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Synthesis and biological evaluation of indole-chalcone derivatives as β-amyloid imaging probe

Synthesis and biological evaluation of indole-chalcone derivatives as β-amyloid imaging probe,10.1016/j.bmcl.2010.12.045,Bioorganic & Medicinal Chemis

Synthesis and biological evaluation of indole-chalcone derivatives as β-amyloid imaging probe   (Citations: 1)
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A series of chaclone derivatives containing an indole moiety were evaluated in competitive binding assays with Aβ1-42 aggregates versus [125I]IMPY. The affinity of these compounds ranged from 4.46 to >1008nM, depending on the substitution on the phenyl ring. Fluorescent staining in vitro showed that one compound with a N,N-dimethylamino group intensely stained Aβ plaques within brain sections of AD transgenic mice. The radioiodinated probe [125I]-(E)-3-(1H-indol-5-yl)-1-(4-iodophenyl)prop-2-en-1-one, [125I]4, was prepared and autoradiography in sections of brain tissue from an animal model of AD showed that it labeled Aβ plaques specifically. However, experiments with normal mice indicated that [125I]4 exhibited a low uptake into the brain in vivo (0.41% ID/g at 2min). Additional chemical modifications of this indole-chalcone structure may lead to more useful imaging agents for detecting β-amyloid plaques in the brains of AD patients.
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