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Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors.

Abstract：

: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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li S,Zhao Y,Wang K,Gao Y,Han J,Cui B,Gong P

doi

10.1016/j.bmc.2013.04.013

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

2843-55

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00330-1

journal_volume

21

pub_type

杂志文章

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