Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
Eur J Med Chem. 2013 Sep;67:447-53. doi: 10.1016/j.ejmech.2013.06.046. Epub 2013 Jul 1.
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).
我们合成了一系列含有 1,2,3-三唑的新型 2-吡啶酮衍生物，并评估了它们在体外的抗肿瘤活性。生物测定结果表明，大多数产物对六种人癌细胞系均有不同程度的抑制作用。特别是化合物 10k 表现出最好的抗肿瘤活性（A549、HeLa 和 SW480 癌细胞系的 IC50 值分别为 0.86±0.17 μM、0.54±0.23 μM 和 0.21±0.13 μM）。
