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

ACS Medicinal Chemistry Letters
2013.0

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).

Knowledge Graph

Similar Paper

A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases
ACS Medicinal Chemistry Letters 2013.0
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-β
Bioorganic & Medicinal Chemistry Letters 2009.0
Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer’s disease
Bioorganic & Medicinal Chemistry Letters 2013.0
New phenylaniline derivatives as modulators of amyloid protein precursor metabolism
Bioorganic & Medicinal Chemistry 2018.0
Novel Fluorinated 8-Hydroxyquinoline Based Metal Ionophores for Exploring the Metal Hypothesis of Alzheimer’s Disease
ACS Medicinal Chemistry Letters 2015.0
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer’s disease
Bioorganic & Medicinal Chemistry 2020.0
Disassembly of preformed amyloid beta fibrils by small organofluorine molecules
Bioorganic & Medicinal Chemistry Letters 2011.0
Design, synthesis and evaluation of 2-arylethenyl- N -methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment
European Journal of Medicinal Chemistry 2017.0
Huprine–Tacrine Heterodimers as Anti-Amyloidogenic Compounds of Potential Interest against Alzheimer’s and Prion Diseases
Journal of Medicinal Chemistry 2012.0
Synthesis and evaluation of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) as effective inhibitor of metal-induced Aβ aggregation and antioxidant
Bioorganic & Medicinal Chemistry 2016.0