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

Abstract

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.

• Authors: Domenico Iacopetta, Rosamaria Lappano, Annaluisa Mariconda, Jessica Ceramella, Maria Stefania Sinicropi, Carmela Saturnino, Marianna Talia, Francesca Cirillo, Fabio Martinelli, Francesco Puoci, Camillo Rosano, Pasquale Longo, Marcello Maggiolini
• Journal: International journal of molecular sciences (Int J Mol Sci) Vol. 21 Issue 20 (Oct 21 2020) ISSN: 1422-0067 [Electronic] Switzerland
• PMID: 33096835 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Imines
• Poly-ADP-Ribose Binding Proteins
• Topoisomerase I Inhibitors
• DNA Topoisomerases, Type I
• TOP1 protein, human
• DNA Topoisomerases, Type II
• TOP2A protein, human
• Resveratrol

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Biological Availability
• Breast Neoplasms (drug therapy)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• DNA Topoisomerases, Type I (chemistry, metabolism)
• DNA Topoisomerases, Type II (chemistry)
• Female
• HEK293 Cells
• Humans
• Imines (chemistry)
• Molecular Docking Simulation
• Poly-ADP-Ribose Binding Proteins (antagonists & inhibitors, chemistry)
• Resveratrol (analogs & derivatives, pharmacology)
• Topoisomerase I Inhibitors (chemistry, pharmacology)