Targeting the cancer antioxidant system provides a viable route to therapeutic development in that cancer cells have a reduced buffering capacity to Reactive Oxygen Species (ROS) accentuation by external stimuli. With this in mind, Au-containing <i>N-</i>Heterocyclic carbenes have been shown to irreversibly inhibit the selenoenzyme thioredoxin reductase (TrxR), the sole regulator of the biological antioxidant thioredoxin. In addition, several redox-active moieties such as ferrocene and quinones have been shown to accentuate exogenous ROS and driving it towards cell death. These two anti-proliferative moieties were fused to evaluate their anticancer properties. Several redox-active gold(I) complexes have been synthesized, and subjected to preliminary cytotoxicity studies. This talk will address the dual targeting approach of reducing ROS tolerance while increasing ROS production to promote cancer cell death.

Dual targeting redox-active gold(I) N-Heterocyclic carbene complexes: A new approach to cancer treatment

253rd National Meeting (2017)

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