Numerous examples in recent literature and first results of our investigations reveal that the lowered toxicity of DiMIQ can be achieved by a construction of a conjugate composed of DiMIQ and amino acids or peptides. Also the strongly hydrophilic guanidinium group can increase the bioavailability of new conjugates, and it can modulate their cytotoxic activity, and can increase their selectivity.

Now, we designed and obtained a series of novel hybrid compounds composed of 5H-indolo[2,3-b]quinoline and the guanidinium group or a residue of a N-guanylamino acid. All the new conjugates displayed a high cytotoxic activity against cell lines: non-small cell lung cancer A549, breast cancer MCF-7, colon cancer LoVo, cervix carcinoma KB. The best compound (I) displays also >1000 – fold more potent cytotoxic activity against all the cancer cell lines than for normal mice fibroblasts BALB/3T3.

IC₅₀ - compound concentration leading to 50% inhibition of cell proliferation [μg/mL]

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