Synthesis and proteasome inhibition of lithocholic acid derivatives.

Journal Article (Journal Article)

A new class of proteasome inhibitors was synthesized using lithocholic acid as a scaffold. Modification at the C-3 position of lithocholic acid with a series of acid acyl groups yielded compounds with a range of potency on proteasome inhibition. Among them, the phenylene diacetic acid hemiester derivative (13) displayed the most potent proteasome inhibition with IC(50) = 1.9 μM. Enzyme kinetic analysis indicates that these lithocholic acid derivatives are noncompetitive inhibitors of the proteasome.

Full Text

Duke Authors

Cited Authors

  • Dang, Z; Lin, A; Ho, P; Soroka, D; Lee, K-H; Huang, L; Chen, C-H

Published Date

  • April 1, 2011

Published In

Volume / Issue

  • 21 / 7

Start / End Page

  • 1926 - 1928

PubMed ID

  • 21388808

Pubmed Central ID

  • PMC3072167

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2011.02.041

Language

  • eng

Conference Location

  • England