| 摘要: |
| 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。 |
| 关键词: 抗癌新药，红豆杉，紫杉醇，构效关系 |
| DOI： |
| 分类号:Q501 |
| 基金项目: |
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| Structure-Activity Relationship of Taxol-A Novel Antineoplastic Agent |
|
Gao Jinming 1 Fu Jianxi 2\ Zhang Anling 1
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| Abstract: |
| Taxol,as a novel anticancer agent,has been proved to treat a broad spectrum of cancers.But it has the defects of low water-solubility and big side-effect.Being a leading compound,the structure-activity relationship (SAR) of the taxol has been established through the structural modifications of C13 side chain and diterpenoid core of taxol,combined with biological evaluation of taxol analogs.The SAR of taxol is elucidated in order to synthesize taxol analogs with high efficiency,low side effect and high water solubility as well as to deduce its pharmacophores. |
| Key words: novel antineoplastic agent,taxus,taxol,structure-activity relationship |
