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New Di(heteroaryl)ethenes as Apoptotic Anti‐proliferative Agents Towards Breast Cancer: Design, One‐Pot Synthesis and In Vitro Evaluation
Author(s) -
Bonaccorso Carmela,
Naletova Irina,
Satriano Cristina,
Spampinato Giorgia,
Barresi Vincenza,
Fortuna Cosimo G.
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201903502
Subject(s) - apoptosis , cytotoxicity , flow cytometry , chemistry , in vitro , cell culture , cell growth , ic50 , furan , cancer cell lines , growth inhibition , stereochemistry , cancer cell , pharmacology , cancer research , biochemistry , cancer , biology , microbiology and biotechnology , organic chemistry , genetics
A new series of di(heteroaryl)ethenes was designed and synthesized by combining 5‐(dichlorophenyl)‐furan‐2‐yl and N‐substituted pyridinum moieties. All the synthesized compounds were screened for their anticancer activity against the MCF‐7 human breast cancer cell line. Most of the tested compounds showed moderate to potent cell growth inhibition; in particular, four of these exhibited promising cytotoxicity against this cell line, with IC50 values in the range of 0.30–0.005 μM. In addition, the potential mechanism of cell growth inhibition and apoptotic induction by these compounds was investigated by using flow cytometry and confocal microscopy. Based on these results, we identified a new and alternative class of anticancer agents that have the potential to be developed as leads.