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

Gary H. Posner, Andrew J. McRiner, Ik Hyeon Paik, Surojit Sur, Kristina Borstnik, Suji Xie, Theresa A. Shapiro, Adebusola Alagbala, Barbara Foster

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)1299-1301
Number of pages3
JournalJournal of medicinal chemistry
Volume47
Issue number5
DOIs
StatePublished - Feb 26 2004

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    Posner, G. H., McRiner, A. J., Paik, I. H., Sur, S., Borstnik, K., Xie, S., Shapiro, T. A., Alagbala, A., & Foster, B. (2004). Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents. Journal of medicinal chemistry, 47(5), 1299-1301. https://doi.org/10.1021/jm0303711