New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids

  • Bioorg Med Chem. 2006 Oct 1;14(19):6726-32. doi: 10.1016/j.bmc.2006.05.066.
Weiqin Jiang  1 ,  George Allan ,  James J Fiordeliso ,  Olivia Linton ,  Pamela Tannenbaum ,  Jun Xu ,  Peifang Zhu ,  Joseph Gunnet ,  Keith Demarest ,  Scott Lundeen ,  Zhihua Sui
Affiliations
  • 1. Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA. [email protected]
PMID: 16806946 DOI: 10.1016/j.bmc.2006.05.066
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.

Products