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New retinoid chemotypes: 9-cis-retinoic acid analogs with hydrophobic rings derived from terpenes as selective RAR agonists.

Abstract : A series of 9-cis-retinoic acid analogs modified at the hydrophobic ring with a (bi)cyclohexenyl moiety derived from natural terpenes has been stereoselectively prepared using a Suzuki cross-coupling as key step. Transient transactivation studies indicate that modification of the hydrophobic ring impacts dramatically on RXR-binding and transactivation, with most retinoids being inactive on RXRbeta, while preserving their RAR pan-agonist profile. Furthermore, only the RARgamma subtype was capable of enantiomeric discrimination with some pairs of enantiomeric terpene-retinoids.
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https://www.hal.inserm.fr/inserm-00350716
Contributor : Maité Peney <>
Submitted on : Wednesday, January 7, 2009 - 3:29:24 PM
Last modification on : Tuesday, May 26, 2020 - 11:50:03 AM

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Susana Alvarez, Yolanda Pazos-Randulfe, Harshal Khanwalkar, Pierre Germain, Rosana Alvarez, et al.. New retinoid chemotypes: 9-cis-retinoic acid analogs with hydrophobic rings derived from terpenes as selective RAR agonists.. Bioorganic and Medicinal Chemistry, Elsevier, 2008, 16 (22), pp.9719-28. ⟨10.1016/j.bmc.2008.09.069⟩. ⟨inserm-00350716⟩

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