Cargando…
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...
Autores principales: | , , , , , , , , , , , , |
---|---|
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 |
_version_ | 1783600658595708928 |
---|---|
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. |
format | Online Article Text |
id | pubmed-7589783 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT iacopettadomenico newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT lappanorosamaria newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT maricondaannaluisa newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT ceramellajessica newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT sinicropimariastefania newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT saturninocarmela newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT taliamarianna newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT cirillofrancesca newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT martinellifabio newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT puocifrancesco newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT rosanocamillo newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT longopasquale newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells AT maggiolinimarcello newlysynthesizediminoderivativesanaloguesofresveratrolexertinhibitoryeffectsinbreasttumorcells |