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

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。

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, 1 H - NMR and ESI - MS. The CDK1 inhibitive ability and the anticaneer 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.