Basic Information
ID: ALA2203135
Journal: Bioorg Med Chem Lett
Title: Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
Authors: McComas C, Cohen J, Huselton C, Marella M, Melenski E, Mugford C, Slayden O, Winneker R, Wrobel J, Yudt MR, Fensome A.
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.
CiteXplore: 23079530
DOI: 10.1016/j.bmcl.2012.09.077
Patent ID: ┄
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