Novel progesterone receptor modulators: 4-Aryl-phenylsulfonamides

Casey McComas, Jeffrey Cohen, Christine Huselton, Michael Marella, Edward Melenski, Cheryl Mugford, Ov Slayden, Richard Winneker, Jay Wrobel, Matthew R. Yudt, Andrew Fensome

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

We have developed a new series of progesterone receptor modulators based upon the 4-aryl-phenylsulfonamide. Initial work in the series afforded potent compounds with good properties, however an advanced intermediate proved to be genotoxic in a non-GLP Ames assay following metabolic activation. We subsequently solved this problem and identified advanced leads which demonstrated oral efficacy in rhesus monkey pharmacodynamic and kinetics models.

Original languageEnglish (US)
Pages (from-to)7119-7122
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number23
DOIs
StatePublished - Dec 1 2012

Keywords

  • Endometriosis
  • Progesterone antagonist
  • Progesterone modulator
  • Uterine fibroids

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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