Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.

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.

journal_name

Bioorg Med Chem Lett

authors

McComas C,Cohen J,Huselton C,Marella M,Melenski E,Mugford C,Slayden O,Winneker R,Wrobel J,Yudt MR,Fensome A

doi

10.1016/j.bmcl.2012.09.077

subject

Has Abstract

pub_date

2012-12-01 00:00:00

pages

7119-22

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01232-2

journal_volume

22

pub_type

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