Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives

Molecules

Dan Liu¹  Tian Luan²  Jian Kong²  Ying Zhang²  Hai-Feng Wang² 

[1] Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China

关键词: 4-anilinoquinolines;    EGFR;    antitumor;    inhibitor;   

DOI  :  10.3390/molecules21010021

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.