Document Detail


Fluorescent schweinfurthin B and F analogs with anti-proliferative activity.
MedLine Citation:
PMID:  20724169     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The natural tetracyclic schweinfurthins are potent and selective inhibitors of cell growth in the National Cancer Institute's 60 cell-line screen. At this time, the mechanism or cellular target that underlies this activity has not yet been identified, and efforts to illuminate the schweinfurthins' mode of action would benefit from development of potent fluorescent analogs that could be readily visualized within cells. This report describes the synthesis of fluorescent analogs of schweinfurthins B and F, and demonstrates that these compounds retain the potent and differentially toxic activities against select human cancer cells that are characteristic of the natural schweinfurthins. In addition, the synthesis of control compounds that maintain parallel fluorescent properties, but lack the potent activity of the natural schweinfurthin is described. Use of fluorescence microscopy shows differences between the localization of the active and relatively inactive schweinfurthin analogs. The active compounds localize in peripheral puncta which may identify the site(s) of activity.
Authors:
Joseph J Topczewski; Craig H Kuder; Jeffrey D Neighbors; Raymond J Hohl; David F Wiemer
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2010-07-29
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-06     Completed Date:  2010-12-30     Revised Date:  2014-04-24    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6734-41     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / analysis,  chemistry*,  pharmacology
Cell Line, Tumor
Fluorescent Dyes / chemistry*
Humans
Microscopy, Fluorescence
Stilbenes / analysis,  chemistry*,  pharmacology
Grant Support
ID/Acronym/Agency:
R41 CA126020-01/CA/NCI NIH HHS; R41CA126020/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Fluorescent Dyes; 0/Stilbenes; 0/schweinfurthin B; 0/schweinfurthin F
Comments/Corrections

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