| 鬼臼毒素脲类衍生物的合成和体外抗癌活性的研究 |
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| 引用本文： | ?李楠
?李楠,,,赵阳 赵阳,,
LI Nan,' target="_blank" rel="external">,ZHAO Yang,' target="_blank" rel="external">,WEI Fei,GAO Chen-guang,CAO Bo,GAO Ying,CHEN Hong.Synthesis and biological evaluation of 4-ureido podophyllotoxin derivatives as anticancer agents[J].Journal of Tianjin Medical University,2016,0(3). |
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| Authors: |
LI Nan" target="_blank">LI Nan' target="_blank" rel="external">
LI Nan " target="_blank">' target="_blank" rel="external"> ZHAO Yang " target="_blank">' target="_blank" rel="external"> WEI Fei GAO Chen-guang CAO Bo GAO Ying CHEN Hong |
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| Affiliation: | (1.School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin300070,China;2.Graduate School，Tianjin University of Traditional Chinese Medicine,Tianjin 300193;3.Department of Pharmacognosy, Logistic University of PAP, Tianjin 300309, China) |
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| Abstract: | Objective: To obtain anticancer agents with higher efficiency through a novel series of 4-ureido podophyllotoxin derivatives. Methods: The novel target compounds were synthesized by reacting podophyllotoxin or 4’-demethylepipodophyllotoxin with secondary amines under catalytic agent N, N’-carbonyldiimidazole(CDI). All the compounds were characterized by 1H-NMR and HR-MS. Meanwhile, MTT assay was used to test their cytotoxicity against K562 and Hela cell lines. Results: Eight novel target compounds were synthesized. Among them, compound 6a exhibits was identified to have stronger inhibition effect. Conclusion: The anticancer activity of podophyllotoxin could be improved when itAs C-4 is combined with the structure of ureido and piperazidine. |
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| Keywords: | podophyllotoxins urea N N’- carbonyldiimidazole antitumor activity |
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