New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles

  • Bioorg Med Chem Lett. 2002 Dec 2;12(23):3487-90. doi: 10.1016/s0960-894x(02)00746-1.
Andrew Fensome  1 ,  Reinhold Bender ,  Jeffrey Cohen ,  Mark A Collins ,  Valerie A Mackner ,  Lori L Miller ,  John W Ullrich ,  Richard Winneker ,  Jay Wrobel ,  Puwen Zhang ,  Zhiming Zhang ,  Yuan Zhu
Affiliations
PMID: 12419390 DOI: 10.1016/s0960-894x(02)00746-1
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.