ArticleBioorganic & medicinal chemistry letters2018
Design, synthesis, and in vitro evaluation of quinolinyl analogues for α-synuclein aggregation.
Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Development of Positron Emission Tomography Radiotracers for Imaging α-Synuclein Aggregates.Cells · 2025Review
- Ligands for Protein Fibrils of Amyloid-β, α-Synuclein, and Tau.Chemical reviews · 2025Review
- A review of the current research on in vivo and in vitro detection for alpha-synuclein: a biomarker of Parkinson's disease.Analytical and bioanalytical chemistry · 2023Review
- Structure-Activity Relationships of Styrylquinoline and Styrylquinoxaline Derivatives as α-Synuclein Imaging Probes.ACS medicinal chemistry letters · 2022Article
- Steroid-Quinoline Hybrids for Disruption and Reversion of Protein Aggregation Processes.ACS medicinal chemistry letters · 2022Article
- Alpha-Synuclein PET Tracer Development-An Overview about Current Efforts.Pharmaceuticals (Basel, Switzerland) · 2021Review
- [European journal of nuclear medicine and molecular imaging · 2021Article
- Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid.Molecules (Basel, Switzerland) · 2021Article
- Alpha Synuclein Fibrils Contain Multiple Binding Sites for Small Molecules.ACS chemical neuroscience · 2018Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
Here we report the synthesis and in vitro evaluation of 25 new quinolinyl analogues for α-synuclein aggregates. Three lead compounds were subsequently labeled with carbon-11 or fluorine-18 to directly assess their potency in a direct radioactive competitive binding assay ng both α-synuclein fibrils and tissue homogenates from Alzheimer's disease (AD) cases. The modest binding affinities of these three radioligands toward α-synuclein were comparable with results from the Thioflavin T fluorescence assay. However, all three ligand also showed modest binding affinity to the AD homogenates and lack selectivity for α-synuclein. The structure-activity relationship data from these 25 analogues will provide useful information for design and synthesis of new compounds for imaging α-synuclein aggregation.
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