2. Academic Validation
  3. New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids

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

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA. wjiang1@prdus.jnj.com
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.

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