Benzodifuran Derivatives as Potential Antiproliferative Agents: Possible Correlation between Their Bioactivity and Aggregation Properties. Issue 2 (29th November 2016)

• Record Type: Journal Article
• Authors: Musumeci, Domenica; Roviello, Giovanni N.; Rigione, Giuseppina; Capasso, Domenica; Di Gaetano, Sonia; Riccardi, Claudia; Roviello, Valentina; Montesarchio, Daniela
• Is Part Of: ChemPlusChem. Volume 82:Issue 2(2017)
• Page Start: 251
• Page End: 260
• Publication Date: 2016-11-29
• Subjects: antiproliferation -- benzodifurans -- dynamic light scattering -- nanoaggregates -- UV/Vis spectroscopy; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/cplu.201600547
• Languages: English
• ISSNs: 2192-6506

Abstract

Abstract: To further explore the properties and bioactivity of benzodifurans, three compounds in this class were synthesised and characterised using spectroscopic and spectrometric techniques, as well as SEM and thermogravimetric analysis. The synthesised compounds showed interesting antiproliferative activity on different human cancer cells (HeLa, Hep‐G2, WM266), whereas no relevant cytotoxic effect was observed on healthy control cells. To study the possible mechanism of action of the benzodifurans, their ability to bind various model DNA systems, their aggregation properties, and their ability to bind biologically relevant metal ions was evaluated. The molecules were found to form monodisperse nanoaggregates stable at physiological temperature, which are likely related to the observed bioactivity. Abstract : The more, the better ! Three benzodifuran derivatives were synthesized, characterized and tested for antiproliferative activity (see figure). They showed interesting cytotoxic effects on human cancer cell lines, with no significant effect on healthy cells. In preliminary efforts to determine the mechanism responsible for their activity, the molecules were found to form monodisperse nanoaggregates stable at physiological temperature, which are likely related to the observed bioactivity.