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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...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Blackwell Publishing Ltd
2011
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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. |
format | Online Article Text |
id | pubmed-3822625 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Blackwell Publishing Ltd |
record_format | MEDLINE/PubMed |
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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