Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Retinoids are natural and synthetic analogues of the hormone retinoic acid. Systemic retinoid agonist therapy is usually associated with toxic side effects, such as mucocutaneous toxicity, which may be alleviated by the use of topical retinoid antagonists. We report the synthesis and biological activity of a new series of potent, RAR-specific antagonists substituted with phenylcyclohexene and phenylcyclohexadiene groups.
Beard
R L
RL
Department of Chemistry, Retinoid Research, Allergan Incorporated, Irvine, CA 92623-9534, USA.
Klein
E S
ES
Standeven
A M
AM
Escobar
M
M
Chandraratna
R A
RA
D000818:Animals; D001565:Benzoates / Q000037:antagonists & inhibitors*; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017453:Dermatitis, Irritant / Q000188:drug therapy; D004195:Disease Models, Animal; D051379:Mice; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors*; D012176:Retinoids / Q000037:antagonists & inhibitors*
D001565:Benzoates; D003510:Cyclohexanes; D018168:Receptors, Retinoic Acid; D012176:Retinoids; C038864:4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid; C034672:1-phenylcyclohex-1-ene