High affinity retinoic acid receptor antagonists: Analogs of AGN 193109

Article abstract of 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.