| Literature DB >> 15925510 |
David G Jones1, Xi Liang, Eugene L Stewart, Robert A Noe, Lara S Kallander, Kevin P Madauss, Shawn P Williams, Scott K Thompson, David W Gray, William J Hoekstra.
Abstract
Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-endometriotic activities. Non-steroidal mimetics of mifepristone and progesterone are important templates for modulation of the progesterone receptor (PR). For our PR program, we sought an unexplored, synthetically accessible non-steroidal mimetic of mifepristone, suitable for parallel synthesis of analogues. Docking of compounds into a PR homology model identified 4-substituted pyrazolines, which, when synthesized and tested, exhibited functional antagonism of PR.Entities:
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Year: 2005 PMID： 15925510 DOI： 10.1016/j.bmcl.2005.05.001
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823