ABSTRACT
This chapter describes the work that has been done towards understanding the biological chemistry and toward rational design and selection of Platinum (Pt) (IV) complexes as anticancer agents. An improved understanding of the chemical and pharmacological parameters affecting Pt(IV) complexes as drugs is helping to elucidate the mechanism of action of this class of complexes and will allow the rational design of future Pt(IV) agents. Lipophilicity, as measured by relative solubilities in water and an organic solvent or partitioning between the two solvents has been investigated as a property relevant to the activity of platinum complexes, particularly as one of the primary mechanisms of resistance to cisplatin is decreased drug accumulation. The interaction of biomolecules with Pt(IV) complexes in vitro has been extensively examined and reviewed elsewhere, and it is intended here to provide an overview of important interactions.
