Design,Synthesis and Anti-cervical Cancer Activity of Piperine-bicycloamide Derivatives
In this paper,a series of piperine-dicycloamide derivatives was synthesized using piperine as parent nucleus,and their structures were confirmed by means of nuclear magnetic resonance hydrogen spectroscopy(1H NMR),nuclear magnetic resonance carbon spectroscopy(13C NMR)and high-resolution mass spectrometry(HRMS).Methyl thiazolyl tetrazolium(MTT)assay showed that these compounds had good inhibitory effects on kidney cells(293T),cervical cancer(HeLa)and breast cancer(MD-MB-321).Most derivatives had better inhibitory activity on HeLa cells than positive controls fluorouracil(5-FU)and piperine,and compound 6b had the highest anti-proliferative activity on HeLa cells.The half maximal inhibitory concentration(IC50)of MDA-MB-321 cells was 3.49 μmol/L,and the IC50 of MDA-MB-321 cells was 20.89 μmol/L.The mechanism study showed that compound 6b not only effectively inhibited the migration,invasion,adhesion and cloning ability of HeLa cells,but also showed a strong inhibitory effect on the growth of xenografts of HeLa cells.Therefore,compound 6b has the potential to be a lead compound in tumor therapy.
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