Antitumor active monofunctional platinum(II) complexes: Synthesis, structural characterization and reactivity towards biomolecules

Monofunctional platinum(II) complexes represent a class of antitumor agents that do not obey the classical structure–activity relationships. We report herein two novel platinum(II) complexes [PtL1Cl] (L1 = l-valine-N-8-quinolylamide) and [PtL2Cl] (L2 = l-leucine-N-8-quinolylamide) in which Cl− acts as the only potential leaving group. These complexes showed comparable cytotoxicity to cisplatin against the murine leukemia cell line (P-388) and the human non-small-cell lung cancer cell line (A-549), and could potentially form monofunctional adducts with DNA.

The platinum(II) complexes of l-valine-N-8-quinolylamide and l-leucine-N-8-quinolylamide were shown to bind to DNA with high affinity and demonstrated comparable cytotoxicity to cisplatin against the murine leukemia cell line (P-388) and the human non-small-cell lung cancer cell line (A-549).Figure optionsDownload as PowerPoint slide