2. Academic Validation
  3. 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

  • J Med Chem. 2004 Feb 26;47(5):1299-301. doi: 10.1021/jm0303711.
Gary H Posner 1,  Andrew J McRiner,  Ik-Hyeon Paik,  Surojit Sur,  Kristina Borstnik,  Suji Xie,  Theresa A Shapiro,  Adebusola Alagbala,  Barbara Foster
Affiliations

Affiliation

  • 1 Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N. Charles Street, Baltimore, Maryland 21218-2685, USA. ghp@jhu.edu
PMID: 14971910 DOI: 10.1021/jm0303711
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.

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