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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...

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Autores principales: Soomro, Shahid, Langenberg, Tobias, Mahringer, Anne, Konkimalla, V Badireenath, Horwedel, Cindy, Holenya, Pavlo, Brand, Almut, Cetin, Canan, Fricker, Gert, Dewerchin, Mieke, Carmeliet, Peter, Conway, Edward M, Jansen, Herwig, Efferth, Thomas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Blackwell Publishing Ltd 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3822625/
https://www.ncbi.nlm.nih.gov/pubmed/20629994
http://dx.doi.org/10.1111/j.1582-4934.2010.01120.x
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author Soomro, Shahid
Langenberg, Tobias
Mahringer, Anne
Konkimalla, V Badireenath
Horwedel, Cindy
Holenya, Pavlo
Brand, Almut
Cetin, Canan
Fricker, Gert
Dewerchin, Mieke
Carmeliet, Peter
Conway, Edward M
Jansen, Herwig
Efferth, Thomas
author_facet Soomro, Shahid
Langenberg, Tobias
Mahringer, Anne
Konkimalla, V Badireenath
Horwedel, Cindy
Holenya, Pavlo
Brand, Almut
Cetin, Canan
Fricker, Gert
Dewerchin, Mieke
Carmeliet, Peter
Conway, Edward M
Jansen, Herwig
Efferth, Thomas
author_sort Soomro, Shahid
collection PubMed
description 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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spelling pubmed-38226252015-04-06 Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties Soomro, Shahid Langenberg, Tobias Mahringer, Anne Konkimalla, V Badireenath Horwedel, Cindy Holenya, Pavlo Brand, Almut Cetin, Canan Fricker, Gert Dewerchin, Mieke Carmeliet, Peter Conway, Edward M Jansen, Herwig Efferth, Thomas J Cell Mol Med Articles 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. Blackwell Publishing Ltd 2011-05 2010-07-12 /pmc/articles/PMC3822625/ /pubmed/20629994 http://dx.doi.org/10.1111/j.1582-4934.2010.01120.x Text en © 2011 The Authors Journal of Cellular and Molecular Medicine © 2011 Foundation for Cellular and Molecular Medicine/Blackwell Publishing Ltd
spellingShingle Articles
Soomro, Shahid
Langenberg, Tobias
Mahringer, Anne
Konkimalla, V Badireenath
Horwedel, Cindy
Holenya, Pavlo
Brand, Almut
Cetin, Canan
Fricker, Gert
Dewerchin, Mieke
Carmeliet, Peter
Conway, Edward M
Jansen, Herwig
Efferth, Thomas
Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title_full Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title_fullStr Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title_full_unstemmed Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title_short Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
title_sort design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties
topic Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3822625/
https://www.ncbi.nlm.nih.gov/pubmed/20629994
http://dx.doi.org/10.1111/j.1582-4934.2010.01120.x
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