Mononuclear tetraamineplatinum(II) complexes: Synthesis, anticancer activity, DNA binding, and cellular uptake

The synthesis of three bis[(tert-butoxy)carbonyl]-protected (tetramine)dich loroplatinum complexes 2a-c of formula cis-[PtCl2(LL)] and of their cationi c deprotected analogs 3a-c and their evaluation with respect to in vitro cy totoxicity, intramolecular stability, DNA binding, and cellular uptake is r eported. The synthesis comprises the complexation of K-2[PtCl4] With di-N-p rotected tetramines la-c to give 2a-c and subsequent acidolysis, yielding 3 a-c. The cytotoxicity of the complexes is in direct relation to the length of the polyamine. Complexes 3a-e display a significant higher affinity for CT DNA as well as for cellular DNA in A2780 cells than cisplatin.