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首页> 外文期刊>Journal of Medicinal Chemistry >Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers.
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Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers.

机译:青蒿素衍生的化学作用强的三恶烷二聚体的抗疟,抗增殖和抗肿瘤活性。

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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.
机译:天然三恶烷青蒿素(1)的九种C-10非缩醛衍生物使用一些新化学方法制备为二聚体。按照设计,每个二聚体在化学上是稳定的。 C-10烯烃二聚体7和C-10饱和二聚体8-13在体外均表现出良好的抗疟和抗增殖活性。在NCI体外60细胞株测定中,二聚体8、10和12在抑制某些人类癌细胞系生长方面特别有效且具有选择性。

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