Synthesis and antitumor activities of 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives

Paper

Synthesis and antitumor activities of 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives

Published 2010 · Gong Ping

Chinese Journal of Medicinal Chemistry

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Abstract

Aim To design and synthesize a series of novel 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives,and to evaluate their antitumor activities.Methods The target compounds were synthesized via several steps with the starting material ethyl cyanoacetate,and their antitumor activities were examined against A549,HT-29 and MDA-MB-231 cell lines in vitro with gefitinib as positive control.Results Eigh-teen target compounds were synthesized and their structures were confirmed by 1H-NMR,IR and MS spectra.The pharmacological tests showed that seven of the tested compounds,Ⅶ2,Ⅶ3,Ⅶ6,Ⅶ12,Ⅶ13,Ⅶ15 and Ⅶ16,exhibited more potent antiproliferative activity than gefitinib did.Conclusion The structure-activity relationships of 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives,as a novel type of EGFR inhibitor,should be further investigated.

In Vitro Study

Study Snapshot

4-(methylphenylamino)-quinoline-3-carbonitrile derivatives show more potent antitumor activity than gefitinib, suggesting their potential as a novel EGFR inhibitor.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Synthesis and antitumor activities of 4-(methylphenylamino)-quinoline-3-carbonitrile derivatives

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