In our study double substituted indolo[2,3-b]quinoline derivatives bearing (dialkylamino)alkyl chains at N-6 and C-2 or C-9 position were tested against various human tumor cell lines and their drug-resistant sublines: human colon cancer (LoVo) and doxorubicin-resistant LoVo/DX (P-gp-dependent, MRP-, LRP-dependent multidrug resistance),  uterine sarcoma (MES-SA) and MES-SA/DX5 (P-gp-dependent resistance to doxorubicin), human promyelocytic leukemia cell line (HL-60) and HL-60/MX2 (P-gp-independent and topoisomerase II-dependent resistance).

The results of our investigations showed that all these compounds were able to overcome the barrier of P-gp-dependent drug resistance. The most effective of the all tested diubstituted indolo[2,3-b]quinoline derivatives were derivatives substituted in position C-2. The tested compounds did not overcome the barrier of topoisomerase II-dependent drug resistance. Only compound ISS-101 showed ability to overcome the barrier of drug resistance against human promyelocytic leukemia cell line.

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