Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodents.

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.

journal_name

J Med Chem

authors

Posner GH,McRiner AJ,Paik IH,Sur S,Borstnik K,Xie S,Shapiro TA,Alagbala A,Foster B

doi

10.1021/jm0303711

keywords:

subject

Has Abstract

pub_date

2004-02-26 00:00:00

pages

1299-301

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

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