Metal complexes can act as enzyme inhibitors. Gold complexes have attracted attention as potential alternatives to platinum drugs due to their anti-proliferative activity in human tumor cells. It has been suggested that the mechanism of action of these compounds involves inhibition of the selenoenzyme thioredoxin reductase (TrxR).Gallium(III) complexes exert anti-proliferative effects by inhibiting ribonucleotide reductase (RR), a key enzyme in DNA biosynthesis, which is involved in the conversion of ribonucleotides into deoxyribonucleotides.Gold(I) and gold(III) complexes with thiosemicarbazones (TSC) and bis(thiosemicarbazones) proved to be cytotoxic to human tumor cell lines and presented pro-apoptotic potential. The complexes inhibited TrxR's activity, indicating inhibition of TrxR to be part of their mechanism of action.Gallium(III) complexes with thiosemicarbazones and hydrazones (HDZ) exhibited cytotoxic activity against human tumor cell lines with apoptosis induction. Cytotoxicity could be due to inhibition of RR by both gallium(III) and the thiosemicarbazone or hydrazone ligand. 

Gold- and gallium-based anticancer drug candidates as potential enzyme inhibitors

243rd National Meeting (2012)

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