Synthesis and Activity of N'-Substitute-4-{3-(Quinoline-6-yl)Urea} Benzoyl Hydrazide Derivatives
OBJECTIVE To design and synthesize N-substituted methylene-3-(4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzo-hydrazide derivatives,and evaluate their anticancer activities.METHODS Using 3-aminobenzoic acid ethyl ester as the starting rea-gent,a series of target compounds 4a-4p were synthesized in a4-step reaction,and all of the target compounds were structurally char-acterized by1H-NMR,13 C-NMR and HRMS.MTT assay was used to detect the inhibitory effect of synthetic compounds on breast canc-er cells.RESULTS It's showed that the target compounds had certain inhibitory activity on the growth of breast cancer cells,among which compound 4e was the best one,showing obvious inhibitory effect on breast cancer cells.The IC50 value of breast cancer cell line MCF-7 was(2.30±0.34)μmol·L-1,and the toxicity of 4e to normal mammary epithelial cells was low(IC50＞100 pmol·L-1).Thus,4e is better than the positive drug cisplatin.In addition,4e could significantly up-regulate the protein expression level of Nur77 and induce the S-phase arrest of MCF-7.CONCLUSION This series of compounds have good anti-cancer activity and are of interest for further study.
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