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
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
收藏
页码:929 / 939
页数:11
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