Synthesis, characterization and tumor cell growth inhibition of new trans platinum complexes with phosphane derivatives

We have reported the synthesis and characterization of two new trans platinum complexes in the phosphane series, where the phosphane ligand is triphenylphosphine [P(Ph)3] and the group in the trans configuration is represented by chiral aliphatic amines, (racemic in complex 1 and S–NH2CH2CH(CH3)CH2CH3 in complex 2). The anti-proliferative activity detected in tumor cells treated with the two new complexes is more pronounced when the aliphatic amine is racemic compared to the S-enantiomer. Moreover, for both compounds, the activity is fast after cell exposure and, unlike that of cisplatin, virtually independent of the duration of cell challenge.

The use of bulky phosphane ligands in active trans platinum complexes leads to an increased cytotoxicity for tumor cells in vitro. Their hydrophobic properties might facilitate drug uptake and may be one of the causes of the increased cytotoxicity. They also produce a faster induction of cell death than cisplatin.Figure optionsDownload as PowerPoint slideHighlights
► trans-Pt(II) Complexes with phosphane as spectator ligands.
► Bulky ligands with hydrophobic properties.
► Increased cytotoxicity for tumor cells in vitro.