基于对多糖基格拉韦结构的修改，我们引入了不同取代基的1,2,3-三唑基团，获得了许多新型多糖基格拉韦衍生物。我们检测了处理了这些衍生物的A549细胞的活性，大多数化合物显示出良好的抑制效果。其中，化合物4b和4g表现出最佳的抑制效果，分别以IC50值为8.72 ± 0.11 μM和12.97 ± 0.32 μM抑制了A549细胞的生长。此外，化合物4g使A549肿瘤细胞发生凋亡和克隆抑制。化合物4g还活化LC3信号通路以诱导肿瘤细胞自噬，并活化γ-H2AX信号通路以诱导肿瘤细胞DNA损伤。 版权所有 © 2023 侯、毛、郭、楼、王、李、王、李和杨。

Based on the modification of the structure of dolutegravir, we introduced 1,2,3-triazole moieties with different substituted groups and obtained a lot of novel dolutegravir derivatives. The activity of A549 cells treated with the derivatives was examined, and most compounds showed good inhibitory effects. Among them, compounds 4b and 4g were the most effective, and inhibited the growth of A549 cells with IC50 values of 8.72 ± 0.11 μM and 12.97 ± 0.32 μM, respectively. In addition, compound 4g induced apoptosis and clonal suppression in A549 tumor cells. Compound 4g also activated the LC3 signaling pathway to induce autophagy in tumor cells, and activated the γ-H2AX signaling pathway to induce DNA damage in tumor cells.Copyright © 2023 Hou, Mao, Guo, Lou, Wang, Li, Wang, Li and Yang.