Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators

  • Bioorg Med Chem Lett. 2003 Jun 16;13(12):2071-4. doi: 10.1016/s0960-894x(03)00255-5.
Lin Zhi  1 ,  Christopher M Tegley ,  Barbara Pio ,  James P Edwards ,  Todd K Jones ,  Keith B Marschke ,  Dale E Mais ,  Boris Risek ,  William T Schrader
Affiliations
  • 1. Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. [email protected]
PMID: 12781197 DOI: 10.1016/s0960-894x(03)00255-5
Abstract

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.