TY - JOUR
T1 - Newly synthesized imino-derivatives analogues of resveratrol exert inhibitory effects in breast tumor cells
AU - Iacopetta, Domenico
AU - Lappano, Rosamaria
AU - Mariconda, Annaluisa
AU - Ceramella, Jessica
AU - Sinicropi, Maria Stefania
AU - Saturnino, Carmela
AU - Talia, Marianna
AU - Cirillo, Francesca
AU - Martinelli, Fabio
AU - Puoci, Francesco
AU - Rosano, Camillo
AU - Longo, Pasquale
AU - Maggiolini, Marcello
N1 - Funding Information:
Acknowledgments: The authors acknowledge (i) the special award namely “Department of Excellence 2018-2022” (Italian Law 232/2016) to the Department of Pharmacy, Health and Nutritional Sciences of the University of Calabria (Arcavacata di Rende, Italy), (ii) PON Ricerca e Competitività 2007–2013 and the “Sistema Integrato di Laboratori per L’Ambiente—(SILA) PONa3_00341” for providing lab tools.
Publisher Copyright:
© 2020 by the authors.
Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020/10/2
Y1 - 2020/10/2
N2 - 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-arylsubstituted 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.
AB - 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-arylsubstituted 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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U2 - 10.3390/ijms21207797
DO - 10.3390/ijms21207797
M3 - Article
C2 - 33096835
AN - SCOPUS:85094617920
VL - 21
SP - 1
EP - 18
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
SN - 1661-6596
IS - 20
M1 - 7797
ER -