5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. doi: 10.1016/j.bmcl.2009.10.008. Epub 2009 Oct 7.

Abstract

Novel 5-aryl indanones, inden-1-one oximes, and inden-1-ols were synthesized and evaluated as progesterone receptor (PR) modulators using the T47D cell alkaline phosphatase assay. Both PR agonists and antagonists were achieved with appropriate 3- and 5-substitution from indanones and inden-1-ols while inden-1-one oximes provided only PR antagonists. Several compounds such as 10 and 11 demonstrated potent in vitro PR agonist potency similar to that of steroidal progesterone (1). In addition, a number of compounds (e.g., 12, 13, 17, 18) showed potent PR antagonist activity indicating the indanones and derivatives are promising PR modulator templates.

MeSH terms

  • Drug Design
  • Indans / chemical synthesis
  • Indans / chemistry
  • Indans / pharmacology*
  • Molecular Structure
  • Receptors, Progesterone / agonists*
  • Receptors, Progesterone / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Indans
  • Receptors, Progesterone