Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Aβ fibril formation

  • Byeon, Seong Rim
  • Lee, Ji Hoon
  • Sohn, Ji-Hoon
  • Kim, Dong Chan
  • Shin, Kye Jung
  • ... Lee, Won Koo
  • 외 3명
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초록

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.

키워드

A beta fibril formation inhibitorAlzheimer diseasebis-styrylpyridinebis-styrylbenzeneamyloid betaALZHEIMERS-DISEASEAMYLOID HYPOTHESISALPHA-SYNUCLEINPLAQUESMEDICINECURCUMIN
제목
Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Aβ fibril formation
저자
Byeon, Seong RimLee, Ji HoonSohn, Ji-HoonKim, Dong ChanShin, Kye JungYoo, Kyung HoMook-Jung, InheeLee, Won KooKim, Dong Jin
DOI
10.1016/j.bmcl.2006.10.090
발행일
2007-03-01
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
17
5
페이지
1466 ~ 1470