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