Design, synthesis and biological evaluation of new 4-(4-substituted-anilino)quinoline derivatives as anticancer agents

被引：36

作者：

Abdellatif, Khaled R. A. ^{[1
,2
]}

Abdelall, Eman K. A. ^{[1
]}

Abdelgawad, Mohamed A. ^{[1
,3
]}

Amin, Dina M. E. ^{[1
]}

Omar, Hany A. ^{[4
,5
]}

机构：

[1] Beni Suef Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Bani Suwayf 62514, Egypt

[2] Ibn Sina Natl Coll Med Studies, Pharmaceut Sci Dept, Jeddah 21418, Saudi Arabia

[3] Al Jouf Univ, Dept Pharmaceut Chem, Fac Pharm, Sakaka, Al Jouf, Saudi Arabia

[4] Beni Suef Univ, Dept Pharmacol & Toxicol, Fac Pharm, Bani Suwayf 62514, Egypt

[5] Univ Sharjah, Sharjah Inst Med Res, Dept Pharmacol, Coll Pharm, Sharjah 27272, U Arab Emirates

来源：

MEDICINAL CHEMISTRY RESEARCH | 2017年 / 26卷 / 05期

关键词：

Quinoline; Antitumor; MCF-7; EGFR; KINASE INHIBITORS; QUINOLINE; ANALOGS; DOCKING;

D O I：

10.1007/s00044-017-1798-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 4-(4-substituted-anilino)quinoline derivatives 6a-f was synthesized from amine derivatives via Gould-Jacobs reaction. All synthesized compounds were evaluated for their cytotoxic activity against two human cancer cell lines; breast carcinoma (MCF-7) and non-small cell lung cancer (A549). The tested compounds showed a broad range of activities (IC50 = 3.42-23.32 and 5.97-22.01 mu M) in comparison with doxorubicin (IC50 = 2.07 and 0.02 mu M) and erlotinib (IC50 = 1.14 and 19.26 mu M) for MCF-7 and A549 respectively. The 4-(4-chloroanilino)quinoline derivative (6c, IC50 = 3.42 and 5.97 mu M) was the most potent among all compounds against both MCF-7 and A549 cell lines respectively. In addition, molecular docking studies were performed and the results were in agreement with the in vitro cytotoxic data.

引用

页码：929 / 939

页数：11

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