Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives

被引：33

作者：

Huang, Li ^{[1
]}

Yu, Donglei ^{[2
]}

Ho, Phong ^{[1
]}

Qian, Keduo ^{[2
]}

Lee, Kuo-Hsiung ^{[2
]}

Chen, Chin-Ho ^{[1
]}

机构：

[1] Duke Univ, Med Ctr, Dept Surg, Durham, NC 27710 USA

[2] Univ N Carolina, Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 14期

关键词：

glycyrrhetinic acid; proteasome inhibitor; triterpene;

D O I：

10.1016/j.bmc.2008.05.078

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This study discovered that glycyrrhetinic acid inhibited the human 20S proteasome at 22.3 mu M. Esterification of the C-3 hydroxyl group on glycyrrhetinic acid with various carboxylic acid reagents yielded a series of analogs with marked improved potency. Among the derivatives, glycyrrhetinic acid 3-O-isophthalate (17) was the most potent compound with IC50 of 0.22 mu M, which was approximately 100-fold more potent than glycyrrhetinic acid. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6696 / 6701

页数：6

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