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Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation

Cited 55 time in Web of Science Cited 57 time in Scopus
Authors
Byun, Ji Hun; Kim, HyeYun; Kim, YoungSoo; Mook-Jung, Inhee; Kim, Dong Jin; Lee, Won Koo; Yoo, Kyung Ho
Issue Date
2008-09-17
Publisher
Elsevier
Citation
Bioorganic & Medicinal Chemistry Letters 2008, 18(20), 5591-5593
Keywords
Alzheimer Disease/drug therapy/metabolismAmyloid beta-Protein/antagonists & inhibitors/*chemistryBenzofurans/*chemical synthesis/pharmacologyBenzoxazoles/chemistryChemistry, Pharmaceutical/*methodsCurcumin/chemical synthesis/pharmacologyDrug DesignElectronsHumansInhibitory Concentration 50Models, ChemicalPeptide Fragments/*antagonists & inhibitors/chemistryStructure-Activity RelationshipStyrenes/*chemical synthesis/pharmacologyThiazoles/chemistry
Abstract
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Abeta fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Abeta fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC(50)=0.07 and 0.08 microM, respectively) than those of Curcumin (IC(50)=0.80 microM) and IMSB (IC(50)=8.00 microM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
ISSN
1464-3405 (Electronic)
Language
English
URI
http://www.sciencedirect.com/science?_ob=MImg&_imagekey=B6TF9-4TC34V1-3-9&_cdi=5221&_user=168665&_orig=search&_coverDate=10%2F15%2F2008&_sk=999819979&view=c&wchp=dGLzVzz-zSkWA&md5=6ffffd80447af670bc66a64bbc6050bc&ie=/sdarticle.pdf

https://hdl.handle.net/10371/67455
DOI
https://doi.org/10.1016/j.bmcl.2008.08.111
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College of Medicine/School of Medicine (의과대학/대학원)Dept. of Biochemistry & Molecular Biology (생화학교실)Journal Papers (저널논문_생화학교실)
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