Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists

  • Bioorg Med Chem Lett. 2003 Apr 7;13(7):1317-20. doi: 10.1016/s0960-894x(03)00129-x.
Andrew Fensome  1 ,  Marci Koko ,  Jay Wrobel ,  Puwen Zhang ,  Zhiming Zhang ,  Jeffrey Cohen ,  Scott Lundeen ,  Kelly Rudnick ,  Yuan Zhu ,  Richard Winneker
Affiliations
PMID: 12657272 DOI: 10.1016/s0960-894x(03)00129-x
Abstract

During the course of our studies on 3,3-disubstituted-5-aryloxindoles derived Progesterone Receptor (PR) antagonists we discovered that changing the amide funtionality to a thio-amide resulted in compounds displaying potent PR agonist activity. In this communication, the synthesis, structure activity relationships (SAR) and in vivo activity of various 5-arylthio-oxindoles will be discussed.