A fluorescent styrylquinoline with combined therapeutic and diagnostic activities against alzheimer’s and prion diseases

Staderini, Matteo; Aulić, Suzana; Bartolini, Manuela; Tran, Hoang Ngoc Ai; González-Ruiz, Víctor; Pérez, Daniel I.; Martínez Gil, Ana; Andrisano, Vincenza; Legname, Giuseppe; Menéndez Ramos, José Carlos; Bolognesi, Maria Laura; Cabezas Baudot, Nieves; Martín Carmona, María Antonia

A fluorescent styrylquinoline with combined therapeutic and diagnostic activities against alzheimer’s and prion diseases

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Staderini-A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases-2013-ACS Medicinal Chemistry Letters.pdf (1.45 MB)

Official URL

https://doi.org/10.1021/ml3003605

Publication date

2013

Authors

González-Ruiz, Víctor

Menéndez Ramos, José Carlos

Publisher

ACS publications

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URI

https://hdl.handle.net/20.500.14352/99813

Citation

Staderini M, Aulić S, Bartolini M, Tran HNA, González-Ruiz V, Pérez DI, et al. A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases. ACS Med Chem Lett 2013;4:225–9. https://doi.org/10.1021/ml300360

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).