Synthesis and evaluation of stilbene derivatives as a potential imaging agent of amyloid plaques
SCIE
SCOPUS
- Title
- Synthesis and evaluation of stilbene derivatives as a potential imaging agent of amyloid plaques
- Authors
- Hong, Myeng Chan; Kim, Yun Kyung; Choi, Jae Yong; Yang, Si Qiang; Rhee, Hakjune; Ryu, Young Hoon; Choi, Tae Hyun; Cheon, Gi Jeong; Il An, Gwang; Kim, Hye Yun; Kim, Youngsoo; Kim, Dong Jin; Lee, Jun-Seok; Chang, Young-Tae; Lee, Kyo Chul
- Date Issued
- 2010-11
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Abstract
- Fluorescence probes that can detect A beta (beta-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 A beta 40 fibrils in vitro. Four compounds exhibited more than sixfold intensity increase, and they were further analyzed for detail bindings and A beta 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 mu M. In AD mouse brain tissue, 42 selectively stained A beta plaque, more specifically peripheral regions of A beta plaque. This finding demonstrated its potential use as brain-imaging agents for AD studies. (C) 2010 Elsevier Ltd. All rights reserved.
- Keywords
- SOLID-PHASE SYNTHESIS; ALZHEIMERS-DISEASE; IN-VIVO; BRAIN; PROBES; PET; TANGLES; LIGANDS
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/50215
- DOI
- 10.1016/j.bmc.2010.06.044
- ISSN
- 0968-0896
- Article Type
- Article
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, vol. 18, no. 22, page. 7724 - 7730, 2010-11
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