类黄酮CDKs抑制剂的合成及其抗肿瘤活性的研究(Ⅰ)

The synthesis and anticancer activity study of flavonoids as CDKs inhibitors(Ⅰ)

目的寻找活性更好的类黄酮细胞周期蛋白依赖性激酶(CDKs)抑制剂。方法利用查尔酮路线合成了9个类黄酮。结果目标化合物的结构经IR、1HNMR、质谱确证,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。结论有5个化合物对CDKs的抑制活性高于对照Flavopiridol,所有化合物对HCT116均显示较强的抑制活性。

OBJECTIVE To search flavonoids with higher cyclin-dependent kinase（CDKs） inhibition.METHODS Chalcone route was applied to the synthesis of 9 chalcones.RESULTS The structure of target compounds was confirmed by IR,1HNMR and MS.CDKs inhibition as well as cytotoxicity activity against HCT116 of above compounds were determined.CONCLUSION The result indicated that five compounds exhibited higher CDKs inhibition than flavopiridol,all compounds demonstrated higher cytotoxicity activity against HCT116.