| Synthesis and antitumour activity of glycyrrhetinic acid derivatives. | |
| | |
MedLine Citation:
|
PMID: 20932766 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
|
Glycyrrhetinic acid (GA) is one of many interesting triterpenoic acids showing anticancerogenic potential. GA is known to trigger apoptosis in tumour cell lines, although GA has a low cytotoxicity. In our study we were able to prepare derivatives of GA that show lowered the IC(50) values as determined by a sulforhodamine B (SRB) assay using 15 different human tumour cell lines. Thus, combining an ester group combined with the presence of an amino acid moiety led to a ca. 60-fold improved antitumor activity. Experiments on mouse embryonic fibroblasts (NiH3T3) revealed that these compounds showed a better selectivity for tumour cells compared to the parent compound GA. An apoptotic effect of some of these compounds was determined using an acridine orange/ethidium bromide (AO/EB) test and DNA laddering experiments. |
| | |
Authors:
|
Stefan Schwarz; René Csuk |
Related Documents
:
|
15080996 - Imidazole acetic acid tafia inhibitors: sar studies centered around the basic p(1)(') g... 19229586 - Recent synthesis of aminophosphonic acids as potential biological importance. 18511276 - Design, synthesis, and structure-activity relationships of piperidine and dehydropiperi... 2709376 - Retinobenzoic acids. 3. structure-activity relationships of retinoidal azobenzene-4-car... 6893316 - Activity of microsomal heme oxygenase in liver and spleen of ascorbic acid-deficient gu... 20438126 - Genotypic variability and genotype by environment interactions in oil and fatty acids i... |
Publication Detail:
|
Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-09-18 |
Journal Detail:
|
Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Nov |
Date Detail:
|
Created Date: 2010-10-18 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
|
Languages: eng Pagination: 7458-74 Citation Subset: IM |
Copyright Information:
|
Copyright © 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
|
Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Saale, Germany. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Visual failure and recovery after thrombosis of a giant carotid ophthalmic aneurysm following vascul...
Next Document: Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are impo...