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目的 为寻找高效低毒且作用谱广的鬼臼脂素类抗肿瘤药物,合成了20个4’-去甲基表鬼臼毒素芳香酰胺类化合物.方法 以4’-去甲基表鬼臼毒素为原料,首先与氯乙腈进行取代反应,再与硫脲反应,最后与不同的取代芳香羧酸成酰胺制得目标化合物.采用MTT法测定目标化合物体外对人肺腺癌细胞A549、人肝肿瘤细胞株HepG2、人口腔癌KB细胞、L1210白血病细胞的抑制活性.结果与结论 合成了20个未见文献报道的新化合物,目标化合物的结构均经1 H-NMR和MS谱确证,活性测试结果表明,大部分目标化合物均具有一定的肿瘤细胞增殖抑制活性.“,”In order to find the novel epipodophyllotoxins antitumor drugs and reduce toxicity and side effect,twenty novel 4’-demethylepipodophyllotoxin aromatic amide derivatives were designed and synthesized.Amino groups were introduced by Ritter reaction,and different side chains were introduced by condensation reaction.All of them have been characterized by 1H-NMR and ESI-MS,and the effects of synthesized compounds against proliferations of A549,HepG2,KB,L1210 cells were evaluated by MTT test.The introduction of halogen in thiophene ring can increase the inhibition of A549,KB,L1210 cells;the introduction of halogen in indole ring can decrease the inhibition activity,however,the introduction of electron-donating group,such as methoxyl group can increase the inhibitory activity;carbon chain elongation can decease the inhibitory activity.