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[植物源抗癌物质。纺锤体毒素:长春新碱、长春新碱和诺维本;紫杉醇和多西他赛]

[Anticancer substances of vegetable origin. Spindle poisons: vincaleukoblastine, leurocristine and navelbine; taxol and taxotere].

作者信息

Guéritte-Voegelein F, Guénard D, Potier P

机构信息

Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette.

出版信息

C R Seances Soc Biol Fil. 1992;186(5):433-40.

PMID:1363958
Abstract

The biological activity of spindle poisons can easily be measured using an in vitro assay based on the interaction of these substances with their cellular "receptor": tubulin. The use of this assay led us to select Navelbine and Taxotere as antimitotic substances. These compounds, as well as their natural parents: vincaleucoblastine, leurocristine and taxol respectively, have been obtained by semi-synthesis using relatively abundant natural precursors as starting materials. This paper summarizes the preparation of these important anticancer drugs.

摘要

纺锤体毒素的生物活性可以通过基于这些物质与其细胞“受体”:微管蛋白相互作用的体外试验轻松测定。使用该试验使我们选择了诺维本和泰索帝作为抗有丝分裂物质。这些化合物及其天然母体:长春碱、长春新碱和紫杉醇,分别是通过以相对丰富的天然前体为起始原料进行半合成而获得的。本文总结了这些重要抗癌药物的制备方法。

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