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类黄酮细胞周期蛋白依赖性激酶抑制剂的合成与抗癌活性研究
The Synthesis and Anticancer Activity Study of Flavonoids as CDK Inhibitors
【摘要】 目的:寻找活性更好的类黄酮CDK s抑制剂。方法:利用M ann ich反应制备7个查尔酮类类黄酮。结果:目标化合物的结构经过IR、1H-NMR、ESI-MS确证,并测定了化合物对CDK1的抑制活性以及对HCT116的体外抗肿瘤活性。结论:其中有3个化合物对CDK1的抑制活性高于对照F lavop iridol,所有化合物对HCT116显示较强的抑制活性。
【Abstract】 Objective: To search flavonoids with higher CDK inhibitive ability.Methods: Chalcone route was applied to synthesize 7 chalcones.Results: The structure of target compounds was confirmed by IR,1H-NMR and ESI-MS.The CDK1 inhibitive ability and the anticancer activity against HCT116 of the compounds were determined.Conclusion: The CDK1 inhibitive ability of three compounds is higher than flavopiridol,and all compounds demonstrate higher cytotoxicity activity against HCT116.
【基金】 以金属蛋白酶为靶点的抗癌先导化合物的发现国家科技部863课题(No2007AA02Z314)
- 【文献出处】 包头医学院学报 ,Journal of Baotou Medical College , 编辑部邮箱 ,2011年04期
- 【分类号】R914.5;R96
- 【被引频次】4
- 【下载频次】126