Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists

Irini Akritopoulou-Zanze; Jyoti R Patel; Kresna Hartandi; Jehrod Brenneman; Martin Winn; John K Pratt; Marlene Grynfarb; Annika Goos-Nisson; Thomas W Von Geldern; Philip R Kym

doi:10.1016/j.bmcl.2004.02.048

Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists

Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82. doi: 10.1016/j.bmcl.2004.02.048.

Authors

Irini Akritopoulou-Zanze¹, Jyoti R Patel, Kresna Hartandi, Jehrod Brenneman, Martin Winn, John K Pratt, Marlene Grynfarb, Annika Goos-Nisson, Thomas W Von Geldern, Philip R Kym

Affiliation

¹ Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA. [email protected]

PMID: 15080982
DOI: 10.1016/j.bmcl.2004.02.048

Abstract

We report the discovery of a novel class of glucocorticoid receptor (GR) antagonists based on the chromene molecular scaffold. The compounds exhibit good functional potency and an improved receptor selectivity profile for GR over other steroid receptors when compared to the classical steroidal GR-antagonist, RU-486.

Publication types

Comparative Study

MeSH terms

Benzopyrans / chemical synthesis*
Benzopyrans / chemistry
Benzopyrans / pharmacology*
Drug Evaluation, Preclinical
Mifepristone / pharmacology
Receptors, Glucocorticoid / antagonists & inhibitors*

Substances

5,7-dimethoxy-2-methyl-2H-benzopyran
Benzopyrans
Receptors, Glucocorticoid
Mifepristone