A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids

V Vuligonda; A M Standeven; M Escobar; R A Chandraratna

doi:10.1016/s0960-894x(99)00077-3

A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids

Bioorg Med Chem Lett. 1999 Mar 8;9(5):743-8. doi: 10.1016/s0960-894x(99)00077-3.

Authors

V Vuligonda¹, A M Standeven, M Escobar, R A Chandraratna

Affiliation

¹ Retinoid Research, Department of Chemistry, Allergan Pharmaceuticals, Irvine, CA 92614, USA.

PMID: 10201840
DOI: 10.1016/s0960-894x(99)00077-3

Abstract

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.

MeSH terms

Animals
Anthracenes / chemical synthesis*
Anthracenes / pharmacology
Anthracenes / toxicity
Cells, Cultured
Chlorocebus aethiops
Humans
Receptors, Retinoic Acid / antagonists & inhibitors*
Receptors, Retinoic Acid / genetics
Retinoids / chemical synthesis*
Retinoids / chemistry
Retinoids / pharmacology
Retinoids / toxicity
Transcriptional Activation
Transfection

Substances

Anthracenes
Receptors, Retinoic Acid
Retinoids
benzochromenyl retinoid
benzothiochromenyl retinoid
dihydroanthracenyl retinoid