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The development of metal-based anticancer compounds mainly focused on cytotoxic platinum compounds [1, 2]; however, recently attention shifted to the development of non-platinum anticancer drugs and it was shown that the ruthenium-based compounds could be clinical alternative of platinum drugs. The tumor specificity of ruthenium compounds can be influence by ligand sphere around metal atom. Addition of Ru part to the targeting biologically active organic molecules can strongly increase anticancer properties. 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 involved in the cell proliferation. This presentation will focus on the hybrid compounds based on lonidamine and bexarotene tethered to the ruthenium unit via an imidazole group. Ru(II) and Ru(III) compounds found to be highly cytotoxic against number of the human cancer cell lines.