期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 19, 页码 6726-6732出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.05.066
关键词
phosphorus-containing steroids; progesterone receptor antagonist
A new series of phosphorus-containing 11 beta-aryl-substituted steroids have been synthesized in an eight-step sequence involving a palladium-catalyzed coupling reaction to introduce a phosphorus group onto the aromatic ring. The compounds were evaluated for progesterone receptor (PR) antagonist activity in a T47D cell-based assay and for glucocorticoid receptor (GR) antagonist activity in an A549 cell-based assay. The structure-activity relationships of these compounds are discussed. Selected compounds were tested in vivo in a rat complement C3 assay. (c) 2006 Elsevier Ltd. All rights reserved.
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