Growth inhibitory activity for cancer cell lines of lapachol and its natural and semi-synthetic derivatives

Bioorg Med Chem Lett. 2014 Jan 15;24(2):454-7. doi: 10.1016/j.bmcl.2013.12.049. Epub 2013 Dec 18.


A series of 17 selected natural and semisynthetic 1,4-naphthoquinones were synthesized, and their growth inhibitory activity was evaluated in vitro. The compounds were tested on six human cancer cell lines using the MTT colorimetric assay. The data revealed that of the chemicals under study only lapachol, its acetate and 3-geranyllawsone displayed the highest activity, recording mean IC50 values ranging from 15 to 22 μM.

Keywords: 1,4-Naphthoquinones; Cancer; In vitro growth inhibition; Lapachol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Cell Line, Tumor
  • Colorimetry / methods
  • Growth Inhibitors / chemistry*
  • Growth Inhibitors / therapeutic use
  • Humans
  • Naphthoquinones / chemistry*
  • Naphthoquinones / therapeutic use
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Plant Extracts / chemistry*
  • Plant Extracts / therapeutic use


  • Antineoplastic Agents, Phytogenic
  • Growth Inhibitors
  • Naphthoquinones
  • Plant Extracts
  • lapachol