Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists

David G. Jones, 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

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    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.
    Original languageEnglish
    Pages (from-to)3203-6
    Number of pages4
    JournalBioorganic & Medicinal Chemistry Letters
    Volume15
    Issue number13
    DOIs
    Publication statusPublished - 2005

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    Jones, D. G., Liang, X., Stewart, E. L., Noe, R. A., Kallander, L. S., Madauss, K. P., Williams, S. P., Thompson, S. K., Gray, D. W., & Hoekstra, W. J. (2005). Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists. Bioorganic & Medicinal Chemistry Letters, 15(13), 3203-6. https://doi.org/10.1016/j.bmcl.2005.05.001