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作为抗癌剂的微管相互作用天然产物。

Tubulin-interactive natural products as anticancer agents.

机构信息

Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061-0212, USA.

出版信息

J Nat Prod. 2009 Mar 27;72(3):507-15. doi: 10.1021/np800568j.

Abstract

This review provides an overview of the discovery, structures, and biological activities of anticancer natural products that act by inhibiting or promoting the assembly of tubulin to microtubules. The emphasis is on providing recent information on those compounds in clinical use or in advanced clinical trials. The vinca alkaloids, the combretastatins, NPI-2358, the halichondrin B analogue eribulin, dolastatin 10, noscapine, hemiasterlin, and rhizoxin are discussed as tubulin polymerization inhibitors, while the taxanes and the epothilones are the major classes of tubulin polymerization promoters presented, with brief treatments of discodermolide, eleutherobin, and laulimalide. The challenges and future directions of tubulin-interactive natural products-based drug discovery programs are also discussed briefly.

摘要

这篇综述概述了通过抑制或促进微管蛋白组装来发挥作用的抗癌天然产物的发现、结构和生物活性。重点是提供那些在临床使用或在临床试验中处于先进阶段的化合物的最新信息。长春碱类生物碱、考布他汀类、NPI-2358、海兔内酯类似物埃博霉素、多紫杉醇 10、石蒜碱、海兔内酯和瑞香毒素被讨论为微管蛋白聚合抑制剂,而紫杉醇类和埃坡霉素类则是主要的微管蛋白聚合促进剂类别,简要讨论了 discodermolide、eleutherobin 和 laulimalide。还简要讨论了基于微管蛋白相互作用的天然产物药物发现计划的挑战和未来方向。

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