New derivatives of 11-methyl-6-[2-(dimethylamino)ethyl]-6H-indolo[2,3-b]quinoline as cytotoxic DNA topoisomerase II inhibitors |
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Authors: | Wojciech Luniewski Joanna Wietrzyk Joanna Godlewska Marta Switalska Malgorzata Piskozub Wanda Peczynska-Czoch Lukasz Kaczmarek |
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Institution: | Pharmaceutical Research Institute, 8 Rydygiera St., Warszawa 01-793, Poland. |
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Abstract: | Novel indolo2,3-b]quinoline derivatives substituted at N-6 and C-2 or C-9 positions with (dimethylamino)ethyl chains linked to heteroaromatic core by ether, amide or amine bonds, were manufactured and evaluated in vitro for their cytotoxic activity against several cell lines of different origin including multidrug resistant sublines and tested for their ability to influence the cell cycle and inhibit topoisomerase II activity. It was found, that all compounds show cytotoxic activity against cell lines tested, including multidrug resistant LoVo/DX, MES-SA/DX5 and HL-60 sublines. The tested compounds induce the G(2)M phase cell cycle arrest in Jurkat cells, and inhibit topoisomerase II activity. |
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