229961-45-9Relevant articles and documents
From Propargylic Alcohols to Substituted Thiochromenes: Gem-Disubstituent Effect in Intramolecular Alkyne Iodo/hydroarylation
Velasco, Noelia,Suárez, Anisley,Martínez-Lara, Fernando,Fernández-Rodríguez, Manuel ángel,Sanz, Roberto,Suárez-Pantiga, Samuel
, p. 7078 - 7091 (2021/05/29)
This work describes the 6-endo-dig cyclization of S-aryl propargyl sulfides to afford 2H-thiochromenes. The substitution at the propargylic position plays a crucial role in allowing intramolecular silver-catalyzed alkyne hydroarylation and N-iodosuccinimide-promoted iodoarylation. Additionally, a PTSA-catalyzed thiolation reaction of propargylic alcohols was developed to synthesize the required tertiary S-aryl propargyl ethers. The applicability of merging these two methods is demonstrated by synthesizing the retinoic acid receptor antagonist AGN194310.
Methods of treatment during vascular procedures
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, (2008/06/13)
The invention provides in one embodiment a method for treating vascular trauma. The method can include administering to an individual undergoing vascular trauma an effective amount of a retinoic acid receptor (RAR) antagonist or an RAR inhibitor. The meth
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.