Zhi Lin, Tegley Christopher M, Pio Barbara, Edwards James P, Motamedi Mehrnouch, Jones Todd K, Marschke Keith B, Mais Dale E, Risek Boris, Schrader William T
Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA.
J Med Chem. 2003 Sep 11;46(19):4104-12. doi: 10.1021/jm020477g.
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.
