Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs
作者:Tao Deng、Xianglan Mao、Yan Xiao、Zhigang Yang、Xing Zheng、Zhong-Xing Jiang
DOI:10.1016/j.bmcl.2018.12.059
日期:2019.2
Camptothecin, which represents a class of natural products with high anticancer activity, suffers low water solubility which hampers its clinic application. To address this issue, monodisperse polyethylene glycols were employed to modify this class of natural products, including Camptothecin, 10-Hydroxycamptothecin, and SN38. Through selective modification with a series of monodisperse polyethylene
喜树碱代表一类具有高抗癌活性的天然产物,其水溶性低,妨碍了其临床应用。为了解决这个问题,单分散聚乙二醇被用于修饰这类天然产物,包括喜树碱,10-羟基喜树碱和SN38。通过使用一系列单分散聚乙二醇进行选择性修饰,使用基于大环硫酸盐的策略制备了31种喜树碱衍生物,其中包括9种醚和22种碳酸酯。单分散聚乙二醇改性为喜树碱衍生物提供了高纯度和微调的水溶性。通过理化和生物学分析,发现了一些具有良好溶解性,细胞毒性的新型前药,