ИСТИНА

The increasing interest in the biological behavior of ruthenium-based anticancer compounds strongly deals with their lower general toxicity compared to known platinum drugs and their specific transport inside cells and cellular uptake [1]. Nowadays ruthenium complex KP1339 is currently in phase II clinical trials as anticancer drug candidate and organometallic compound RAPTA-C, is progressing towards clinical trials. It was shown, that the ligands strongly influences anticancer and antimetastatic properties of organometallic ruthenium compounds [2]. Thus, the tumor specificity can be tuned by attachment of Ru moiety to the cancer related enzymes inhibitors. This presentation will focus on synthesis and characterization of ligands and hybrid ruthenium compounds based on imidazole modified Lonidamine and Bexarotene. Lonidamine inhibitor of mitochondrial bound hexokinase and known to specifically interfere with aerobic glycolysis in the cancer cells. Bexarotene act as agonist of the retinoid X receptor and specific against T-cell lymphoma. Ligands and ruthenium compounds shows nano-molar cytotoxicity in the MTT test and notably more active against number of the human cancer cell lines compare to Lonidamine and Bexarotene. Moreover lonidamine-modified complexes are remarkably active against brain cancer cell lines.