1. Academic Validation
  2. New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles

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

Affiliation

  • 1 Chemical Sciences, Wyeth Research, Collegeville, PA 19426, USA. fensoma@wyeth.com
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.

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