2. Academic Validation
  3. Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists

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

Affiliation

  • 1 Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. steven.richards@abbott.com
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.

Figures