Design and synthesis of novel 2′-hydroxy group substituted 2-pyridone derivatives as anticancer agents

•We synthesized a series of novel 2-pyridone derivatives.•Click reaction was employed.•All resultant compounds were evaluated for their in vitro cytotoxic activities.•The results showed some of resultant compounds have potential anti-cancer activity.

We have synthesized a series of novel 2-pyridone derivatives with 1,2,3-triazole and evaluated their anti-tumor activities in vitro. The bioassays showed that the majority of the resultant compounds exerted inhibitory effects on six human cancer cell lines to various extents. In particular, compound 10k showed the best anti-tumor activities (IC50 values of A549, HeLa and SW480 cancer cell lines were 0.86 ± 0.17 μM, 0.54 ± 0.23 μM and 0.21 ± 0.13 μM, respectively).

Graphical abstractThis work describes the design and synthesis of 2-pyridone derivatives with moderate to good in vitro anti-cancer activity.Figure optionsDownload full-size imageDownload as PowerPoint slide