Benzodifurans for biomedical applications: BZ4, a selective anti-proliferative and anti-amyloid lead compound

Author:

Vicidomini Caterina1,Cioffi Federica2,Broersen Kerensa2,Roviello Valentina3,Riccardi Claudia4,Montesarchio Daniela4,Capasso Domenica5,Gaetano Sonia Di1,Musumeci Domenica14,Roviello Giovanni N1

Affiliation:

1. CNR, Institute of Biostructure & Bioimaging, Via Mezzocannone site & Headquarters, 80134 Naples, Italy

2. Nanobiophysics, Faculty of Science & Technology (TNW), Technical Medical Centre, University of Twente, The Netherlands

3. Advanced Metrologic Service Center (CeSMA), University of Naples Federico II, Corso N.  Protopisani, 80146 Naples, Italy

4. Department of Chemical Sciences, University of Naples Federico II, Via Cintia 21, 80126 Naples, Italy

5. Department of Pharmacy, University of Naples Federico II, Via Mezzocannone 16, 80134 Naples, Italy

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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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