Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.

Journal Article (Journal Article)

Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds (2, 4, 8, 9, 10, and 13) showed antiproliferative activities comparable to that of PI-083. Among them, compound 8 was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings endorse further optimization efforts based on this structural phenotype to develop potential anticancer drug candidates.

Full Text

Duke Authors

Cited Authors

  • Xu, K; Xiao, Z; Tang, YB; Huang, L; Chen, C-H; Ohkoshi, E; Lee, K-H

Published Date

  • April 15, 2012

Published In

Volume / Issue

  • 22 / 8

Start / End Page

  • 2772 - 2774

PubMed ID

  • 22437113

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2012.02.086


  • eng

Conference Location

  • England