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Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation
Cited 59 time in
Web of Science
Cited 62 time in Scopus
- Authors
- Issue Date
- 2008-09-17
- Publisher
- Elsevier
- Citation
- Bioorganic & Medicinal Chemistry Letters 2008, 18(20), 5591-5593
- Keywords
- Alzheimer Disease/drug therapy/metabolism ; Amyloid beta-Protein/antagonists & inhibitors/*chemistry ; Benzofurans/*chemical synthesis/pharmacology ; Benzoxazoles/chemistry ; Chemistry, Pharmaceutical/*methods ; Curcumin/chemical synthesis/pharmacology ; Drug Design ; Electrons ; Humans ; Inhibitory Concentration 50 ; Models, Chemical ; Peptide Fragments/*antagonists & inhibitors/chemistry ; Structure-Activity Relationship ; Styrenes/*chemical synthesis/pharmacology ; Thiazoles/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
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