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OBJECTIVE: To design and synthesize phenylpyridine substituted semicarbazides and investigate their in vitro antitumor activities. METHODS: The target compounds were synthesized from acetophenone through condensation, cyclization,hydrazinolysis and reaction with isocyanates. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human hepatocelular carcinoma (QGY-7703), non-small cell lung (NCl-H460) and human breast (MCF-7) cancer cell lines by MTT assay. RESULTS Sixteen novel compounds were obtained, and their structures were characterized by 1H-NMR, 13C-NMR and HRMS. In vitro bioassay indicated that most compounds had a certain degree of antitumor activity. Compound 51 displayed the most potential anticancer activity against these cancer cell lines with IC50 value of 9.15, 10.45 and 12.50 μmol·L-1, respectively. CONCLUSION: The series of compounds show preferable antitumor activities, which are worthy of further study.
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Objective To investigate the expression of mitochondrial transcription termination factors (MTERFs) in various tissues and cells, and the changes of MTERFs induced by l-methyl-4-phenyl-l, 2, 3, 6-tetrahydropyridine (MPTP)/l-methyl-4-pheny lpyridine (MPP+). Methods Western blotting was used to measure the expression of the MTERFs in brain, liver, kidney of C57BL mice and in human SH-SY5Y, HCM, L-02 cells. MPTP/MPP+ was injected to imitate PD animal/cell models. The changes of MTERFs protein were detected through western blotting. Results The expression of MTERFs was higher in mice brain and SH-SY5Y cells. In PD mouse model induced by MPTP, MTERF3 reduced significantly. Conclusion The expression of MTERFs was higher in mouse brain and SH-SY5Y cells. After induced by MPTP/MPP+, MTERF3 decreased obviously, which increased transcription level and might involve in a process of Parkinsons disease.