Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists

  • Bioorg Med Chem. 2010 Jun 15;18(12):4255-68. doi: 10.1016/j.bmc.2010.04.092.
Yongli Du  1 ,  Qunyi Li ,  Bing Xiong ,  Xin Hui ,  Xin Wang ,  Yang Feng ,  Tao Meng ,  Dingyu Hu ,  Datong Zhang ,  Mingwei Wang ,  Jingkang Shen
Affiliations
  • 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
PMID: 20510622 DOI: 10.1016/j.bmc.2010.04.092
Abstract

A novel class of non-steroidal Progesterone Receptor antagonists with aromatic beta-amino-ketone scaffold have been synthesized and characterized with high binding affinity and great selectivity for the cognate receptors. Among them, compound 22 was shown to be the most potent Progesterone Receptor antagonist in cotransfection assay and a murine model of ligand-induced decidualization.