Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.
Journal Article (Journal Article)
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.
Full Text
Duke Authors
Cited Authors
- Huang, L; Yu, D; Ho, P; Qian, K; Lee, K-H; Chen, C-H
Published Date
- July 15, 2008
Published In
Volume / Issue
- 16 / 14
Start / End Page
- 6696 - 6701
PubMed ID
- 18562200
Pubmed Central ID
- PMC2579312
Electronic International Standard Serial Number (EISSN)
- 1464-3391
Digital Object Identifier (DOI)
- 10.1016/j.bmc.2008.05.078
Language
- eng
Conference Location
- England