Guéritte-Voegelein F, Guénard D, Potier P
Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette.
C R Seances Soc Biol Fil. 1992;186(5):433-40.
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.
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。