New progesterone receptor antagonists: Phosphorus-containing 11β-aryl-substituted steroids

A new series of phosphorus-containing 11β-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.

A series of phosphorus-containing 11β-aryl-substituted steroids were synthesized and evaluated for their in vitro progesterone receptor and glucocorticoid receptor antagonist activities. Selected compounds were tested in rat in C3 assay for PR antagonist activities.Figure optionsDownload as PowerPoint slide