- High affinity retinoic acid receptor antagonists: analogs of AGN 193109.
High affinity retinoic acid receptor antagonists: analogs of AGN 193109.
Bioorganic & medicinal chemistry letters (1999-03-31)
A T Johnson, L Wang, S J Gillett, R A Chandraratna
PMID10098666
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.
MATERIALS