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为寻找高效低毒且作用谱广的鬼臼毒素类抗肿瘤药物,以4’-去甲基表鬼臼毒素为起始原料,用不同结构的芳香羧酸对其进行修饰,设计合成了17个4’-去甲基表鬼臼毒素酯类新化合物,通过1H NMR和ESI-MS确证其结构,并采用MTT法评价了目标化合物对人肝癌(HepG2)、人肺癌(A549)、人口腔癌(KB)及小鼠白血病细胞(L1210)的抑制活性。结果表明,大多数化合物对肿瘤细胞均表现出较好的抑制作用。
In order to find a potent and potent podophyllotoxin antitumor drug with high activity and low toxicity, 4’-demethylated epipodophyllotoxin was used as a starting material to modify podophyllotoxins with aromatic carboxylic acids with different structures. 17 A novel 4’-demethylated epipodophyllotoxin was identified by 1H NMR and ESI-MS, and its structure was evaluated by MTT assay. The target compounds were evaluated on HepG2, human lung cancer (A549), human oral cavity Cancer (KB) and mouse leukemia cells (L1210). The results showed that most of the compounds showed good inhibitory effect on tumor cells.