Synthesis and biological activity of high-affinity retinoic acid receptor antagonists

Synthesis and biological activity of high-affinity retinoic acid receptor antagonists 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Elsevier

Synthesis and biological activity of high-affinity retinoic acid receptor antagonists

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Publisher
Elsevier
Copyright
Copyright © 1999 Elsevier Science Ltd
ISSN
0968-0896
D.O.I.
10.1016/S0968-0896(99)00055-3
Publisher site
See Article on Publisher Site

Abstract

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.

Journal

Bioorganic & Medicinal ChemistryElsevier

Published: Jul 1, 1999

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