Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles

被引:10
作者
Christodoulou, Antonios [1 ]
Kostakis, Ioannis K. [1 ]
Kourafalos, Vassilios [1 ]
Pouli, Nicole [1 ]
Marakos, Panagiotis [1 ]
Trougakos, Ioannis P. [2 ]
Tsitsilonis, Ourania E. [3 ]
机构
[1] Univ Athens, Dept Pharm, Div Pharmaceut Chem, GR-15771 Athens, Greece
[2] Univ Athens, Dept Cell Biol & Biophys, Fac Biol, Athens 15784, Greece
[3] Univ Athens, Fac Biol, Dept Anim & Human Physiol, Athens 15784, Greece
关键词
Thioxanthone analogues; Fuzed isoindoles; Nitracrine; Cytotoxic activity; Multi-drug resistance; BREAST-CANCER CELLS; ANTI-TUMOR; 1-NITROACRIDINES; GROWTH-INHIBITORY-ACTIVITY; SELECTIVE TOXICITY; BACTERIAL-CELLS; SIDE-CHAIN; NITRACRINE; RING; DERIVATIVES; LEDAKRIN;
D O I
10.1016/j.bmcl.2011.03.021
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
The synthesis of a number of new benzothiopyrano[4,3,2-cd] isoindole aminoderivatives designed as structural analogues of the key metabolite of the anticancer agent Ledacrine ( nitracrine) and their in vitro cytotoxic activity evaluation against HCT-116, MES-SA, and MES-SA/Dx cancer cell lines is reported. The majority of the derivatives possessed noticeable cytotoxicity in a low mu M range indicating an interesting structure-activity relationship. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3110 / 3112
页数:3
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