| 引用本文: | 于跃，王军飞，王长云，李英霞.抗多药耐药紫杉烷类抗肿瘤药物研究进展[J].中国现代应用药学,2012,29(1):16-23. |
| YU Yue, WANG Junfei, WANG Changyun, LI Yingxia.Progress in the Study of Taxanes against Multi-Drug Resistant Tumor[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(1):16-23. |
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| 摘要: |
| 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。 |
| 关键词: 紫杉烷 多药耐药 抗肿瘤 |
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| 基金项目:国家自然科学基金资助项目(81072525) |
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| Progress in the Study of Taxanes against Multi-Drug Resistant Tumor |
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YU Yue, WANG Junfei, WANG Changyun, LI Yingxia1,2
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1. Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China;2. School of Pharmacy, Fudan University, Shanghai 201203, China
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| Abstract: |
| OBJECTIVE To introduce the structure activity relationships (SAR) of taxanes toward multi-drug resistant tumors and progress on its clinical research. METHODS According to the correlative reports in recent years, both the modifications of taxanes and advances in the development of taxane candidates that either have potential for, or are already in, clinical use are reviewed. RESULTS A number of taxanes exhibiting virtually no difference in potency against the drug-sensitive and drug-resistant cell lines were discovered. CONCLUSION It is essential to grasp the SAR of taxanes against drug-resistant tumors and there is far-reaching significance for the discovery of new generation taxane anticancer agents. |
| Key words: taxane multi-drug resistant anti-tumor |
