Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Article Details
- CitationCopy 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
Drug Target Property Measurement pH Temperature (°C) Tretinoin Retinoic acid receptor alpha Kd (nM) 14 N/A N/A Details Tretinoin Retinoic acid receptor alpha EC 50 (nM) 240 N/A N/A Details Tretinoin Retinoic acid receptor beta EC 50 (nM) 38 N/A N/A Details Tretinoin Retinoic acid receptor beta Kd (nM) 11 N/A N/A Details Tretinoin Retinoic acid receptor gamma EC 50 (nM) 6 N/A N/A Details Tretinoin Retinoic acid receptor gamma Kd (nM) 16 N/A N/A Details