Author/Authors :
Andrew Fensome، نويسنده , , Reinhold Bender، نويسنده , , Jeffrey Cohen، نويسنده , , Mark A. Collins، نويسنده , , Valerie A. Mackner، نويسنده , , Lori L. Miller، نويسنده , , John W. Ullrich، نويسنده , , Richard Winneker، نويسنده , , Jay Wrobel، نويسنده , , Puwen Zhang، نويسنده , , Zhiming Zhang، نويسنده , , Yuan Zhu، نويسنده ,
Abstract :
A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist (PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this communication, the synthesis and structure–activity relationships (SARs) of various 3,3-substituents are discussed where it is clear that small alkyl and spiroalkyl groups are required to achieve better PR antagonist activity.
