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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7667-71. doi: 10.1016/j.bmcl.2012.09.109. Epub 2012 Oct 6.

2-Styrylindolium based fluorescent probes visualize neurofibrillary tangles in Alzheimer's disease.

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Clemens Schöpf Institute of Chemistry and Biochemistry, Technische Universität Darmstadt, Petersenstrasse 22, Darmstadt 64287, Germany.


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.

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