title: Gold(III)-pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents.
abstract: Transition metals offer many possibilities in developing potent chemotherapeutic agents. They are endowed with a variety of oxidation states, allowing for the selection of their coordination numbers and geometries via the choice of proper ligands, leading to the tuning of their final biological properties. We report here on the synthesis, physico-chemical characterization, and solution behavior of two gold(III) pyrrolidinedithiocarbamates (PDT), namely [Au(III)Br2(PDT)] and [Au(III)Cl2(PDT)]. We found that the bromide derivative was more effective than the chloride one in inducing cell death for several cancer cell lines. [Au(III)Br2(PDT)] elicited oxidative stress with effects on the permeability transition pore, a mitochondrial channel whose opening leads to cell death. More efficient antineoplastic strategies are required for the widespread burden that is cancer. In line with this, our results indicate that [Au(III)Br2(PDT)] is a promising antineoplastic agent that targets cellular components with crucial functions for the survival of tumor cells.
authors.affiliation: Department of Chemical Sciences, University of Padova Via F. Marzolo 1, 35131, Padova, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Nardon
authors.affiliation: Department of Cardiac, Thoracic, and Vascular Sciences, University of Padova Via Giustiniani 2, 35128, Padova, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Chiara
authors.affiliation: Department of Chemical Sciences, University of Padova Via F. Marzolo 1, 35131, Padova, Italy.
authors.forename: Leonardo
authors.initials: L
authors.lastname: Brustolin
authors.affiliation: Department of Cardiac, Thoracic, and Vascular Sciences, University of Padova Via Giustiniani 2, 35128, Padova, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Gambalunga
authors.affiliation: Department of Biomedical Sciences, University of Padova Viale G. Colombo 3, 35131, Padova, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Ciscato
authors.affiliation: Department of Biomedical Sciences, University of Padova Viale G. Colombo 3, 35131, Padova, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Rasola
authors.affiliation: Department of Cardiac, Thoracic, and Vascular Sciences, University of Padova Via Giustiniani 2, 35128, Padova, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Trevisan
authors.affiliation: Department of Chemical Sciences, University of Padova Via F. Marzolo 1, 35131, Padova, Italy.
authors.forename: Dolores
authors.initials: D
authors.lastname: Fregona
keywords: antitumor; gold(III); mitochondrial permeability transition pore; pyrrolidinedithiocarbamates (PDT); reactive oxygen species (ROS)