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

Steven J Richards; 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

doi:10.1016/j.bmcl.2006.08.133

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. Epub 2006 Sep 20.

Authors

Steven J Richards¹, 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

Affiliation

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

MeSH terms

Animals
Bile Acids and Salts / chemistry*
Humans
Microsomes / drug effects
Microsomes / metabolism
Molecular Structure
Rats
Receptors, Glucocorticoid / antagonists & inhibitors*
Receptors, Glucocorticoid / metabolism
Structure-Activity Relationship

Substances

Bile Acids and Salts
Receptors, Glucocorticoid