Synthesis and evaluation of novel isoxazolyl chalcones as potential anticancer agents
作者： Maosheng Wan , Linyan Xu , Li Hua , Ailing Li , Shuqing Li
DOI: 10.1016/J.BIOORG.2014.03.004
关键词:
摘要: Abstract A series of novel isoxazolyl chalcones were synthesized and evaluated for their activities in vitro against four types human non-small cell lung cancer cells, including H1792, H157, A549 Calu-1 cells. The preliminary biological screening showed that compounds 5d 5f – i exhibited significant cytotoxicity, particularly, 5h identified as the most potent anticancer agents with IC 50 values 1.35–2.07 μM 7.27–11.07 μM H175, lines, respectively. Compounds 5f–i could induce apoptosis cells by death receptor 5 (DR5) mediated extrinsic pathways. structure–activity relationship study bearing electron withdrawing groups (EWG) at 2-position phenyl ring Ar group more effective than those EWG 4-position. These results further demonstrated scaffolds designed this work might lead to discovery anti-lung agents.
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