王小淑,许丽丽,侯星,朱守记.化学通报,2022,85(8):943-950.
喜树碱功能化修饰及抗肿瘤活性研究进展
Research progress in functionalized modification and antitumor activity of camptothecin
投稿时间:2021-12-15  修订日期:2022-03-06
DOI:
中文关键词:  喜树碱  结构修饰  抗肿瘤活性  喹啉环  内酯环
英文关键词:camptothecin  structural modification  antitumor activity  quinoline ring  lactone ring
基金项目:国家自然科学基金项目(21901055)、广西高校中青年教师基础能力提升项目(2018KY0697)和潮州市科技计划项目(2019ZC01)资助
作者单位E-mail
王小淑 广西科技师范学院 食品与生化工程学院 360050592@qq.com 
许丽丽 韩山师范学院 化学与环境工程学院  
侯星 广西科技师范学院 食品与生化工程学院  
朱守记 广西科技师范学院 食品与生化工程学院
韩山师范学院 化学与环境工程学院 
549091121@qq.com 
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中文摘要:
      喜树碱是一种重要的天然产物,具有很强的抗肿瘤活性。然而,喜树碱存在水溶性差、在生理条件下易水解而转为无活性的喜树碱羧酸盐等缺陷,限制了其通过静脉注射的临床应用。而对喜树碱的喹啉环、α-羟基内酯环进行功能化修饰可克服上述缺陷。本文就喜树碱结构的功能化修饰及其抗肿瘤活性进行了综述,以期为其他研究人员更快地开发出具有高效、低毒的新型喜树碱类抗癌药物提供参考。
英文摘要:
      Camptothecin is an important natural product with strong antitumor activity. However, there were some disadvantages for camptothecin, such as poor solubility in water, easy hydrolysis and conversion to camptothecin carboxylate under physiological condition, limiting its clinical applications via intravenous injection. However, it was found that these defects have been overcome via the functionalized modification for the quinoline ring and α-hydroxylactone ring of camptothecin. In order to provide a reference for the development of novel camptothecin anticancer drugs with high efficiency and low toxicity could be more quickly by other researchers, the functionalized modification and antitumor activity of camptothecin have been extensively summarized in this paper.
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