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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BlackWell Publishing Ltd
2015
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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 |
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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 |
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