Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site.
Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site.
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DOI：
10.3390/molecules21101375
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发表时间：
2016-10-15
期刊：
影响因子：
--
通讯作者：
Yan B
中科院分区：
文献类型：
--
作者：
Dong M;Liu F;Zhou H;Zhai S;Yan B
微管蛋白抑制剂是一种有效的抗癌药物，但现有的微管蛋白抑制剂在临床应用中存在许多局限性，如多药耐药、不良反应严重、生物利用度低等。因此，一直需要寻找能够克服这些限制的新型微管蛋白抑制剂。针对微管蛋白的天然产物和特权结构促进了微管蛋白抑制剂的发现和优化。本综述将集中于来源于天然产物的新型微管蛋白抑制剂和针对微管蛋白上秋水仙碱结合位点的特权结构。
Tubulin inhibitors are effective anticancer agents, however, there are many limitations to the use of available tubulin inhibitors in the clinic, such as multidrug resistance, severe side-effects, and generally poor bioavailability. Thus, there is a constant need to search for novel tubulin inhibitors that can overcome these limitations. Natural product and privileged structures targeting tubulin have promoted the discovery and optimization of tubulin inhibitors. This review will focus on novel tubulin inhibitors derived from natural products and privileged structures targeting the colchicine binding site on tubulin.
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