Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists

  • Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. doi: 10.1016/j.bmcl.2006.08.133.
Steven J Richards  1 ,  Thomas W von Geldern ,  Peer Jacobson ,  Denise Wilcox ,  Phong Nguyen ,  Lars Ohman ,  Marie Osterlund ,  Birgitta Gelius ,  Marlena Grynfarb ,  Annika Goos-Nilsson ,  Jiahong Wang ,  Steven Fung ,  Masha Kalmanovich
Affiliations
  • 1. Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. [email protected]
PMID: 16987661 DOI: 10.1016/j.bmcl.2006.08.133
Abstract

A series of potent steroidal Glucocorticoid Receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for GR in vitro and had modest in vivo efficacy.