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

被引：42

作者：

Vuligonda, V

Lin, Y

Chandraratna, RAS

机构：

[1] ALLERGAN PHARMACEUT INC,DEPT CHEM,IRVINE,CA 92715

[2] ALLERGAN PHARMACEUT INC,DEPT BIOL,IRVINE,CA 92715

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 02期

关键词：

D O I：

10.1016/0960-894X(95)00588-K

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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页码：213 / 218

页数：6

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