| Literature DB >> 23127889 |
Jiamin Gu1, Upendra Rao Anumala, Fabio Lo Monte, Thomas Kramer, Roland Heyny von Haußen, Jana Hölzer, Valérie Goetschy-Meyer, Gerhard Mall, Ingrid Hilger, Christian Czech, Boris Schmidt.
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 ß-amyloid (Aß) 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 (IC(50) values of 5.1 and 1.4 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.Entities:
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Year: 2012 PMID： 23127889 DOI： 10.1016/j.bmcl.2012.09.109
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823