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| Synthesis and Antitumor Activity of Two Pyridine-Substituted α,β-Unsaturated Ketones Drugs |
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| DOI： |
| KeyWord:α,β-unsaturated ketone piperidone antitumor cytotoxicity confocal laser scanning microscopy cellular uptake |
| Author | Institution |
| LIU Wen-shuai，CHEN Qin，SUN Ju-feng，WANG Chun-hua，ZHAO Feng，HOU Gui-ge* |
滨州医学院药学院 |
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| Abstract: |
| Two drugs L1 and L2 were prepared by Claisen-Schmidt condensation reaction of 3-pyridinecarboxaldehyde with cyclohexanone or N-methyl-4-piperidinone.They were characterized by FTIR,1H NMR and elemental analysis.Their antitumor activities against human neoplastic cell lines A549,HePG2,MCF-7,SGC-7901,OVCA-433 and their cytotoxicities for HUVEC cell lines by CCK-8 method were subsequently evaluated.Their half maximal inhibitory concentration IC50 values were lower than 10 μmol/L,but their cytotoxicities were markedly lower.In addition,cellular uptake of L2 by HePG2 cells and HUVEC lines was carried out by confocal fluorescence images.The result showed that fluorescent enhancement following the change of time and concentration,further demonstrated the increase of cellular uptake amount of L2 by HePG2 cells.But the result showed that fluorescent intensity uniformity following the change of time and concentration,further demonstrated the uniformity of cellular uptake amount of L2 by HUVEC cells. |
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