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合成了13个新的鬼臼毒素衍生物5-17,经元素分析、IR、MS、ESR和1HNMR分析确证了其组成和结构,并对它们进行了抑制小鼠淋巴白血病P388和人胃腺癌SGC-7901细胞的体外筛选.发现新化合物5、7-10对两种瘤株均有显著抑制活性,4’-O-去甲基鬼臼毒素5、10-13的抗癌活性大于相应的4’-甲氧基类似物6、14-17,用“-O-”桥取代C-4位的“-NH-”桥可导致抗癌活性降低.
Thirteen new derivatives of podophyllotoxin 5-17 were synthesized and their composition and structure were confirmed by elemental analysis, IR, MS, ESR and 1H NMR. Their inhibitory effects on mouse lymphoid leukemia P388 and human gastric adenocarcinoma SGC -7901 cells in vitro screening. New compounds 5 and 7-10 were found to have significant inhibitory activity against both tumorous strains. The antitumor activity of 4’-O-desmethylpodophyllotoxin 5 and 10-13 was greater than that of the corresponding 4’-methoxy analog 6,14-17, substitution of the “-O-” bridge for the “-NH-” bridge at the C-4 position results in a decrease in anticancer activity.