Synthesis and biological activity of retinoic acid receptor-alpha specific amides

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8. doi: 10.1016/s0960-894x(02)00647-9.


Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.

MeSH terms

  • Amides / chemical synthesis*
  • Amides / pharmacology*
  • Amides / toxicity
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Breast Neoplasms / drug therapy
  • Female
  • Humans
  • Hydrogen Bonding
  • Receptors, Retinoic Acid / drug effects*
  • Retinoic Acid Receptor alpha
  • Retinoids / chemical synthesis
  • Retinoids / pharmacology
  • Retinoids / toxicity
  • Structure-Activity Relationship


  • Amides
  • Antineoplastic Agents
  • RARA protein, human
  • Receptors, Retinoic Acid
  • Retinoic Acid Receptor alpha
  • Retinoids