Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers

被引：136

作者：

Posner, GH ^{[1
]}

Ploypradith, P

Parker, MH

O'Dowd, H

Woo, SH

Northrop, J

Krasavin, M

Dolan, P

Kensler, TW

Xie, SJ

Shapiro, TA

机构：

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

[2] Johns Hopkins Univ, Sch Hyg & Publ Hlth, Div Toxicol Sci, Baltimore, MD 21205 USA

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 42卷 / 21期

关键词：

D O I：

10.1021/jm990363d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

引用

页码：4275 / 4280

页数：6

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