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Molecules 2012, 17(4), 4252-4265; doi:10.3390/molecules17044252

(E)-5-Styryl-1H-indole and (E)-6-Styrylquinoline Derivatives Serve as Probes for β-Amyloid Plaques

*  and *
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
* Authors to whom correspondence should be addressed.
Received: 20 February 2012 / Revised: 28 March 2012 / Accepted: 29 March 2012 / Published: 10 April 2012
(This article belongs to the Section Medicinal Chemistry)
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We report the synthesis and biological evaluation of novel (E)-5-styryl-1H-indole and (E)-6-styrylquinoline derivatives as probes for imaging β-amyloid (Aβ) plaques. These derivatives showed binding affinities for Aβ1–40 aggregates with Ki values varying from 4.1 to 288.4 nM. (E)-5-(4-iodostyryl)-1H-indole (8) clearly stained Aβ plaques in the brain sections of Alzheimer’s disease (AD) model mice (APP/PS1). Furthermore, autoradiography for [125I]8 displayed intense and specific labeling of Aβ plaques in the brain sections mentioned above with low background. In biodistribution experiments using normal mice [125I]8 showed high initial brain uptake followed by rapid washout (4.27 and 0.64% ID/g at 2 and 30 min post injection, respectively). These findings suggests that [123I]8 may be a potential SPECT imaging agent for detecting Aβ plaques in AD brain.
Keywords: Alzheimer’s disease; β-amyloid plaques; binding affinity; imaging agent; SPECT Alzheimer’s disease; β-amyloid plaques; binding affinity; imaging agent; SPECT
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Yang, Y.; Jia, H.-M.; Liu, B.-L. (E)-5-Styryl-1H-indole and (E)-6-Styrylquinoline Derivatives Serve as Probes for β-Amyloid Plaques. Molecules 2012, 17, 4252-4265.

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