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

Cited 32 time in Web of Science Cited 34 time in Scopus
Authors
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
2007-02-03
Publisher
Elsevier
Citation
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1466-70. Epub 2006 Nov 2.
Keywords
Amyloid beta-Protein/*antagonists & inhibitorsAnimalsBenzene Derivatives/*chemical synthesis/*pharmacologyCell LineCell Survival/drug effectsDrug DesignInhibitory Concentration 50MicePyridines/chemical synthesis/pharmacologyStructure-Activity RelationshipStyrenes/chemical synthesis/pharmacologyThiazoles
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.
ISSN
0960-894X (Print)
Language
English
URI
http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF9-4M81C09-5&_user=10&_rdoc=1&_fmt=&_orig=search&_sort=d&_docanchor=&view=c&_acct=C000050221&_version=1&_urlVersion=0&_userid=10&md5=0766e824064330fa3ec9090b1988c661

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=17270435

https://hdl.handle.net/10371/22852
DOI
https://doi.org/10.1016/j.bmcl.2006.10.090
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College of Medicine/School of Medicine (의과대학/대학원)Program in Cancer Biology (협동과정-종양생물학전공)Journal Papers (저널논문_협동과정-종양생물학전공)
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