ИСТИНА

The introduction of biologically active organic ligands into the ruthenium coordination sphere makes it possible to adjust the profile of antiproliferative activity and pharmacokinetic parameters, for example, water-solubility of potential drug candidates. Within the framework of this work, binuclear complexes of Ru(II) with imidazole ligands containing a fragment of biologically active pyridones maltol, ethylmaltol, and allomaltol were obtained. This work is devoted to the synthesis and detailed physicochemical and biological studies of water-soluble ruthenium binuclear complexes with high antiproliferative activity in in vitro. For the obtained compounds, the values of antiproliferative activity were determined in in vitro MTT tests on a small library of human cancer cell lines, and structure-activity analysis was carried out, the lead-compounds were selected, for which the ability to induce apoptosis of tumor cells and the caspase activation was studied.