- Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation.
Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation.
Bioorganic & medicinal chemistry letters (2007-02-03)
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
PMID17270435
ABSTRACT
New bis-styrylpyridine and bis-styrylbenzene derivatives were designed and synthesized. These 34 compounds were evaluated by Abeta fibril formation inhibitory assay using thioflavin T as a dye (named ThT assay). Most of them showed excellent inhibitory activities for Abeta fibril formation at IC50 of 0.1-2.7 microM which is comparable to curcumin (IC50 of 0.8 microM). Among them, nine compounds were screened for their cytotoxicities on HT-22 cell by MTT assay at 1, 10, and 50 microM. In particular, I-7 and II-2 exhibited the best combination of inhibitory activity and compound cytotoxicity.
MATERIALS