| 许颖,付纪源,王雨情,刘冰,陈宁,刘颖杰,于蕾,吴健.化学通报,2022,85(10):1196-1208. |
| 粉防己碱及其衍生物的全合成与结构修饰 |
| Progresses in the Total Synthesis and Structure Modification Studies of Tetrandrine and its Derivatives |
| 投稿时间：2021-11-19 修订日期：2022-03-07 |
| DOI： |
| 中文关键词: 粉防己碱 药理活性 全合成 结构修饰 抗肿瘤 |
| 英文关键词:Tetrandrine Pharmacological activity Fully synthetic structure modification Anti-tumor |
| 基金项目:黑龙江省自然科学基金联合引导项目(LH2020H068)和2021年哈尔滨商业大学教师“创新”项目支持计划资助 |
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| 中文摘要: |
| 粉防己碱为双苄基异喹啉类化合物，主要分布在防已科千金藤属植物粉防己的块根中，具有多种生物活性如镇痛消炎、降压、抗肝纤维化和抗肿瘤等，其中，粉防己碱在抗肿瘤方面的药理活性尤为突出。由于此类化合物具有良好的药理活性，吸引了大量有机合成和药物化学等领域学者的关注。因此，本文从粉防己碱的全合成出发，重点综述了其C-5位，C-14及N-甲基位等位点的结构修饰的方法。在此基础上，对粉防己碱抗肿瘤方面的应用进展进行综述，并简要介绍其合成路线，为新药的研究与开发寻找一条条件温和、产率高、绿色安全、原料易得的合成路线。 |
| 英文摘要: |
| Tetrandrine is a dibenzyl isoquinoline compound, it is mainly distributed in the root tubers of Stephania tetrandra. It has a variety of biological activities such as analgesic and anti-inflammatory, antihypertensive, anti-liver fibrosis and anti-tumor and so on. Among them, the pharmacological activity of tetrandrine in anti-tumor is particularly prominent. Because these compounds have good pharmacological activities, they have attracted the attention of many scholars in the fields of organic synthesis and medicinal chemistry. Therefore, starting from the total synthesis of tetrandrine, this article focuses on the structural modification methods of C-5, C-14 and N-methyl positions. On this basis, the application progress of tetrandrine in anti-tumor is reviewed, and its synthetic route is briefly introduced. so as to find a mild, high yield, green, safe and easy to obtain synthetic route for the research and development of new drugs. |
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