title: Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation.
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.
authors.affiliation: Life Sciences Research Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors.forename: Ji Hun
authors.initials: JH
authors.lastname: Byun
authors.forename: HyeYun
authors.initials: H
authors.lastname: Kim
authors.forename: YoungSoo
authors.initials: Y
authors.lastname: Kim
authors.forename: Inhee
authors.initials: I
authors.lastname: Mook-Jung
authors.forename: Dong Jin
authors.initials: DJ
authors.lastname: Kim
authors.forename: Won Koo
authors.initials: WK
authors.lastname: Lee
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Yoo
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors / Q000737:chemistry*; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D052160:Benzothiazoles; D001583:Benzoxazoles / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003474:Curcumin / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D004583:Electrons; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D010446:Peptide Fragments / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000737:chemistry
chemical_list: C472244:1-iodo-2,5-bis-(3-hydroxycarbonyl-4-methoxy)styryl-benzene; D016229:Amyloid beta-Peptides; D001572:Benzofurans; D052160:Benzothiazoles; D001583:Benzoxazoles; D010446:Peptide Fragments; D013343:Styrenes; D013844:Thiazoles; C075222:amyloid beta-protein (1-42); C009462:thioflavin T; D003474:Curcumin; C105430:benzofuran