Title: Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
Authors: Soomro, Shahid ×
Konkimalla, V Badireenath
Langenberg, Tobias
Mahringer, Anne
Horwedel, Cindy
Holenya, Pavlo
Brand, Almut
Catin, Canan
Fricker, Gert
Dewerchin, Mieke
Carmeliet, Peter
Conway, Edward M
Jansen, Herwig
Efferth, Thomas #
Issue Date: May-2011
Publisher: Wiley-Blackwell Publishing Ltd.
Series Title: Journal of Cellular and Molecular Medicine vol:15 issue:5 pages:1122-1135
Abstract: Abstract 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, and 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.
ISSN: 1582-4934
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular and Vascular Biology
Vesalius Research Centre (-)
Laboratory of Angiogenesis and Vascular Metabolism (Vesalius Research Center) (+)
× corresponding author
# (joint) last author

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