Ruthenium complexes of 6,6'-dihydroxybipyridine form pro-drugs that can potentially have enhanced toxicity towards cancer cells versus normal cells.  The nature of this enhanced selectivity is based on the fact that cancer cells often exhibit lower pH values due to enhanced metabolism.  This can lead to a mechanism for selectivity because 6,6'-dihydroxybipyridine binds more weakly to a metal when the metal bound ligand is protonated (in its native state) in a cancerous cell.  In contrast, in a normal cell the metal bound ligand is more likely deprotonated and bound more strongly.  Ligand release is thus more favorable in the cancerous cells and can lead to selective toxicity.   Here we present our work on improving the properties of ruthenium anticancer pro-drugs by exploring the impact of the supporting ligands.  We are interested in tuning both the acid dissociation constants of the protic ligands and achieving enhanced targeting of cancer cells.

Ruthenium dihydroxybipyridine complexes are tumor activated prodrugs due to low pH and blue light induced ligand release

248th National Meeting (2014)

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