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Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells

Breast cancer represents the most frequently diagnosed malignancy in women worldwide. Various therapeutics are currently used in order to halt the progression of breast tumor, even though certain side effects may limit the beneficial effects. In recent years, many efforts have been addressed to the...

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Autores principales: Iacopetta, Domenico, Lappano, Rosamaria, Mariconda, Annaluisa, Ceramella, Jessica, Sinicropi, Maria Stefania, Saturnino, Carmela, Talia, Marianna, Cirillo, Francesca, Martinelli, Fabio, Puoci, Francesco, Rosano, Camillo, Longo, Pasquale, Maggiolini, Marcello
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7589783/
https://www.ncbi.nlm.nih.gov/pubmed/33096835
http://dx.doi.org/10.3390/ijms21207797
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author Iacopetta, Domenico
Lappano, Rosamaria
Mariconda, Annaluisa
Ceramella, Jessica
Sinicropi, Maria Stefania
Saturnino, Carmela
Talia, Marianna
Cirillo, Francesca
Martinelli, Fabio
Puoci, Francesco
Rosano, Camillo
Longo, Pasquale
Maggiolini, Marcello
author_facet Iacopetta, Domenico
Lappano, Rosamaria
Mariconda, Annaluisa
Ceramella, Jessica
Sinicropi, Maria Stefania
Saturnino, Carmela
Talia, Marianna
Cirillo, Francesca
Martinelli, Fabio
Puoci, Francesco
Rosano, Camillo
Longo, Pasquale
Maggiolini, Marcello
author_sort Iacopetta, Domenico
collection PubMed
description Breast cancer represents the most frequently diagnosed malignancy in women worldwide. Various therapeutics are currently used in order to halt the progression of breast tumor, even though certain side effects may limit the beneficial effects. In recent years, many efforts have been addressed to the usefulness of natural compounds as anticancer agents due to their low toxicity. Resveratrol, a stilbene found in grapes, berries, peanuts and soybeans, has raised a notable interest for its antioxidant, anti-inflammatory, and antitumor properties. Here, we report the design, the synthesis and the characterization of the anticancer activity of a small series of imino N-aryl-substituted compounds that are analogues of resveratrol. In particular, the most active compound, named 3, exhibited anti-tumor activity in diverse types of breast cancer cells through the inhibition of the human topoisomerase II and the induction of apoptotic cell death. Therefore, the abovementioned compound maybe considered as a promising agent in more comprehensive treatments of breast cancer.
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spelling pubmed-75897832020-10-29 Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells Iacopetta, Domenico Lappano, Rosamaria Mariconda, Annaluisa Ceramella, Jessica Sinicropi, Maria Stefania Saturnino, Carmela Talia, Marianna Cirillo, Francesca Martinelli, Fabio Puoci, Francesco Rosano, Camillo Longo, Pasquale Maggiolini, Marcello Int J Mol Sci Article Breast cancer represents the most frequently diagnosed malignancy in women worldwide. Various therapeutics are currently used in order to halt the progression of breast tumor, even though certain side effects may limit the beneficial effects. In recent years, many efforts have been addressed to the usefulness of natural compounds as anticancer agents due to their low toxicity. Resveratrol, a stilbene found in grapes, berries, peanuts and soybeans, has raised a notable interest for its antioxidant, anti-inflammatory, and antitumor properties. Here, we report the design, the synthesis and the characterization of the anticancer activity of a small series of imino N-aryl-substituted compounds that are analogues of resveratrol. In particular, the most active compound, named 3, exhibited anti-tumor activity in diverse types of breast cancer cells through the inhibition of the human topoisomerase II and the induction of apoptotic cell death. Therefore, the abovementioned compound maybe considered as a promising agent in more comprehensive treatments of breast cancer. MDPI 2020-10-21 /pmc/articles/PMC7589783/ /pubmed/33096835 http://dx.doi.org/10.3390/ijms21207797 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
Iacopetta, Domenico
Lappano, Rosamaria
Mariconda, Annaluisa
Ceramella, Jessica
Sinicropi, Maria Stefania
Saturnino, Carmela
Talia, Marianna
Cirillo, Francesca
Martinelli, Fabio
Puoci, Francesco
Rosano, Camillo
Longo, Pasquale
Maggiolini, Marcello
Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title_full Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title_fullStr Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title_full_unstemmed Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title_short Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells
title_sort newly synthesized imino-derivatives analogues of resveratrol exert inhibitory effects in breast tumor cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7589783/
https://www.ncbi.nlm.nih.gov/pubmed/33096835
http://dx.doi.org/10.3390/ijms21207797
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