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 journalArticle

    3 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

    Fingerprint Dive into the research topics of 'Novel progesterone receptor modulators: 4-Aryl-phenylsulfonamides'. Together they form a unique fingerprint.

  • Cite this

    McComas, C., Cohen, J., Huselton, C., Marella, M., Melenski, E., Mugford, C., Slayden, O., Winneker, R., Wrobel, J., Yudt, M. R., & Fensome, A. (2012). Novel progesterone receptor modulators: 4-Aryl-phenylsulfonamides. Bioorganic and Medicinal Chemistry Letters, 22(23), 7119-7122. https://doi.org/10.1016/j.bmcl.2012.09.077