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

被引：114

作者：

Posner, GH

McRiner, AJ

Paik, IH

Sur, S

Borstnik, K

Xie, SJ

Shapiro, TA

Alagbala, A

Foster, B

机构：

[1] Johns Hopkins Univ, Sch Arts & Sci, Dept Chem, Baltimore, MD 21218 USA

[2] Johns Hopkins Univ, Malaria Res Inst, Johns Hopkins Bloomberg Sch Publ Hlth, Baltimore, MD 21205 USA

[3] Johns Hopkins Univ, Sch Med, Dept Med, Div Clin Pharmacol, Baltimore, MD 21205 USA

[4] Roswell Pk Canc Inst, Dept Pharmacol & Therapeut, Buffalo, NY 14263 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 05期

关键词：

D O I：

10.1021/jm0303711

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1299 / 1301

页数：3

共 15 条

[1] Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates [J].