Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid

Bioorg Med Chem Lett. 2003 Jan 20;13(2):261-4. doi: 10.1016/s0960-894x(02)00924-1.

Abstract

A series of novel cyclopropanyl methyl hexadienoic acid retinoids was designed and prepared. These compounds exhibited either selective activity as RXR agonists or pan-agonists on one or more of each of the RAR and RXR isoforms. The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226.

MeSH terms

  • Binding, Competitive / drug effects
  • Cell Differentiation / drug effects
  • Cell Division / drug effects
  • Cyclopropanes / chemical synthesis*
  • Cyclopropanes / pharmacology*
  • Humans
  • Indicators and Reagents
  • Ligands
  • Receptors, Retinoic Acid / agonists
  • Receptors, Retinoic Acid / drug effects*
  • Receptors, Retinoic Acid / genetics
  • Sorbic Acid / analogs & derivatives*
  • Sorbic Acid / chemical synthesis
  • Sorbic Acid / pharmacology
  • Transfection
  • Tumor Cells, Cultured

Substances

  • Cyclopropanes
  • Indicators and Reagents
  • Ligands
  • Receptors, Retinoic Acid
  • Sorbic Acid