Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation.
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.
Byun
Ji Hun
JH
Life Sciences Research Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Kim
HyeYun
H
Kim
YoungSoo
Y
Mook-Jung
Inhee
I
Kim
Dong Jin
DJ
Lee
Won Koo
WK
Yoo
Kyung Ho
KH
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
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