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.

New Di(heteroaryl)ethenes as Apoptotic Anti-proliferative Agents Towards Breast Cancer: Design, One-Pot Synthesis and In Vitro Evaluation

Naletova I.;Satriano C.;Barresi V.
Penultimo
;
Fortuna C. G.
2020

Abstract

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.
Cancer; Cytotoxicity; Di(heteroaryl)ethenes; Drug design; Subcellular localization
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/20.500.11769/420046
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