Pascal Collette

Highly Potent Naphthofuran-Based Retinoic Acid Receptor Agonists

A series of arotinoids with a central benzofuran or naphthofuran ring structure were synthesized by an efficient three‐step process. Most of these 3‐substituted naphthofuran arotinoids are potent agonists of the retinoic acid receptor (RAR) subtypes, with activities in the nanomolar range.

Pyrazine arotinoids with inverse agonist activities on the retinoid and rexinoid receptors.

RAR and RXR agonists: A collection of pyrazine‐based RAR/RXR ligands were prepared by a series of palladium catalyzed cross‐coupling reactions and characterized. Structure–activity relationships were elucidated. Retinoic acid receptor (RAR) α/β‐subtype‐selective and retinoid X receptor (RXR) inverse agonist activities are described for pyrazine acrylic acid arotinoid, 14 d.