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目的综述喜树碱类衍生物的抗癌药理机制及开发应用方面的研究进展。方法以国内外研究文献为基础,对文献资料进行分析和总结。结果喜树碱类衍生物是拓扑异构酶Ⅰ抑制剂,抗癌药物研究中的热点,已广泛应用于临床。本文综述了5种喜树碱类衍生物药物的开发应用最新进展。结论喜树碱类衍生物的抗癌药理作用机制尚未完全阐明,随着对其构效关系及作用机制的不断研究,将会有更多更有效的喜树碱类衍生物成为抗癌的一线药物。
OBJECTIVE: To review the anticancer pharmacological mechanism of camptothecin derivatives and their research progress in the development and application. Methods Based on the domestic and foreign research literature, the literature is analyzed and summarized. Results Camptothecin derivatives are topical inhibitors of topoisomerase I and have been widely used in clinical research. This review summarizes the recent advances in the development and application of five camptothecin derivatives. Conclusions The mechanism of anti-cancer pharmacological action of camptothecin derivatives has not yet been fully elucidated. With the continuous study on their structure-activity relationship and mechanism of action, more and more effective camptothecin derivatives will become the first line of anti-cancer drug.