| 熊樱,李英霞.海洋来源的微管蛋白聚集抑制剂Tubulysins的研究进展[J].中国海洋药物,2020,39(2):87-92. |
| 海洋来源的微管蛋白聚集抑制剂Tubulysins的研究进展 |
| Research progress on tubulin aggregation inhibitor tubulysins |
| 投稿时间：2019-05-11 修订日期：2019-10-20 |
| DOI： |
| 中文关键词: tubulysins 微管蛋白 构效关系 合成研究；抗肿瘤药物 |
| English Keywords:tubulysins tubulin structure-activity relationship chemosynthesis anti-tumor drug |
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| 中文摘要: |
| 自2000年首次分离得到以来,tubulysins以其异常强力的抗增殖活性和在抗肿瘤药物研究方面表现出的潜力,引起了人们的广泛关注。在二十年的时间里,研究者完成了结构鉴定,生合成,全合成,构效关系,药物偶联等一系列工作,并将EC1456作为晚期实体瘤治疗药物推进临床Ⅰ期实验。本文将回顾这类化合物的分离鉴定、合成方法和构效关系的取得的研究进展,以期为进一步的药物开发提供帮助。 |
| English Summary: |
| Ever since first isolated in 2000, tubulysins have sparked great interest due to their exceptionally potent antiproliferative activity due to its strong anti-proliferative activity and potential in anti-tumor drug discovery. Over twenty years, the researchers completed a series of work including structure identification, biosynthesis, total synthesis, structure-activity relationship and drugs coupling development, and the a folate-tubulysin conjugate EC1456 has been advanced to phaseⅠclinical trials for solid tumor treatment. This article will review the progress in the isolation, synthesis, and structure-activity relationships of these compounds, so as to provied information for further drug development. |
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