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High affinity retinoic acid receptor antagonists: analogs of AGN 193109
A T Johnson1, L Wang, S J Gillett
1Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92713, USA.
Bioorganic & Medicinal Chemistry Letters
|March 31, 1999
Abstract:
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.