Synthesis and Proteasome Inhibition of Glycyrrhetinic Acid Derivatives

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2008 Jun 20

PMID 18562200

Citations 6

Authors

Li Huang

Donglei Yu

Phong Ho

Keduo Qian

Kuo-Hsiung Lee

Chin-Ho Chen

Affiliations

Soon will be listed here.

Abstract

This study discovered that glycyrrhetinic acid inhibited the human 20S proteasome at 22.3microM. 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 IC(50) of 0.22microM, which was approximately 100-fold more potent than glycyrrhetinic acid.

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