sp2-bridged diaryl retinoids: effects of bridge-region substitution on retinoid X receptor (RXR) selectivity

Bioorg Med Chem Lett. 2000 Jun 19;10(12):1307-10. doi: 10.1016/s0960-894x(00)00243-2.


RXR class selectivity and RXR transcriptional activation activity compared to those for the retinoic acid receptor subtypes were enhanced on the 4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenylethenyl)be nzoic acid scaffold and its 3-methyl analogue by replacing their 1,1-ethenyl bridge by a 1,1-(2-methylpropenyl) or cyclopropylidenylmethylene group.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Cell Division / drug effects
  • Humans
  • Molecular Structure
  • Receptors, Retinoic Acid / metabolism*
  • Retinoid X Receptors
  • Retinoids / chemistry
  • Retinoids / metabolism*
  • Retinoids / pharmacology
  • Transcription Factors / metabolism*
  • Tumor Cells, Cultured


  • Receptors, Retinoic Acid
  • Retinoid X Receptors
  • Retinoids
  • Transcription Factors