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Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents

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Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents

Auteurs : Gary H. Posner [États-Unis] ; Andrew J. Mcriner [États-Unis] ; Ik-Hyeon Paik [États-Unis] ; Surojit Sur [États-Unis] ; Kristina Borstnik [États-Unis] ; Suji Xie [États-Unis] ; Theresa A. Shapiro [États-Unis] ; Adebusola Alagbala [États-Unis] ; Barbara Foster [États-Unis]

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2004.

RBID : ISTEX:F24B472F738FE900C856810DA852F30241659F85

Abstract

In only four chemical steps from naturally occurring artemisinin (1), trioxane dimers 6 and 7 were prepared on a multigram scale in overall 32−44% yields. In mice, both isonicotinate N-oxide dimer 6 and isobutyric acid dimer 7 were considerably more antimalarially efficacious than clinically used sodium artesunate (2) via both oral and intravenous administration. In the transgenic adenocarcinoma of mouse prostate model, some of the trioxane dimers had potent anticancer activity.

Url:

https://api.istex.fr/ark:/67375/TPS-QK2K5DKN-R/fulltext.pdf

DOI: 10.1021/jm0303711

Affiliations:

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Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents

Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents

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Abstract

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