4.5 Article

Synthesis and biological activity of novel shikonin analogues

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 3, Pages 735-737

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.032

Keywords

Shikonin analogue; Synthesis; Cytotoxicity; Hypoxia-inducible factor 1 alpha

Funding

  1. National Science Foundation of China [0801031005, 0801281005]
  2. Chinese National Programs for High Technology Research and Development [0604071005, 0704051005]

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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-1 alpha in breast cancer cells MDA-MB-231 under hypoxia. The features of these analogues suggest their potential in cancer therapy. (C) 2008 Elsevier Ltd. All rights reserved.

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