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

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Abstract

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.

Graphical abstract

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).

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Acknowledgements

We thank the financial supports from the National Natural Science Foundation of China (Nos. 20231010, 20228102 and 30370351) and the Natural Science Foundation of Jiangsu Province (No. BK 2005209).

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