Science Foundation of Jiangxi Province [20171BAB215071]
- Top-notch talent project of Jiangxi Science & Technology Normal University [2016QNBJRC002]
- Jiangxi Provincial Key Laboratory of Drug Design and Evaluation [20171BCD40015]
A series of 2-substituted-4-phenoxypyridine derivatives were designed, synthesized, and evaluated for their antiproliferative activity against 4 cancer cell lines (A549, HT-29, H460, and U87MG) in vitro. Most compounds showed moderate to excellent potency. Nine tyrosine kinases (c-Met, Flt-3, ALK, VEGFR-2, VEGFR-3, PDGFR-alpha, PDGFR-beta, c-Kit, and EGFR) were used to evaluate the inhibitory activities with the most promising analogue 39, which showed the Flt-3/c-Met IC50 values of 2.18/2.61 nM. Structure-activity relationship studies indicated that n-Pr served as R-1 group showed a higher preference, and stronger mono-EWGs on the phenyl ring (such as R-2 = 4-F) was benefited to the potency. (C) 2017 Elsevier Ltd. All rights reserved.
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