4β-卤代芳香酸4′-去甲表鬼臼酯类的合成及抗肿瘤活性

Synthesis and anticancer activity of the derivatives of 4β-halogenated arylacylester-4′-demethylepipodophyllotoxin

通过 4′-去甲表鬼臼毒素 (DMEP)与卤代苯甲酸缩合 ,合成了 12个新的 4 β-卤代芳香酸 4′-去甲表鬼臼酯类化合物 (1～ 12 ) .测定了这些化合物对 KB,HCT- 8和 A- 2 780细胞的杀伤效应 (体外细胞试验 ) .结果显示化合物 3,4 ,5显示了比目前临床应用的抗癌药物 VP- 16更强的对 KB,HCT- 8和 A- 2

Twleve new derivatives of 4β-Halogenated arylacylester-4′-demethyl epipodophyllotoxin have been synthesized.The inhibitory activities to KB,HCT-8 and A-2780 cells were screened in vitro.The results indicated that compouds 3,4,5 showed stronger activities in the inhibition against KB,HCT-8 and A-2780 cells than Etoposide.