摘要
目的寻找活性更好的类黄酮CDKs抑制剂。方法利用查尔酮路线制得8个类黄酮。结果与结论目标化合物结构经IR1、H-NMR、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,其中有4个化合物对CDK1的抑制活性高于对照Flavopiridol,1个化合物对HCT116的抑制活性高于Flavopiridol。
OBJECTIVE To search flavonoids with higher CDK inhibition.METHODS Chalcone route was applied to the synthesis of eight chalcones.RESULTS The structure of target compounds was confirmed by IR,1H-NMR and MS.CDK1 inhibition as well as cytotoxicity activity against HCT116 of above compounds were determined.CONCLUSION The result indicated that four compounds exhibited higher CDK1 inhibition than flavopiridol,one compound demonstrated higher cytotoxicity against HCT116 than flavopiridol.
出处
《海峡药学》
2011年第8期197-199,共3页
Strait Pharmaceutical Journal
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)