Cancer is a leading cause of death in industrialized nations. Reactive oxygen species are elevated in cancers such as leukemia and renal cell carcinoma. Our group sought to synthesize DNA-modifying agents activated by reactive oxygen species, which would increase selectivity and retain high cytotoxicity. Cell studies confirm that our agents are over three times more selective for leukemia cancer cells than for normal blood cells. These agents contain a nucleophile tethered to an oxidizable hydroquinone. Due to the unique structure of the molecule, selective activation of the hydroquinone occurs in the presence of reactive oxygen which results in a highly reactive electrophilic molecule that adds to DNA. Therefore, design of clinically relevant and selective DNA damaging agents may be possible using an oxidatively activated strategy.

Derivation of hydroquinone to create selective oxidatively activated anticancer agents

246th National Meeting (2013)

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