Enhancement of Aqueous Solubility and Stability Employing a Trans Acetate Axis in Trans Planar Amine Platinum Compounds while Maintaining the Biological Profile

A general approach to solubilization and possible in vivo activation of the transplatinum geometry is presented. The synthesis and characterization of new water-soluble cytotoxic transplatinum compounds are described. Use of acetate ligands (and carboxylate ligands in general) in trans-[Pt(OAc)2(L)(L‘)] results in significantly enhanced aqueous solubility and chemical stability in comparison to the parent dichlorides. The new compounds are the first cytotoxic transplatinum compounds containing an N2O2 donor set, similar to carboplatin and oxaliplatin.