2. Academic Validation
  3. 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators

5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators

  • J Med Chem. 2003 Sep 11;46(19):4104-12. doi: 10.1021/jm020477g.
Lin Zhi 1,  Christopher M Tegley,  Barbara Pio,  James P Edwards,  Mehrnouch Motamedi,  Todd K Jones,  Keith B Marschke,  Dale E Mais,  Boris Risek,  William T Schrader
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA. lzhi@ligand.com
PMID: 12954062 DOI: 10.1021/jm020477g
Abstract

A series of 5-benylidene-1,2-dihydrochromeno[3,4-f]quinolines (4) were synthesized and tested in bioassays to evaluate their progestational activities, receptor- and tissue-selectivity profiles as selective Progesterone Receptor modulators (SPRMs). Most of the new analogues exhibited as highly potent progestins with more than 100-fold receptor selectivity over Other steroid hormone receptors and LG120920 (7b) demonstrated tissue selectivity toward uterus and vagina versus breasts in a rodent model after oral administration.

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