紫杉醇是一种广谱抗癌新药，但存在水溶性差、副作用大的缺点。构效关系是以紫杉醇为先导化合物，通过Ｃ１３侧链和二萜环侧链的改造以及生物学评价而建立的。本文讨论了结构与活性的关系，以期通过化学结构的修饰合成高效低毒易溶于水的紫杉醇类似物。 Paclitaxel is a broad-spectrum anticancer drug, but it has the disadvantages of poor water solubility and large side effects. The structure-activity relationship is based on paclitaxel as the lead compound, established through the modification of the C13 side chain and the diterpene side chain, and biological evaluation. This article discusses the structure and activity of the relationship, with a view to chemical structure modification of the synthesis of highly efficient, low toxicity and water-soluble paclitaxel analogues.