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

  • Eur J Med Chem. 2013 Sep:67:447-53. doi: 10.1016/j.ejmech.2013.06.046.
Zhiliang Lv  1 ,  Yikai Zhang ,  Mingfeng Zhang ,  Huan Chen ,  Zhenliang Sun ,  Dongping Geng ,  Chunjuan Niu ,  Ke Li
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
PMID: 23920246 DOI: 10.1016/j.ejmech.2013.06.046
Abstract

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).

Keywords
2-Pyridone derivatives; Anti-cancer activity; Click chemistry; Synthesis.