| Literature DB >> 12036351 |
Bradley P Morgan1, Andrew G Swick, Diane M Hargrove, Janet A LaFlamme, Melinda S Moynihan, Richard S Carroll, Kelly A Martin, Eunsun Lee, Debra 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.Entities:
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Year: 2002 PMID： 12036351 DOI： 10.1021/jm0105530
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446