| 非喜树碱类DNA拓扑异构酶Ⅰ抑制剂的研究进展 |
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| 引用本文： | 孙远,王华萍,周游,尤启冬.非喜树碱类DNA拓扑异构酶Ⅰ抑制剂的研究进展[J].药学进展,2011,35(9):385-395. |
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| 作者姓名： | 孙远 王华萍 周游 尤启冬 |
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| 作者单位： | 中国药科大学药物化学教研室,江苏南京,210009 |
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| 基金项目： | "重大新药创制"国家科技重大专项课题 |
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| 摘 要： | DNA拓扑异构酶Ⅰ（TopoⅠ）是抗肿瘤治疗的重要靶点。喜树碱类TopoⅠ抑制剂已在肿瘤的临床治疗中被广泛使用,但受分子骨架制约,其存在水溶性低、稳定性差、毒副作用大等缺点,而具有新颖结构的非喜树碱类TopoⅠ抑制剂则有望克服这些缺点。按结构分类综述非喜树碱类TopoⅠ抑制剂的抗肿瘤活性及构效关系研究新进展。
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| 关 键 词： | 拓扑异构酶Ⅰ抑制剂 非喜树碱类化合物 抗肿瘤活性 构效关系 |
Recent Advances in Non-camptothecin DNA Topoisomerase Ⅰ Inhibitors as Anticancer Drugs |
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| SUN Yuan,WANG Hua-ping,ZHOU You,YOU Qi-dong.Recent Advances in Non-camptothecin DNA Topoisomerase Ⅰ Inhibitors as Anticancer Drugs[J].Progress in Pharmaceutical Sciences,2011,35(9):385-395. |
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| Authors: | SUN Yuan WANG Hua-ping ZHOU You YOU Qi-dong |
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| Affiliation: | SUN Yuan,WANG Hua-ping,ZHOU You,YOU Qi-dong*(Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China) |
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| Abstract: | DNA Topoisomerase I(Topo I) is a promising and important target for cancer therapy.Camptothecin derivatives as Topo I inhibitors have been widely used to treat tumors in clinic.However,due to some defects of molecular scaffold,camptothecin derivatives have commonly shown poor aqueous-solubility,instability and high toxicity.Developing non-camptothecins as Topo I inhibitors with new scaffold can be expected to overcome these shortcomings.The recent advances in study on the anti-tumor activities and structure... |
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| Keywords: | topoisomerase Iinhibitor non-camptothecins antitumor activity structure-activity relationship |
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