Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore

  • Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8. doi: 10.1016/s0960-894x(03)00256-7.
Lin Zhi  1 ,  Josef D Ringgenberg ,  James P Edwards ,  Christopher M Tegley ,  Sarah J West ,  Barbara Pio ,  Mehrnouch Motamedi ,  Todd K Jones ,  Keith B Marschke ,  Dale E Mais ,  William T Schrader
Affiliations
  • 1. Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. [email protected]
PMID: 12781198 DOI: 10.1016/s0960-894x(03)00256-7
Abstract

A series of 1,2-dihydrochromeno[3,4-f]quinoline derivatives was synthesized and tested in biological assays to evaluate the nonsteroidal Progesterone Receptor Modulator pharmacophore (4) as antiprogestins. A number of potent analogues were identified by modification of the substituents at the D-ring.