Platinum(0)-η2-1,2-(E)ditosylethene Complexes Bearing Phosphine, Isocyanide and N-Heterocyclic Carbene Ligands: Synthesis and Cytotoxicity towards Ovarian and Breast Cancer Cells

Author:

Compagno Nicola1,Piccolo Rachele1,Bortolamiol Enrica1ORCID,Demitri Nicola2,Rizzolio Flavio13ORCID,Visentin Fabiano1,Scattolin Thomas4ORCID

Affiliation:

1. Department of Molecular Sciences, Nanosystems Università Ca’ Foscari, Campus Scientifico, Via Torino 155, 30174 Venezia, Italy

2. Area Science Park Elettra-Sincrotrone Trieste, S.S. 14 Km 163.5, Basovizza, 34149 Trieste, Italy

3. Pathology Unit, Department of Molecular Biology and Translational Research, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, Via Franco Gallini 2, 33081 Aviano, Italy

4. Dipartimento di Scienze Chimiche, Università degli Studi di Padova, Via Marzolo 1, 35131 Padova, Italy

Abstract

A wide range of platinum(0)-η2-(E)-1,2-ditosylethene complexes bearing isocyanide, phosphine and N-heterocyclic carbene ancillary ligands have been prepared with high yields and selectivity. All the novel products underwent thorough characterization using spectroscopic techniques, including NMR and FT-IR analyses. Additionally, for some compounds, the solid-state structures were elucidated through X-ray diffractometry. The synthesized complexes were successively evaluated for their potential as anticancer agents against two ovarian cancer cell lines (A2780 and A2780cis) and one breast cancer cell line (MDA-MB-231). The majority of the compounds displayed promising cytotoxicity within the micromolar range against A2780 and MDA-MB-231 cells, with IC50 values comparable to or even surpassing those of cisplatin. However, only a subset of compounds was cytotoxic against cisplatin-resistant cancer cells (A2780cis). Furthermore, the assessment of antiproliferative activity on MRC-5 normal cells revealed certain compounds to exhibit in vitro selectivity. Notably, complexes 3d, 6a and 6b showed low cytotoxicity towards normal cells (IC50 > 100 µM) while concurrently displaying potent cytotoxicity against cancer cells.

Funder

Fondazione AIRC per la Ricerca sul Cancro

Publisher

MDPI AG

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