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Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex

Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin...

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Autores principales: D’Errico, Stefano, Falanga, Andrea Patrizia, Capasso, Domenica, Di Gaetano, Sonia, Marzano, Maria, Terracciano, Monica, Roviello, Giovanni Nicola, Piccialli, Gennaro, Oliviero, Giorgia, Borbone, Nicola
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7407906/
https://www.ncbi.nlm.nih.gov/pubmed/32635488
http://dx.doi.org/10.3390/pharmaceutics12070627
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author D’Errico, Stefano
Falanga, Andrea Patrizia
Capasso, Domenica
Di Gaetano, Sonia
Marzano, Maria
Terracciano, Monica
Roviello, Giovanni Nicola
Piccialli, Gennaro
Oliviero, Giorgia
Borbone, Nicola
author_facet D’Errico, Stefano
Falanga, Andrea Patrizia
Capasso, Domenica
Di Gaetano, Sonia
Marzano, Maria
Terracciano, Monica
Roviello, Giovanni Nicola
Piccialli, Gennaro
Oliviero, Giorgia
Borbone, Nicola
author_sort D’Errico, Stefano
collection PubMed
description Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit in the molecular scaffold. The behavior of the synthesized complex with a double-strand DNA model was monitored by CD spectroscopy and compared with that of cisplatin and tubercidin. In addition, the cell viability was evaluated against HeLa, A375 and WM266 human cancer cell lines using the MTT test. Lastly, the results of the apoptotic assay (FITC Annexin V) performed on the HeLa cancer cell line are also reported.
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spelling pubmed-74079062020-08-12 Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex D’Errico, Stefano Falanga, Andrea Patrizia Capasso, Domenica Di Gaetano, Sonia Marzano, Maria Terracciano, Monica Roviello, Giovanni Nicola Piccialli, Gennaro Oliviero, Giorgia Borbone, Nicola Pharmaceutics Article Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit in the molecular scaffold. The behavior of the synthesized complex with a double-strand DNA model was monitored by CD spectroscopy and compared with that of cisplatin and tubercidin. In addition, the cell viability was evaluated against HeLa, A375 and WM266 human cancer cell lines using the MTT test. Lastly, the results of the apoptotic assay (FITC Annexin V) performed on the HeLa cancer cell line are also reported. MDPI 2020-07-04 /pmc/articles/PMC7407906/ /pubmed/32635488 http://dx.doi.org/10.3390/pharmaceutics12070627 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
D’Errico, Stefano
Falanga, Andrea Patrizia
Capasso, Domenica
Di Gaetano, Sonia
Marzano, Maria
Terracciano, Monica
Roviello, Giovanni Nicola
Piccialli, Gennaro
Oliviero, Giorgia
Borbone, Nicola
Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title_full Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title_fullStr Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title_full_unstemmed Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title_short Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex
title_sort probing the dna reactivity and the anticancer properties of a novel tubercidin-pt(ii) complex
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7407906/
https://www.ncbi.nlm.nih.gov/pubmed/32635488
http://dx.doi.org/10.3390/pharmaceutics12070627
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