High affinity retinoic acid receptor antagonists: analogs of AGN 193109.
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.
Johnson
A T
AT
Retinoid Research, Department of Chemistry, Allergan Inc., Irvine, CA 92713, USA.
Wang
L
L
Gillett
S J
SJ
Chandraratna
R A
RA
D009281:Naphthalenes / Q000737:chemistry* / Q000494:pharmacology; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D009281:Naphthalenes; D018168:Receptors, Retinoic Acid; C096920:AGN 193109