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The development of metal-based anticancer compounds traditionally based on cytotoxic platinum compounds [1]; however, in recent years there has been much of interest in the development of non-platinum anticancer drugs and it was shown that the ruthenium-based compounds could be clinical alternative of platinum drugs for the number of tumours The tumour specificity of ruthenium compounds can be influence by ligand sphere around metal atom. Linking Ru part to the targeting biologically active organic molecules can strongly increase anticancer properties [2,3]. Lonidamine is known to inhibit the aerobic glycolysis in cancer cells while simultaneously enhancing glycolysis in the normal cells. Bexarotene is agonist of the retinoid X receptor and specific against T-cell lymphoma. This presentation will focus on the hybrid complexes based on lonidamine and bexarotene tethered to the ruthenium unit via an imidazole group. Ru(II) compounds found to be highly cytotoxic against number of the human cancer cell lines. Importantly, lonidamine-modified complexes were remarkable active against brain cancer cell lines and the hybrid bexarotene-ruthenium compound, showed highly specific cytotoxicity against cancer cells.