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Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.

Journal article
Authors Henrik Sundén
Anja Schäfer
Marcel Scheepstra
Seppe Leysen
Marcus Malo
Jian-Nong Ma
Ethan S Burstein
Christian Ottmann
Luc Brunsveld
Roger Olsson
Published in Journal of Medicinal Chemistry
Volume 59
Issue 3
Pages 1232-1238
ISSN 0022-2623
Publication year 2016
Published at Department of Chemistry and Molecular Biology
Pages 1232-1238
Language en
Subject categories Organic synthesis


The nuclear receptor Nurr1 can be activated by RXR via heterodimerization (RXR-Nurr1) and is a promising target for treating neurodegenerative diseases. We herein report the enantioselective synthesis and SAR of sterically constricted benzofurans at RXR. The established SAR, using whole cell functional assays, lead to the full agonist 9a at RXR (pEC50 of 8.2) and RXR-Nurr1. The X-ray structure shows enantiomeric discrimination where 9a optimally addresses the ligand binding pocket of RXR.

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