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为考察4′-去甲表鬼臼毒素C_4位上联结含卤素原子的酯化侧链时对化合物抗肿瘤活性的影响,设计并采用选择性酯化方法合成了9个新的4′-去甲基表鬼臼毒素酯化产物。其中标题化合物在L_(1210)白血病肿瘤细胞与KB细胞的体外生长抑制试验中普遍表现出显著的抑制活性,大部分化合物活性超过依托泊甙。而普通脂酸酯的活性较弱。
In order to investigate the antitumor activity of 4’-demethylepipodophyllotoxin (C_4) on the antitumor activity of the compound with the halogen atom-containing esterification side chain, nine new 4’- Methyl epipodophyllotoxin esterification product. Among them, the title compound generally showed significant inhibitory activity in the in vitro growth inhibition test of L 1210 leukemia tumor cells and KB cells, and most of the compounds were more active than etoposide. Ordinary fatty acid ester activity is weak.