Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.

Article Details

Citation
Copy to clipboard

Beard RL, Klein ES, Standeven AM, Escobar M, Chandraratna RA

Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.

Bioorg Med Chem Lett. 2001 Mar 26;11(6):765-8.

PubMed ID
11277515 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TretinoinRetinoic acid receptor alphaKd (nM)14N/AN/ADetails
TretinoinRetinoic acid receptor alphaEC 50 (nM)240N/AN/ADetails
TretinoinRetinoic acid receptor betaEC 50 (nM)38N/AN/ADetails
TretinoinRetinoic acid receptor betaKd (nM)11N/AN/ADetails
TretinoinRetinoic acid receptor gammaEC 50 (nM)6N/AN/ADetails
TretinoinRetinoic acid receptor gammaKd (nM)16N/AN/ADetails