Issue Date: May 21, 2012
Ruthenium Switches On To Kill Cancer Cells
Cisplatin [PtCl2(NH3)2], a widely used cancer drug, cross-links DNA to disrupt replication and transcription, thereby killing cancer cells. But cisplatin also attacks healthy cells, causing debilitating side effects. Chemists have now developed two ruthenium complexes that might reduce side effects: The complexes are inert and nontoxic in the dark, but when activated with light, they switch on their cancer-cell-killing ability and become more toxic than cisplatin (J. Am. Chem. Soc., DOI: 10.1021/ja3009677). Edith C. Glazer and colleagues at the University of Kentucky focused on octahedral ruthenium bipyridine complexes (one shown) that, because of steric strain, shed a ligand (red) when illuminated with blue-green light. These light-activated ruthenium complexes cross-link DNA, just as cisplatin does. The researchers found that the ruthenium complexes were up to 200 times as toxic in the light as in the dark, and after light activation they were up to three times as potent as cisplatin against tumor cells.
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