Ms. Robillard et al., Mononuclear tetraamineplatinum(II) complexes: Synthesis, anticancer activity, DNA binding, and cellular uptake, HELV CHIM A, 84(10), 2001, pp. 3023-3030
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.