2. Academic Validation
  3. Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists

Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists

  • J Med Chem. 2002 Jun 6;45(12):2417-24. doi: 10.1021/jm0105530.
Bradley P Morgan 1,  Andrew G Swick,  Diane M Hargrove,  Janet A LaFlamme,  Melinda S Moynihan,  Richard S Carroll,  Kelly A Martin,  Eunsun Lee,  Debra Decosta,  Jon Bordner
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Pfizer Inc., Eastern Point Road, Groton, CT 06371, USA. bmorgan@cytokinetics.com
PMID: 12036351 DOI: 10.1021/jm0105530
Abstract

An approach to the computer-assisted, pharmacophore design of nonsteroidal templates for the Glucocorticoid Receptor (GR) that contained an element of pseudo-C2 symmetry was developed. The enatiomer of the initial design, 1Ra, and not the designed molecule, 1S, showed the desired ligand binding to the GR. The pseudo-C2 symmetry of the template allowed for rapid improvements in GR activity resulting in potent, selective, nonsteroidal GR antagonists, CP-394531 and CP-409069.

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