Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 5, Pages 1299-1301Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0303711
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Funding
- NCI NIH HHS [CA52284] Funding Source: Medline
- NCRR NIH HHS [RR-00052] Funding Source: Medline
- NIAID NIH HHS [AI34885] Funding Source: Medline
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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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