Phenolic bis-styrylbenzenes as β-amyloid binding ligands and free radical scavengers

DP Flaherty, T Kiyota, Y Dong, T Ikezu…

Index: Flaherty, Daniel P.; Kiyota, Tomomi; Dong, Yuxiang; Ikezu, Tsuneya; Vennerstrom, Jonathan L. Journal of Medicinal Chemistry, 2010 , vol. 53, # 22 p. 7992 - 7999

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Citation Number: 24

Abstract

Starting from bisphenolic bis-styrylbenzene DF-9 (4), β-amyloid (Aβ) binding affinity and specificity for phenolic bis-styrylbenzenes, monostyrylbenzenes, and alkyne controls were determined by fluorescence titration with β-amyloid peptide Aβ1− 40 and a fluorescence assay using APP/PS1 transgenic mouse brain sections. Bis-styrylbenzene SAR is derived largely from work on symmetrical compounds. This study is the first to describe Aβ binding ...