| 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 |
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| 引用本文： | 李艳玲,方浩,徐文方.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[J].包头医学院学报,2011,27(4):12-14. |
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| 作者姓名： | 李艳玲 方浩 徐文方 |
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| 作者单位： | 山东大学药学院,山东济南250012;包头医学院药学院;山东大学药学院,山东济南,250012 |
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| 基金项目： | 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) |
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| 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。
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| 关 键 词： | 查尔酮 CDK1抑制活性 体外抗肿瘤活性 |
The Synthesis and Anticancer Activity Study of Flavonoids as CDK Inhibitors |
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| LI Yanling,FANG Hao,XU Wenfang.The Synthesis and Anticancer Activity Study of Flavonoids as CDK Inhibitors[J].Journal of Baotou Medical College,2011,27(4):12-14. |
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| Authors: | LI Yanling FANG Hao XU Wenfang |
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| Institution: | LI Yanling(1,2),FANG Hao1,XU Wenfang1(1.School of Pharmacy,Shandong University,Ji'nan 250012,China,2.Baotou Medical College) |
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| 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. |
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| Keywords: | Chalcones CDK1 inhibitive ability Anticancer activity |
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