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

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

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com
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.

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