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50. Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Aβ fibril formation - Bioorg. Med. Chem. Lett. 2007, 17, 1466-1470

조회 수 3431 추천 수 0 2010.05.12 20:25:02
aziridine *.239.207.65

Seong Rim Byeon,Ji Hoon Lee,ji-Hoon Sohn,Dong Chan Kim,Kye jung Shin,Kyung Ho Yoo,Inhee Mook-Jung,Won Koo Lee and Dong Jin Kim　　　　　

 

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

 

1Bioorg. Med. Chem. Lett. 2007, 17, 1466-1470.jpg

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