229961-23-3Relevant academic research and scientific papers
SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES
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, (2008/06/13)
2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula STR1 where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.
Synthesis and biological activity of high-affinity retinoic acid receptor antagonists
Johnson, Alan T.,Wang, Liming,Standeven, Andrew M.,Escobar, Maria,Chandraratna, Roshantha A.S.
, p. 1321 - 1338 (2007/10/03)
This article reports the synthesis and biological activity of new high affinity retinioic acid receptor (RAR) antagonists. The effect of introducing heteroatoms in the bicyclic ring system of the potent dihydronaphthalene RAR antagonist 8, and the variation of the pendant aromatic group on the ability of these compounds to function as RAR antagonists is discussed. The use of binding, transcriptional, and in vivo assays revealed that the 2,2-dimethylthiochromene analogue 59, and the 2,2-dimethylchromene derivative 85, were the most effective in blocking retinoid agonist induced activity. Copyright (C) 1999 Elsevier Science Ltd.
