S-Space College of Medicine/School of Medicine (의과대학/대학원) Program in Cancer Biology (협동과정-종양생물학전공) Journal Papers (저널논문_협동과정-종양생물학전공)
Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation
- Byeon, Seong Rim; Lee, Ji Hoon; Sohn, Ji-Hoon; Kim, Dong Chan; Shin, Kye Jung; Yoo, Kyung Ho; Mook-Jung, Inhee; Lee, Won Koo; Kim, Dong Jin
- Issue Date
- Bioorg Med Chem Lett. 2007 Mar 1;17(5):1466-70. Epub 2006 Nov 2.
- Amyloid beta-Protein/*antagonists & inhibitors; Animals; Benzene Derivatives/*chemical synthesis/*pharmacology; Cell Line; Cell Survival/drug effects; Drug Design; Inhibitory Concentration 50; Mice; Pyridines/chemical synthesis/pharmacology; Structure-Activity Relationship; Styrenes/chemical synthesis/pharmacology; Thiazoles
- 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.
- 0960-894X (Print)
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