9-cis-Retinoic acid analogues with bulky hydrophobic rings: new RXR-selective agonists

…, MJ Vega, S Kammerer, A Rossin, P Germain…

文献索引：Alvarez, Rosana; Vega, M. Jesus; Kammerer, Sabrina; Rossin, Aurelie; Germain, Pierre; Gronemeyer, Hinrich; De Lera, Angel R. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 24 p. 6117 - 6122

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被引用次数: 16

摘要

Stille cross-coupling of aryltriflates 10 and dienylstannane 11, oxidation and Horner– Wadsworth–Emmons reaction afforded stereoselectively retinoates 15. Saponification provided the carboxylic acids 8a and 8b, retinoids that incorporate a bulky hydrophobic ring while preserving the 9-cis-geometry of the parent system. In contrast to the pan-RAR/RXR agonistic profile of the lower homologue of 8a, compound 7 (LG100567), retinoids 8 ...