Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties. J Cell Mol Med

Dafra Pharma Research & Development, Slachthuisstraat, Turnhout, Belgium.
Journal of Cellular and Molecular Medicine (Impact Factor: 4.01). 05/2011; 15(5):1122-35. DOI: 10.1111/j.1582-4934.2010.01120.x
Source: PubMed


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.

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Available from: Gert Fricker, Jul 29, 2014
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    • "As a consequence of this awareness, increased research efforts are focused on new derivatives with innovative applications and improved properties. Major pharmaceutical companies are beginning to take an interest in developing new trioxane compounds [18] [19] [20] [21]. Current analytical techniques describe derivatisation-based methods [22], gas chromatography (GC) [23], thin layer chromatography (TLC) [24], supercritical fluid chromatography (SCFC) [25], spectroscopic [26] and immunological techniques [27] [28], but it is clear that the main-stream methods are mainly based on high performance liquid chromatography (HPLC), coupled to ultra violet (UV), evaporative light scattering detector (ELSD), electron capture detection (ECD) or electrospray ionisation (ESI)–mass spectrometry (MS) detection [29] [30] [31] [32]. "
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