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
- Author
- 이학준
- Keywords
- Alzheimer's disease (AD); beta-Amyloid peptide (A beta); Fluorescence imaging probe
- Issue Date
- 2010-11
- Publisher
- Pergamon Press Ltd.
- Citation
- Bioorganic and Medicinal Chemistry, v. 18, NO. 22, Page. 7724-7730
- 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.
- URI
- https://www.sciencedirect.com/science/article/pii/S0968089610005729?via%3Dihubhttps://repository.hanyang.ac.kr/handle/20.500.11754/183980
- ISSN
- 0968-0896;1464-3391
- DOI
- 10.1016/j.bmc.2010.06.044
- Appears in Collections:
- COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
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