Cargando…

Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**

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 prop...

Descripción completa

Detalles Bibliográficos
Autores principales: Nardon, Chiara, Chiara, Federica, Brustolin, Leonardo, Gambalunga, Alberto, Ciscato, Francesco, Rasola, Andrea, Trevisan, Andrea, Fregona, Dolores
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BlackWell Publishing Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4420591/
https://www.ncbi.nlm.nih.gov/pubmed/25969817
http://dx.doi.org/10.1002/open.201402091
_version_ 1782369751754866688
author Nardon, Chiara
Chiara, Federica
Brustolin, Leonardo
Gambalunga, Alberto
Ciscato, Francesco
Rasola, Andrea
Trevisan, Andrea
Fregona, Dolores
author_facet Nardon, Chiara
Chiara, Federica
Brustolin, Leonardo
Gambalunga, Alberto
Ciscato, Francesco
Rasola, Andrea
Trevisan, Andrea
Fregona, Dolores
author_sort Nardon, Chiara
collection PubMed
description 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)Br(2)(PDT)] and [Au(III)Cl(2)(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)Br(2)(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)Br(2)(PDT)] is a promising antineoplastic agent that targets cellular components with crucial functions for the survival of tumor cells.
format Online
Article
Text
id pubmed-4420591
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher BlackWell Publishing Ltd
record_format MEDLINE/PubMed
spelling pubmed-44205912015-05-12 Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents** Nardon, Chiara Chiara, Federica Brustolin, Leonardo Gambalunga, Alberto Ciscato, Francesco Rasola, Andrea Trevisan, Andrea Fregona, Dolores ChemistryOpen Full Papers 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)Br(2)(PDT)] and [Au(III)Cl(2)(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)Br(2)(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)Br(2)(PDT)] is a promising antineoplastic agent that targets cellular components with crucial functions for the survival of tumor cells. BlackWell Publishing Ltd 2015-04 2015-02-19 /pmc/articles/PMC4420591/ /pubmed/25969817 http://dx.doi.org/10.1002/open.201402091 Text en © 2014 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made.
spellingShingle Full Papers
Nardon, Chiara
Chiara, Federica
Brustolin, Leonardo
Gambalunga, Alberto
Ciscato, Francesco
Rasola, Andrea
Trevisan, Andrea
Fregona, Dolores
Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title_full Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title_fullStr Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title_full_unstemmed Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title_short Gold(III)–pyrrolidinedithiocarbamato Derivatives as Antineoplastic Agents**
title_sort gold(iii)–pyrrolidinedithiocarbamato derivatives as antineoplastic agents**
topic Full Papers
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4420591/
https://www.ncbi.nlm.nih.gov/pubmed/25969817
http://dx.doi.org/10.1002/open.201402091
work_keys_str_mv AT nardonchiara goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT chiarafederica goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT brustolinleonardo goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT gambalungaalberto goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT ciscatofrancesco goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT rasolaandrea goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT trevisanandrea goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents
AT fregonadolores goldiiipyrrolidinedithiocarbamatoderivativesasantineoplasticagents