Discovery of Potent, Nonsteroidal, and Highly Selective Glucocorticoid Receptor Antagonists
Journal of Medicinal Chemistry2002Vol. 45(12), pp. 2417–2424
Citations Over TimeTop 15% of 2002 papers
B. Paul Morgan, Andrew G. Swick, Diane M. Hargrove, Janet A. LaFlamme, Melinda S. Moynihan, Richard S. Carroll, Kelly A. Martin, Eun-Sun Lee, D.L. Decosta, Jon Bordner
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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