Monofunctional Pt(II) complexes based on 8-aminoquinoline: synthesis and pharmacological characterization

Among the heterocyclic compounds, 8-aminoquinoline and its derivatives have become important candidates for the preparation of new antiproliferative metallo-drugs. Here, we reported the synthesis and cytotoxicity evaluation of a series of platinum complexes using 8-aminoquinoline and its chiral 5,6,7,8-tetrahydro-derivatives as chelating ligands. In the proposed complexes, a differently and opportunely alkylated imidazole was used to prepare the corresponding monofunctional platinum complexes. The preliminary cytotoxicity evaluation was carried out on the highly aggressive MDA-MB-231, invasive and poorly differentiated triple-negative breast cancer (TNBC) cell line, furnishing a significant IC50 10.9 +/- 1.3 mu M for Pt-IV. This series of complexes revealed an induction of p53, interfering with the progression of the G0/G1 phase of the cell cycle.