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. 2012 Dec 1;22(23):7119-22.
doi: 10.1016/j.bmcl.2012.09.077. Epub 2012 Sep 29.

Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides

Casey McComas  1 , Jeffrey Cohen, Christine Huselton, Michael Marella, Edward Melenski, Cheryl Mugford, Ov Slayden, Richard Winneker, Jay Wrobel, Matthew R Yudt, Andrew Fensome
Affiliations

Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides

Casey McComas et al. Bioorg Med Chem Lett. .

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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