High affinity retinoic acid receptor antagonists: analogs of AGN 193109

Bioorg Med Chem Lett. 1999 Feb 22;9(4):573-6. doi: 10.1016/s0960-894x(99)00047-5.


A series of high affinity retinoic acid receptor (RAR) antagonists were prepared based upon the known antagonist AGN 193109 (2). Introduction of various phenyl groups revealed a preference for substitution at the para-position relative to the meta-site. Antagonists with the highest affinities for the RARs possessed hydrophobic groups, however, the presence of polar functionality was also well tolerated.

MeSH terms

  • Naphthalenes / chemistry*
  • Naphthalenes / pharmacology
  • Receptors, Retinoic Acid / antagonists & inhibitors*
  • Structure-Activity Relationship


  • Naphthalenes
  • Receptors, Retinoic Acid
  • AGN 193109