新型黄酮-Tr?ger’s碱类衍生物的合成及其生物活性（英文）

Synthesis and Biological Evaluation of Novel Flavonoid-Substituted Tr?ger's Bases

通过多步反应合成了一系列类黄酮取代的Tr?ger’s base衍生物,测试了其对Hep G2肝癌细胞的抗癌活性和四种细菌(铜绿假单胞菌PAM1032、野生型金黄色葡萄球菌,野生型大肠杆菌和大肠杆菌-大肠杆菌NMD-1)的抗菌活性.实验结果表明,该系列中有两种化合物在1μg/mL下对金黄色葡萄球菌有很高的抑制率,有五种产物对Hep G2肝癌细胞的IC50值低于阳性对照紫杉醇(30.87?g/m L),表现出较高的抑制活性,显示了其在新药研发领域潜在的应用价值.

A series of flavonoid-substituted Troger’s base analogues were synthesized via multi-step reaction. Their anti-cancer activities on the HepG2 hepatocellular carcinoma cell and antibacterial activities on four bacterial(Pseudomonas aeruginosa PAM1032, wild type Staphylococcus aureus, wild type Escherichia coli and Escherichia.coli-NMD-1) were evaluated. Two compounds were screened out because of their high inhibitory rate on Staphylococcus aureus at 1 μg/m L. The IC50 values of five products on the HepG2(hepatocellular carcinoma cell) were lower than that of positive control paclitaxel(30.87 μg/mL), displaying their high inhibitory activity. The results indicated their potential applications in new drug development.