Synthesis and biological evaluation of novel spin labeled 18β-glycyrrhetinic acid derivatives.

Published

Journal Article

Eighteen novel spin-labeled 18β-glycyrrhetinic acid (GA) derivatives were designed, synthesized, and evaluated for cytotoxicity against four human tumor cell lines (A-549, DU-145, KB and KBvin). Most of the derivatives showed more significant cytotoxicity than that of the parent compound GA. The best compound, 6j, with a tryptophan amino moiety and piperidine nitroxyl radical showed GI(50) values of 13.7-15.0 μM, and was fivefold more potent than GA. In a mechanism of action study, compound 7a was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings support further optimization efforts based on 18β-GA as a lead compound to develop potential anticancer drug candidates.

Full Text

Duke Authors

Cited Authors

  • Liu, Y; Qian, K; Wang, C-Y; Chen, C-H; Yang, X; Lee, K-H

Published Date

  • December 15, 2012

Published In

Volume / Issue

  • 22 / 24

Start / End Page

  • 7530 - 7533

PubMed ID

  • 23122524

Pubmed Central ID

  • 23122524

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2012.10.041

Language

  • eng

Conference Location

  • England