Synthesis and antitumor activity in vitro of indole-1,3,4-oxadiazole derivatives
Objective To synthesize indole-1,3,4-oxadiazole derivatives and investigate antitumor activities in vitro.Methods Taking 1H-indole-3-carbohydrazide as the starting material,the target compounds were obtained through[4+1]cycloaddition reaction,hydrolysis reaction and condensation reaction.Antitumor activity in vitro of target compounds against HeLa,SCG-7901,and MDA-MB-231 cells were evaluated by MTT assay.The effect of compound 6f against the growth of SCG-7901 cells was assessed by colony formation assay,the effect of it on apoptosis and necrosis in SCG-7901 cells was detected using Annexin V-APC/PI double staining method,the effect of it on nuclear chromatin morphological changes of SCG-7901 cells were examined using DAPI staining method,and the effect of it on contents of reactive oxygen species(ROS)in SCG-7901 cells was detected using DCFH-DA staining method.Results Fifteen indole-1,3,4-oxadiazole derivatives were synthesized and their structures were characterized by 1H-NMR,13C-NMR,and HR-ESI-MS.Some compounds exhibited significant antitumor activity,among which compound 6f exhibited significant anti-proliferative effects against all three tumor cell lines and had certain selectivity.Further research has shown that compound 6f promoted cell production of ROS generation,inhibited cell proliferation,and induced cell apoptosis in a concentration dependent manner.Conclusion Some indole-1,3,4-oxadiazole derivatives have shown good antitumor activity,providing ideas for further research on the anti-tumor activity of these compounds.
NETL
NSTL
万方数据
