Ruthenium-carbohydrate conjugates as cytostatic drugs with an enhanced selectivity to cancer cells

Grant Agency
Grant Agency of the Czech Republic
Organometallic Catalysis.
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Cancer diseases are among the major causes of death worldwide. The diseases are characteristic by a fast cell proliferation, which costs a large amount of energy. Since the energy production from D-glucose is inefficient, the cancer cells display an order higher D-glucose uptake in comparison to normal ones. The project goal is to connect ruthenium cytostatics with D-glucose (as well as other carbohydrates undergoing active transport into cells), which will lead to its selective transfer into cancer cells. We plan to synthesize a series of ruthenium complexes bearing coordinated arene ligand connected to a carbohydrate framework. D-glucose derivatives monobenzylated in specific C1-C6 positions will be used as arene ligands. Cytotoxic activity of the prepared compounds will be tested towards selected cancer and normal cell lines, while the echanism of action of the most active species will be evaluated. Electrochemical methods will be used for determination of intracellular metal complexes uptake. A rational design of new selective drug candidates will be the main project outcome.

Mgr. PINKAS Jiří Ph.D.

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