New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids |
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Authors: | Jiang Weiqin Allan George Fiordeliso James J Linton Olivia Tannenbaum Pamela Xu Jun Zhu Peifang Gunnet Joseph Demarest Keith Lundeen Scott Sui Zhihua |
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Institution: | Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA. wjiang1@prdus.jnj.com |
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Abstract: | A new series of phosphorus-containing 11beta-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. |
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