New derivatives of 11-methyl-6-[2-(dimethylamino)ethyl]-6H-indolo[2,3-b]quinoline as cytotoxic DNA topoisomerase II inhibitors

作者：Luniewski Wojciech; Wietrzyk Joanna; Godlewska Joanna; Switalska Marta; Piskozub Malgorzata; Peczynska Czoch Wanda; Kaczmarek Lukasz^*

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(19): 6103-6107.

DOI：10.1016/j.bmcl.2012.08.032

• Indolo[2,3-b]quinoline derivatives
• Neocryptolepine
• Cytotoxic activity
• Multidrug resistance
• Topoisomerase II inhibition

Novelindolo[2,3-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.

• 出版日期2012-10-1