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.
Monofunctional Pt(II) complexes based on 8-aminoquinoline: synthesis and pharmacological characterization / G. Facchetti, N. Ferri, Lupo Maria Giovanna, G.A. Lucchini, I. Rimoldi. - In: EUROPEAN JOURNAL OF INORGANIC CHEMISTRY. - ISSN 1099-0682. - 2019:29(2019 Aug 07), pp. 3389-3395. [10.1002/ejic.201900644]
Monofunctional Pt(II) complexes based on 8-aminoquinoline: synthesis and pharmacological characterization
G. FacchettiPrimo
;N. Ferri
Secondo
;G.A. LucchiniPenultimo
;I. Rimoldi
Ultimo
2019
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 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.File | Dimensione | Formato | |
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