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Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Huang L,Yu D,Ho P,Qian K,Lee KH,Chen CH

doi

10.1016/j.bmc.2008.05.078

subject

Has Abstract

pub_date

2008-07-15 00:00:00

pages

6696-701

issue

14

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00517-8

journal_volume

16

pub_type

杂志文章

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