Monofunctional PtII Complexes Based on 8‐Aminoquinoline: Synthesis and Pharmacological Characterization

Abstract

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 µM 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.