Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives

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...

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Bibliographic Details
Main Authors: Dan Liu, Tian Luan, Jian Kong, Ying Zhang, Hai-Feng Wang
Format: Article
Language:English
Published: MDPI AG 2015-12-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/21/1/21
Description
Summary: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.
ISSN:1420-3049