A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.
The synthesis and biological activity of a novel series of tricyclic retinoic acid receptor antagonists are described. These compounds bind with high affinity to the RARs and are potent antagonists of retinoid function in in vitro and in vivo systems.
Vuligonda
V
V
Retinoid Research, Department of Chemistry, Allergan Pharmaceuticals, Irvine, CA 92614, USA.
Standeven
A M
AM
Escobar
M
M
Chandraratna
R A
RA
D000818:Animals; D000873:Anthracenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002478:Cells, Cultured; D002522:Chlorocebus aethiops; D006801:Humans; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors* / Q000235:genetics; D012176:Retinoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D015533:Transcriptional Activation; D014162:Transfection
D000873:Anthracenes; D018168:Receptors, Retinoic Acid; D012176:Retinoids; C119121:benzochromenyl retinoid; C119122:benzothiochromenyl retinoid; C119123:dihydroanthracenyl retinoid