Synthesis and Biological Activity of 5-Methylidene 1,2-Dihydrochromeno[3,4-f]quinoline Derivatives as Progesterone Receptor Modulators.

A series of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives were synthesized and tested in biological assays to evaluate scope and limitations of the nonsteroidal SPRM pharmacophore (3). A number of orally available highly potent nonsteroidal modulators were identified by modification of the substituents at 5-methylidene position.