Synthesis and evaluation of stilbene derivatives as a potential imaging agent of amyloid plaques

Title
Synthesis and evaluation of stilbene derivatives as a potential imaging agent of amyloid plaques
Authors
Myeng Chan Hong김윤경Jae Yong ChoiSi Qiang YangHakjune RheeYoung Hoon RyuTae Hyun ChoiGi Jeong CheonGwang Il An김혜연김영수김동진이준석장영태이교철
Keywords
알츠하이머; Alzheimer’s disease (AD); amyloid; imaging agent; 신약; β-Amyloid peptide (Aβ); Fluorescence imaging probe
Issue Date
2010-11
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 18, NO 22, 7724-7730
Abstract
Fluorescence probes that can detect Aβ (β-amyloid peptide) plaque are important tools for diagnosis of Alzheimer’s disease (AD), and 4-N-methylamino-4'-hydroxystilbene (SB-13) is one of the promising candidate molecules. We report here the synthesis of SB-13 derivatives that consist of various electron donating/ withdrawing moieties and distinct size of N-substituents. The synthesized compounds were screened for detection of Aβ40 fibrils in vitro. Four compounds exhibited more than sixfold intensity increase, and they were further analyzed for detail bindings and Aβ plaque imaging. Among these molecules, compound 42 meets two critical requirements for imaging agent; high fluorescence responsiveness and strong binding affinity. This compound showed more than 25-fold increase with the dissociation constant of 1.13 ± 0.37 lM. In AD mouse brain tissue, 42 selectively stained Ab plaque, more specifically peripheral regions of Ab plaque. This finding demonstrated its potential use as brain-imaging agents for AD studies.
URI
https://pubs.kist.re.kr/handle/201004/38855
ISSN
0968-0896
Appears in Collections:
KIST Publication > Article
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