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
- Issue Date
- Nov-2010
- Publisher
- Pergamon Press Ltd.
- Keywords
- Alzheimer' s disease (AD); beta-Amyloid peptide (A beta); Fluorescence imaging probe
- Citation
- Bioorganic and Medicinal Chemistry, v.18, no.22, pp.7724 - 7730
- Indexed
- SCIE
SCOPUS
- Journal Title
- Bioorganic and Medicinal Chemistry
- Volume
- 18
- Number
- 22
- Start Page
- 7724
- End Page
- 7730
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/39355
- DOI
- 10.1016/j.bmc.2010.06.044
- ISSN
- 0968-0896
- 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.
- Files in This Item
-
Go to Link
- Appears in
Collections - COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY > DEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.