Synthesis and in vitro antiproliferative effect of novel quinoline-based potential anticancer agents

被引:65
|
作者
Arafa, Reem K. [1 ]
Hegazy, Gehan H. [1 ]
Piazza, Gary A. [2 ]
Abadi, Ashraf H. [1 ,3 ]
机构
[1] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo 11562, Egypt
[2] Univ S Alabama, Mitchell Canc Inst, Dept Oncol Sci, Mobile, AL 36604 USA
[3] German Univ Cairo, Fac Pharm & Biotechnol, Dept Pharmaceut Chem, Cairo 11835, Egypt
关键词
Quinolines; Antiproliferative agents; Cytotoxicity; HT29 human colon cancer cell line; MDA-MB231 human breast cancer cell line; TUMOR-CELLS; DERIVATIVES; REVERSAL; MT477;
D O I
10.1016/j.ejmech.2013.03.008
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several derivatives with a quinoline scaffold and a flexible, semi-flexible or rigid side chains at position 8 of the quinoline ring were synthesized and assessed for their in vitro activity versus the human colon cancer cell line HT29 and the human breast cancer cell line MDA-MB231. The HT29 cell line was more refractory to the cytotoxic activity of some compounds, meanwhile all the quinoline derivatives except one displayed high to moderate activity against MDA-MB231 with IC50 values ranging between 4.6 and 48.2 mu M. The most active derivative in this study against both tested cell lines was the Schiff's base 4e with IC50 of 4.7 and 4.6 mu M against HT29 and MDA-MB231, respectively. (C) 2013 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:826 / 832
页数:7
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