Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere

Retinoids act through two distinct hormonal pathways activated by RAR and RXR ligands. We describe the synthesis of C9C10 locked retinoid analogs, including the most potent RXR - specific agonist known to date (Compound 5), and discuss the structural features that lead to this specificity. We descr...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996, Vol.6 (2), p.213-218
Main Authors: Vuligonda, Vidyasagar, Lin, Yuan, Chandraratna, Roshantha A.S.
Format: Article
Language:English
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Summary:Retinoids act through two distinct hormonal pathways activated by RAR and RXR ligands. We describe the synthesis of C9C10 locked retinoid analogs, including the most potent RXR - specific agonist known to date (Compound 5), and discuss the structural features that lead to this specificity. We describe the synthesis of C9-C10 locked retinoid analogs including the most potent RXR - specific agonist known to date (Compound 5, RH), and discuss the structural features that lead to this specificity.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00588-K