Benzodifurans for biomedical applications: BZ4, a selective anti-proliferative and anti-amyloid lead compound. (25th February 2019)

• Record Type: Journal Article
• Authors: Vicidomini, Caterina; Cioffi, Federica; Broersen, Kerensa; Roviello, Valentina; Riccardi, Claudia; Montesarchio, Daniela; Capasso, Domenica; Gaetano, Sonia Di; Musumeci, Domenica; Roviello, Giovanni N
• Is Part Of: Future medicinal chemistry. Volume 11:Number 4(2019)
• Page Start: 285
• Page End: 302
• Publication Date: 2019-02-25
• Subjects: anti-amyloid -- anticancer -- synthesis; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc-2018-0473
• Languages: English
• ISSNs: 1756-8919

Abstract

Aim: Our goal is to evaluate benzodifuran-based scaffolds for biomedical applications.Methodology: We here explored the anticancer and anti-amyloid activities of a novel compound (BZ4) in comparison with other known benzodifuran analogs, previously studied in our group, and we have explored its ability to interact with different DNA model systems.Results: BZ4 shows antiproliferative activity on different cancer cells; does not affect noncancerous control cells and alters the aggregation properties of β-amyloid, as ascertained by circular dichroism, fluorescence spectroscopy and scanning electron microscopy analysis. An overall, qualitative picture on the mechanistic aspects related to the biological activities is discussed in light of the dynamic light scattering, UV, circular dichroism and fluorescence data, as well as of the metal ion-binding properties of BZ4. Graphical abstract: