Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties.

Artemisinins are plant products with a wide range of medicinal applications. Most prominently, artesunate is a well tolerated and effective drug for treating malaria, but is also active against several protozoal and schistosomal infections, and additionally exhibits anti-angiogenic, anti-tumorigenic and anti-viral properties. The array of activities of the artemisinins, and the recent emergence of malaria resistance to artesunate, prompted us to synthesize and evaluate several novel artemisinin-like derivatives. Sixteen distinct derivatives were therefore synthesized and the in vitro cytotoxic effects of each were tested with different cell lines. The in vivo anti-angiogenic properties were evaluated using a zebrafish embryo model. We herein report the identification of several novel artemisinin-like compounds that are easily synthesized, stable at room temperature, may overcome drug-resistance pathways and are more active in vitro and in vivo than the commonly used artesunate. These promising findings raise the hopes of identifying safer and more effective strategies to treat a range of infections and cancer.
AuthorsShahid Soomro, Tobias Langenberg, Anne Mahringer, V Badireenath Konkimalla, Cindy Horwedel, Pavlo Holenya, Almut Brand, Canan Cetin, Gert Fricker, Mieke Dewerchin, Peter Carmeliet, Edward M Conway, Herwig Jansen, Thomas Efferth
JournalJournal of cellular and molecular medicine (J Cell Mol Med) Vol. 15 Issue 5 Pg. 1122-35 (May 2011) ISSN: 1582-4934 [Electronic] England
PMID20629994 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Copyright© 2011 The Authors Journal of Cellular and Molecular Medicine © 2011 Foundation for Cellular and Molecular Medicine/Blackwell Publishing Ltd.
Chemical References
  • Angiogenesis Inhibitors
  • Artemisinins
  • Plant Extracts
  • artemisinine
  • Angiogenesis Inhibitors (chemical synthesis, pharmacology)
  • Animals
  • Artemisia annua (chemistry)
  • Artemisinins (chemistry, pharmacology)
  • Cell Proliferation (drug effects)
  • Cells, Cultured
  • Drug Resistance
  • Flow Cytometry
  • Plant Extracts (chemistry)
  • Structure-Activity Relationship
  • Swine
  • Zebrafish (embryology)

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