School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Eur J Med Chem. 2012 Jan;47(1):424-31. doi: 10.1016/j.ejmech.2011.11.011. Epub 2011 Nov 13.
Recently, a novel glycosylated diphyllin derivative 11 which exhibiting potent anticancer activity by targeting topoisomerase IIα was reported by our group. In order to provide more molecules for structure-activity relationship (SAR) studies, 12 new glycosylated diphyllin analogs have been designed, synthesized, and evaluated for their biological activities. The SAR analysis revealed that (i) the sugar moiety on the diphyllin is essential for the anticancer activity; (ii) equatorial C4'-OH on the sugar is superior to the axial one, and (iii) a proper cyclic lipophilic group at the C4' and C6' of sugar might enhance the anticancer activity.
最近，我们小组报道了一种新型的糖苷化二萜内酯衍生物 11，它通过靶向拓扑异构酶 IIα 表现出很强的抗癌活性。为了提供更多的分子进行结构活性关系（SAR）研究，我们设计、合成了 12 种新的糖苷化二萜内酯类似物，并对它们的生物活性进行了评价。SAR 分析表明：（i）二萜内酯上的糖基对于抗癌活性是必需的；（ii）糖上的 C4'-OH 处于平伏键优于直立键；（iii）在糖的 C4'和 C6'位上引入适当的环状脂环基团可能会增强抗癌活性。
