Document Detail


Carbamate derivatives of betulinic acid and betulin with selective cytotoxic activity.
MedLine Citation:
PMID:  20451375     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Synthesis and antiproliferative activity of eight new derivatives of betulinic acid (1) and betulin (2) are described. The compounds were tested against fifteen tumor cell lines. The toxicity against normal human fibroblasts and the mode of cell death on lung cancer cell line induced by the most active compounds 9 (bis(ethylcarbamate)betulin) and 11 (3-O-ethylcarbamate of 28-O-acetylbetulin) was investigated. Caspase 3 activity on lung cancer cell line (A549) was determined for 1, 5 (3-O-ethylcarbamate of betulinic acid), 9 and 11. All derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of lung cancer cells for 24h with 9 and 11 induced apoptosis, as observed by the appearance of a typical ladder pattern in the DNA fragmentation assay.
Authors:
Harish Kommera; Goran N Kaluderović; Sebastian Dittrich; Jutta Kalbitz; Birgit Dräger; Thomas Mueller; Reinhard Paschke
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-18
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-05-21     Completed Date:  2010-08-10     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3409-12     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Biozentrum, Martin-Luther-Universität Halle-Wittenberg, Weinbergweg 22, 06120 Halle, Germany.
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MeSH Terms
Descriptor/Qualifier:
Carbamates / chemistry*
Cell Line, Tumor
Cell Proliferation / drug effects
Humans
Triterpenes / chemistry,  pharmacology*
Chemical
Reg. No./Substance:
0/Carbamates; 0/Triterpenes; 472-15-1/betulinic acid; 473-98-3/betulin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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