Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
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Updated: Mar 28, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Dan Liu1, Tian Luan2, Jian Kong3
1Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. liudan20040318@163.com.
Abstract:
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 (1a-g; 2c; 2e and 2i) exhibited excellent antitumor activity superior to that of gefitinib. Among the ten compounds; seven (1a-c; 1e-1g 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.
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