Abstract: Despite the clinical success and proven efficacies of the conventional platinum-based drugs cisplatin, carboplatin, and oxaliplatin, these drugs suffer from a number of challenges that limit their more widespread therapeutic potential. These limitations, including toxic side effects and susceptibility to cancer drug resistance mechanisms, have prompted researchers to explore alternative metal complexes as anticancer agents. In this presentation, an overview of our work on the development and understanding of rhenium-containing organometallic complexes as potential drug candidates is discussed. We will disclose our discovery that a wide range of rhenium(I) tricarbonyl complexes exhibit potent in vitro anticancer activity via diverse biological mechanisms of action. Furthermore, several classes of rhenium(I) tricarbonyl complexes that we have investigated undergo photochemical processes that can be harnessed to trigger cancer cell death selectively upon irradiation or can be used for imaging applications. For this class of compounds, we have carried out detailed biological studies to determine their mechanisms of action. Our results indicate that subtle structural modifications of these compounds can lead to significant changes in their biological properties. Lastly, in vivo studies will be presented, demonstrating that the potential of these compounds as anticancer drug candidates exists beyond in vitro cellular experiments.
