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

Abstract

(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).

• Authors: 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
• Journal: ACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 4 Issue 2 Pg. 225-9 (Feb 14 2013) ISSN: 1948-5875 [Print] United States
• PMID: 24900645 (Publication Type: Journal Article)