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J Med Chem. 2002 Jun 6;45(12):2417-24.

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

Author information

  • 1Pfizer Global Research and Development, Pfizer Inc., Eastern Point Road, Groton, CT 06371, USA. bmorgan@cytokinetics.com

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.

PMID:
12036351
[PubMed - indexed for MEDLINE]

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