Document Report Card

ID: ALA1135457

Journal: J Med Chem

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

Authors: Morgan BP, Swick AG, Hargrove DM, LaFlamme JA, Moynihan MS, Carroll RS, Martin KA, Lee E, Decosta D, Bordner J.

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.

CiteXplore: 12036351

DOI: 10.1021/jm0105530