Jiang Weiqin, Allan George, Fiordeliso James J, Linton Olivia, Tannenbaum Pamela, Xu Jun, Zhu Peifang, Gunnet Joseph, Demarest Keith, Lundeen Scott, Sui Zhihua
Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA.
Bioorg Med Chem. 2006 Oct 1;14(19):6726-32. doi: 10.1016/j.bmc.2006.05.066. Epub 2006 Jun 27.
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.
