In our study disubstituted 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: human colon (LoVo), uterine (MES-SA), promyelocytic leukemia (HL-60), lung (A-549) and human melanoma (Hs294T), as well as normal mouse fibroblast cell line (BALB/3T3).

We found that all indoloquinolines showed cytotoxic activity against the cells of all cancer lines used. ID₅₀ values of tested compounds against the normal mouse fibroblast cell line (BALB/3T3) were comparable to the results obtained for the tumor cell lines. It suggests that the compounds show similar cytotoxic activity against normal and tumor cell lines.

The studied indoloquinolines were highly active against the cell of human promyelocytic leukemia (HL-60) and human uterine sarcoma cell line (MES-SA). The compound ISS-101 showed the highest of all the derivatives tested cytotoxic activity against the tumor and normal cell lines.

Table 1. Cytotoxic activity in vitro of indolo[2,3-b]quinolines against the cells of LoVo, HL-60 , MES-SA, A-549, MCF-7, Hs294T and BALB/3T3 cell lines.

Table2. Structures of disubstituted indolo[2,3-b]quinoline derivatives.

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