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.

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.

MeSH terms

  • Animals
  • Cell Line
  • Chlorocebus aethiops
  • Humans
  • Inhibitory Concentration 50
  • Progesterone / pharmacology
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Receptors, Progesterone / agonists
  • Receptors, Progesterone / antagonists & inhibitors*
  • Receptors, Progesterone / metabolism
  • Receptors, Steroid / antagonists & inhibitors
  • Structure-Activity Relationship
  • Transcription, Genetic / drug effects
  • Transfection

Substances

  • Quinolines
  • Receptors, Progesterone
  • Receptors, Steroid
  • Progesterone