A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases

  • Matteo Staderini, Suzana Aulić, Manuela Bartolini, Hoang Ngoc Ai Tran, Víctor González-Ruiz, Daniel I. Pérez, Nieves Cabezas, Ana Martínez, M. Antonia Martín, Vincenza Andrisano, Giuseppe Legname, J. Carlos Menéndez, Maria Laura Bolognesi
  • ACS Medicinal Chemistry Letters, February 2013, American Chemical Society (ACS)
  • DOI: 10.1021/ml3003605

What is it about?

(E)-6-Methyl-4′-amino-2-styrylquinoline (3) is a small molecule with the proper features to potentially diagnose, deliver therapy and monitor response to therapy in protein misfolding diseases. These features include compound fluorescent emission in the NIR region and its ability to interact with both Aβ and prion fibrils, staining them with high selectivity. Styrylquinoline 3 also inhibits Aβ self-aggregation in vitro and prion replication in the submicromolar range in a cellular context. Furthermore, it is not toxic and is able to cross the blood brain barrier in vitro (PAMPA test).

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http://dx.doi.org/10.1021/ml3003605

The following have contributed to this page: M. Antonia Martín