2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs)

Bioorg Med Chem Lett. 2003 Feb 10;13(3):479-83. doi: 10.1016/s0960-894x(02)00985-x.

Abstract

A series of 2-phenylspiroindenes was prepared. The most active analogue (2) was found to be comparable in potency to raloxifene (1) as an estrogen receptor ligand.

MeSH terms

  • Alkylation
  • Animals
  • Borohydrides
  • Crystallography, X-Ray
  • Humans
  • In Vitro Techniques
  • Indenes / chemical synthesis*
  • Indenes / pharmacology*
  • Indicators and Reagents
  • Raloxifene Hydrochloride / pharmacology
  • Rats
  • Receptors, Estrogen / drug effects
  • Selective Estrogen Receptor Modulators / chemical synthesis*
  • Selective Estrogen Receptor Modulators / pharmacology*
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / pharmacology*
  • Structure-Activity Relationship

Substances

  • 2-Phenylspiroindene
  • Borohydrides
  • Indenes
  • Indicators and Reagents
  • Receptors, Estrogen
  • Selective Estrogen Receptor Modulators
  • Spiro Compounds
  • Raloxifene Hydrochloride
  • sodium borohydride