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Molecules 2016, 21(1), 21;

Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives

Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China
Author to whom correspondence should be addressed.
Academic Editor: D. Hadjipavlou-Litina
Received: 2 November 2015 / Revised: 26 November 2015 / Accepted: 2 December 2015 / Published: 23 December 2015
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [708 KB, uploaded 23 December 2015]   |  


Twenty-two 7-fluoro (or 8-methoxy)-4-anilinoquinolines compounds were designed and synthesized as potentially potent and selective antitumor inhibitors. All the prepared compounds were evaluated for their in vitro antiproliferative activities against the HeLa and BGC823 cell lines. Ten compounds (1ag; 2c; 2e and 2i) exhibited excellent antitumor activity superior to that of gefitinib. Among the ten compounds; seven (1ac; 1e1g and 2i) displayed excellent selectivity for BGC823 cells. In particular; 1f and 2i exhibited potent cytotoxic activities against HeLa cells and BGC823 cells with better IC50 values than gefitinib. View Full-Text
Keywords: 4-anilinoquinolines; EGFR; antitumor; inhibitor 4-anilinoquinolines; EGFR; antitumor; inhibitor

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Liu, D.; Luan, T.; Kong, J.; Zhang, Y.; Wang, H.-F. Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives. Molecules 2016, 21, 21.

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