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目的介绍紫杉烷类活性分子与多药耐药肿瘤的构效关系及其临床研究进展。方法综述了近年来国内外相关报道,对紫杉醇6大区域的相关改造分别进行讨论,并就其临床研究及开发上市状况进行概述。结果发现了许多对敏感肿瘤和多药耐药肿瘤抑制活性相当的紫杉烷类药物候选分子。结论熟悉紫杉烷类活性分子与多药耐药肿瘤的构效关系,对开发新一代紫杉烷类抗肿瘤药物具有深远意义。
Objective To introduce the structure-activity relationship of taxane-like active molecules and multi-drug resistant tumor and its clinical research progress. Methods The related reports at home and abroad in recent years were reviewed. The related transformation of paclitaxel in six major regions were discussed respectively, and the clinical research and the status of development and listing were summarized. As a result, many taxane-like drug candidates have been found that are comparable in sensitivity to tumor and multi-drug resistant tumors. Conclusion It is of great significance to develop a new generation of taxane anti-tumor drugs to be familiar with the structure-activity relationship of taxane active molecules and multidrug-resistant tumors.