Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594275 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
We evaluated 2-styrylindolium derivatives (6-11) as novel and selective probes for neurofibrillary tangles (NFTs) on brain sections of AD patients. The staining experiments indicated that these compounds may bind selectively to NFTs in the presence of Ã-amyloid (AÃ) plaques. Cell free binding assays confirmed that 2-[2-[4-(1-pyrrolidinyl)phenyl]ethenyl]-1,3,3-trimethyl-3H-indolium iodide (9) and 2-[2-[4-(diethylamino)phenyl]ethenyl]-1-butyl-3,3-dimethyl-3H-indolium iodide (11) display excellent affinities to Tau-aggregates (IC50 values of 5.1 and 1.4Â nM, respectively) in the displacement of Thiazin Red R. These probes have good solubility in distilled water and low or no cytotoxicity in zebrafish embryo and liver hepatocellular carcinoma cell assays.
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Authors
Jiamin Gu, Upendra Rao Anumala, Fabio Lo Monte, Thomas Kramer, Roland Heyny von HauÃen, Jana Hölzer, Valérie Goetschy-Meyer, Gerhard Mall, Ingrid Hilger, Christian Czech, Boris Schmidt,