S-Space College of Medicine/School of Medicine (의과대학/대학원) Dept. of Biochemistry & Molecular Biology (생화학교실) Journal Papers (저널논문_생화학교실)
Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation
- Byun, Ji Hun; Kim, HyeYun; Kim, YoungSoo; Mook-Jung, Inhee; Kim, Dong Jin; Lee, Won Koo; Yoo, Kyung Ho
- Issue Date
- Bioorganic & Medicinal Chemistry Letters 2008, 18(20), 5591-5593
- 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
- 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.
- 1464-3405 (Electronic)
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