Synthesis and biological activity of novel shikonin analogues

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):735-7. doi: 10.1016/j.bmcl.2008.12.032.
Wenjing Wang  1 ,  Mei Dai ,  Caihua Zhu ,  Jiangang Zhang ,  Liping Lin ,  Jian Ding ,  Wenhu Duan
Affiliations
  • 1. Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
PMID: 19111464 DOI: 10.1016/j.bmcl.2008.12.032
Abstract

A series of shikonin analogues with side chain variants have been synthesized and evaluated for antitumor activity. These novel analogues show a broad spectrum of in vitro cytotoxicity against various Cancer cell lines. Additionally, some analogues were also found to have the ability to decrease the expression level of HIF-1alpha in breast Cancer cells MDA-MB-231 under hypoxia. The features of these analogues suggest their potential in Cancer therapy.