Dalby Stephen M, Paterson Ian
Cambridge University Chemical Laboratory, Lensfield Road, Cambridge, CB2 1EW, UK.
Curr Opin Drug Discov Devel. 2010;13(6):777-94.
Recent highlights in the synthesis of polyketide natural products and structural analogs as promising anticancer agents are described, focusing on the halichondrins and eribulin (Eisai), together with recently published research on bryostatin, dictyostatin, spongistatin, peloruside, spirastrellolide, palmerolide, reidispongiolide, spirangien and saliniketals. These examples demonstrate the centrality of bioactive polyketides in current and future anticancer drug discovery, and the increasingly key role of efficient total synthesis in providing a sustainable supply of such compounds for drug development.
本文描述了聚酮类天然产物及其结构类似物作为有前景的抗癌药物合成方面的近期亮点，重点介绍了海兔毒素和艾日布林（卫材公司），以及最近发表的关于苔藓抑素、双鞭甲藻素、海绵抑素、帕罗西汀、螺旋星孢菌素、帕默罗利德、瑞德海绵内酯、螺旋海绵素和盐基缩酮的研究。这些例子表明了生物活性聚酮化合物在当前和未来抗癌药物发现中的核心地位，以及高效全合成在为药物开发可持续供应此类化合物方面日益关键的作用。
