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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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
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author Dan Liu
Tian Luan
Jian Kong
Ying Zhang
Hai-Feng Wang
author_facet Dan Liu
Tian Luan
Jian Kong
Ying Zhang
Hai-Feng Wang
author_sort Dan Liu
collection DOAJ
description 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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spelling doaj.art-4fd0cfd48c90492bbddbf6482c251bf62022-12-21T23:23:06ZengMDPI AGMolecules1420-30492015-12-012112110.3390/molecules21010021molecules21010021Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline DerivativesDan Liu0Tian Luan1Jian Kong2Ying Zhang3Hai-Feng Wang4Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, ChinaDepartment of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, ChinaDepartment of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, ChinaDepartment of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, ChinaDepartment of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, ChinaTwenty-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.http://www.mdpi.com/1420-3049/21/1/214-anilinoquinolinesEGFRantitumorinhibitor
spellingShingle Dan Liu
Tian Luan
Jian Kong
Ying Zhang
Hai-Feng Wang
Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
Molecules
4-anilinoquinolines
EGFR
antitumor
inhibitor
title Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
title_full Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
title_fullStr Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
title_full_unstemmed Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
title_short Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
title_sort synthesis and anti tumor activities of 4 anilinoquinoline derivatives
topic 4-anilinoquinolines
EGFR
antitumor
inhibitor
url http://www.mdpi.com/1420-3049/21/1/21
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AT yingzhang synthesisandantitumoractivitiesof4anilinoquinolinederivatives
AT haifengwang synthesisandantitumoractivitiesof4anilinoquinolinederivatives