Novel progesterone receptor modulators: 4-Aryl-phenylsulfonamides

…, E Melenski, C Mugford, O Slayden, R Winneker…

文献索引：McComas, Casey; Cohen, Jeffrey; Huselton, Christine; Marella, Michael; Melenski, Edward; Mugford, Cheryl; Slayden, Ov; Winneker, Richard; Wrobel, Jay; Yudt, Matthew R.; Fensome, Andrew Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7119 - 7122

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被引用次数: 2

摘要

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 ...