A new family of water-soluble, third generation antitumor platinum complexes

Article abstract of DOI:10.1021/jm00129a008

[1,1-Cyclobutanedicarboxylato(2-)-0,0'](1,3-dioxane-5,5-dimethanamine- ,N')platinum (II), 3a, a third generation, very water-soluble platinum complex, has been synthesized along with several of its analogues. All members of the new family contain a 1,3-dioxane or 1,3-dioxolane-1,3-diamine as their basic ligand, a moiety which contributes to their increased water solubility, and a bidentate acid ligand, which is responsible for their good stability. They were all easily crystallized and characterized by ¹H NMR and elemental analysis, and the parent complex 3a was further characterized by ¹³C NMR. Their very desirable physical properties combined with their broad spectrum of antitumor activity and reduced toxicity make them good candidates in further development.