Author/Authors :
David G. Jones، نويسنده , , Xi Liang، نويسنده , , Eugene L. Stewart، نويسنده , , Robert A. Noe، نويسنده , , Lara S. Kallander، نويسنده , , Kevin P. Madauss، نويسنده , , Timothy M. Willson and Shawn P. Williams، نويسنده , , Scott K. Thompson، نويسنده , , David W. Gray، نويسنده , , William J. Hoekstra، نويسنده ,
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.
