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Highly potent naphthofuran-based retinoic acid receptor agonists.

Abstract : A collection of arotinoids with a central benzofuran or naphthofuran ring structure was efficiently synthesized by a three-step process that comprises a Sonogashira coupling, an iodine-induced 5-endo-dig cyclization of the o-methoxyphenyl- or naphthyl-ethynyl benzoates, and finally a Suzuki/Sonogashira coupling of the corresponding 3-iodobenzo- or naphthofurans. Most of these 3-substituted naphthofuran arotinoids (but not the 5,7-di-tert-butylbenzofurans with the same substitution pattern at the C2 and C3 positions) are potent agonists of the retinoic acid receptor (RAR) subtypes, with activities in the nanomolar range.
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Submitted on : Friday, May 15, 2009 - 2:23:49 PM
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Efrén Pérez Santín, Harshal Khanwalkar, Johannes J. Voegel, Pascal Collette, Pascale Mauvais, et al.. Highly potent naphthofuran-based retinoic acid receptor agonists.. ChemMedChem, Wiley-VCH Verlag, 2009, 4 (5), pp.780-91. ⟨10.1002/cmdc.200900015⟩. ⟨inserm-00384552⟩



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