4-[3-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and heterocyclic-bridged analogues are novel retinoic acid receptor subtype and retinoid X receptor alpha agonists

Bioorg Med Chem Lett. 2000 Jun 19;10(12):1311-3. doi: 10.1016/s0960-894x(00)00244-4.


Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzo ic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and retinoid X receptors to induce gene transcription, and thereby provide novel scaffolds for retinoid drug development. Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth.

Publication types

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

MeSH terms

  • Benzoates / chemistry
  • Benzoates / pharmacology*
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Naphthalenes / chemistry
  • Naphthalenes / pharmacology*
  • Receptors, Retinoic Acid / agonists*
  • Retinoid X Receptors
  • Transcription Factors / agonists*
  • Tumor Cells, Cultured


  • 4-(3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl)benzoic acid
  • Benzoates
  • Heterocyclic Compounds
  • Naphthalenes
  • Receptors, Retinoic Acid
  • Retinoid X Receptors
  • Transcription Factors