Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Aβ fibril formation
作者:Seong Rim Byeon、Ji Hoon Lee、Ji-Hoon Sohn、Dong Chan Kim、Kye Jung Shin、Kyung Ho Yoo、Inhee Mook-Jung、Won Koo Lee、Dong Jin Kim
DOI:10.1016/j.bmcl.2006.10.090
日期:2007.3
New bis-styrylpyridine and bis-styrylbenzene derivatives were designed and synthesized. These 34 compounds were evaluated by A beta fibril formation inhibitory assay using thioflavin T as a dye (named ThT assay). Most of them showed excellent inhibitory activities for A beta fibril formation at IC50 of 0.1-2.7 mu M which is comparable to curcumin (IC50 of 0.8 mu M). Among them, nine compounds were screened for their cytotoxicities on HT-22 cell by MTT assay at 1, 10, and 50 mu M. In particular, 1-7 and II-2 exhibited the best combination of inhibitory activity and compound cytotoxicity. (c) 2006 Elsevier Ltd. All rights reserved.