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通过在DCC(二环已基碳酰二亚胺)存在下用4β-氨基-4-去氧-4′-去甲表鬼臼毒与卤代苯甲酸缩合,合成了12个新的4β-卤代芳香酰胺基-4-去氧-4′-去甲表鬼臼毒衍生物(2~13).测定了这些化合物对KB,HCT-8,A-2780和HeLa-60细胞的杀伤效应(体外细胞试验).结果显示,这些化合物中大多数比目前临床使用的抗癌药物依托泊甙,即VP-16在HCT-8,A-2780和HeLa-60细胞的杀伤中有较强的效果.对这些化合物进行了大鼠肝微粒体脂质过氧化试验.结果显示这些化合物具有明显的抗脂质过氧化能力.用QSAR(定量的结构-活性相关关系)方法分析了该类化合物的结构和对KB,HCT-8和HeLa-60细胞抑制作用间的相互关系
By condensing 4β-amino-4-deoxy-4’-norvulopodin with halobenzoic acid in the presence of DCC (dicyclohexylcarbodiimide), 12 new 4β- Haloaromatic amide-4-deoxy-4’-norvulopodophyllotoxin derivatives (2-13). The killing effect of these compounds on KB, HCT-8, A-2780 and HeLa-60 cells was determined (in vitro cell assay). The results show that the majority of these compounds have a stronger effect than the current clinical use of the anticancer drug etoposide, VP-16 in the killing of HCT-8, A-2780 and HeLa-60 cells. The rat liver microsomal lipid peroxidation test was performed on these compounds. The results show that these compounds have significant anti-lipid peroxidation ability. The QSAR (quantitative structure-activity relationship) method was used to analyze the relationship between the structure of these compounds and the inhibitory effect on KB, HCT-8 and HeLa-60 cells