4.5 Article

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

Journal

FUTURE MEDICINAL CHEMISTRY
Volume 11, Issue 4, Pages 285-302

Publisher

FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0473

Keywords

anti-amyloid; anticancer; synthesis

Funding

  1. ZonMw Memorabel
  2. Italian Association for Cancer Research (AIRC) [17037]
  3. Ministero dell'Istruzione, dell'Universita e della Ricerca (MIUR) [PON03PE_00060_4]

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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 beta-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.

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