Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5754-7. doi: 10.1016/j.bmcl.2007.08.064.
Chunyang Jin  1 ,  G Manikumar ,  John A Kepler ,  C Edgar Cook ,  George F Allan ,  Margaret Kiddoe ,  Sheela Bhattacharjee ,  Olivia Linton ,  Scott G Lundeen ,  Zhihua Sui
Affiliations
  • 1. Center for Organic and Medicinal Chemistry, RTI International, PO Box 12194, Research Triangle Park, NC 27709, USA. [email protected]
PMID: 17855092 DOI: 10.1016/j.bmcl.2007.08.064
Abstract

A series of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based Alkaline Phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486).