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为考察4′-去甲基表鬼臼毒素4位上取代基结构变化与抗肿瘤活性的关系,设计并合成了23个标题化合物。体外L_(1210)白血病细胞与KB细胞生长抑制试验的结果表明,化合物11,16和18的抗肿瘤活性超过依托泊甙,化合物8的活性与依托泊甙相当。
In order to investigate the relationship between the structural changes of 4 substituent of 4’-demethylepipodophyllotoxin and anti-tumor activity, 23 title compounds were designed and synthesized. The results of the in vitro growth inhibition test of L 1210 leukemia cells and KB cells showed that the antitumor activity of compounds 11, 16 and 18 over etoposide, and the activity of compound 8 was comparable to that of etoposide.