Stanetty, Christian and Czollner, Laszlo and Koller, Iris and Shah, Priti and Gaware, Rawindra and Cunha, Thierry Da and Odermatt, Alex and Jordis, Ulrich and Kosma, Paul and Classen-Houben, Dirk. (2010) Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11?-hydroxysteroid dehydrogenase 2 inhibitors. Bioorganic & medicinal chemistry, Vol. 18, H. 21. pp. 7522-7541.
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Official URL: http://edoc.unibas.ch/dok/A5841135
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Abstract
Glycyrrhetinic acid, the metabolite of the natural product glycyrrhizin, is a well known nonselective inhibitor of 11?-hydroxysteroid dehydrogenase (11?-HSD) type 1 and type 2. Whereas inhibition of 11?-HSD1 is currently under consideration for treatment of metabolic diseases, such as obesity and diabetes, 11?-HSD2 inhibitors may find therapeutic applications in chronic inflammatory diseases and certain forms of cancer. So far, no selective 11?-HSD2 inhibitor has been developed and neither animal studies nor clinical trials have been reported based on 11?-HSD2 inhibition. Starting from the lead compound glycyrrhetinic acid, novel triterpene type derivatives were synthesized and analyzed for their biological activity against overexpressed human 11?-HSD1 and 11?-HSD2 in cell lysates. Several hydroxamic acid derivatives showed high selectivity for 11?-HSD2. The most potent and selective compound is active against human 11?-HSD2 in the low nanomolar range with a 350-fold selectivity over human 11?-HSD1.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molecular and Systems Toxicology (Odermatt) |
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| UniBasel Contributors: | Odermatt, Alex |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Pergamon |
| ISSN: | 0968-0896 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
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| Last Modified: | 14 Sep 2012 07:17 |
| Deposited On: | 14 Sep 2012 06:37 |
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