| Literature DB >> 15265495 |
Xiangdong Su1, Harshani Lawrence, Dharshini Ganeshapillai, Adrian Cruttenden, Atul Purohit, Michael J Reed, Nigel Vicker, Barry V L Potter.
Abstract
Extensive structural modifications to the 18beta-glycyrrhetinic acid template are described and their effects on the SAR of the 11beta-hydroxysteroid dehydrogenase isozymes type 1 and 2 from the rat are investigated. Isoform selective inhibitors have been discovered and compound 7 N-(2-hydroxyethyl)-3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic acid amide is highlighted as a very potent selective inhibitor of 11beta-hydroxysteroid dehydrogenase 2 with an IC(50) = 4pM.Entities:
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Year: 2004 PMID： 15265495 DOI： 10.1016/j.bmc.2004.06.008
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641