| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594363 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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.
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Authors
Casey McComas, Jeffrey Cohen, Christine Huselton, Michael Marella, Edward Melenski, Cheryl Mugford, Ov Slayden, Richard Winneker, Jay Wrobel, Matthew R. Yudt, Andrew Fensome,