中文摘要：

目的获得更高活性且具有抗多药耐药活性的抗肿瘤新化合物。方法将4β-氨基-4-脱氧鬼臼毒素与醇类化合物以丁二酸为桥连接合成了7个鬼臼毒素衍生物,其结构经1H-NMR、TOF-MS证实。采用K562和K562/AO2细胞经MTT法对目标化合物进行体外抗肿瘤活性筛选。结果7个化合物均为新化合物,其中5b、5d的抗肿瘤活性显著高于VP-16,并且5b、5c、5d、5e的抗多药耐药活性显著高于VP-16。结论合成的鬼臼毒素衍生物的抗肿瘤活性与阳性对照药VP-16相比均有所提高。

英文摘要：

Aim To find compounds with superior antitumor bioactivity and overcoming multidrug resistance. Methods Seven derivatives of podophyllotoxin were synthesized by linking 4β-amino-4-deoxypodophyllotoxin with alcohols through succinic acid. Their structures were confirmed by ^1H-NMR, TOF-MS. Their antitumot activity was tested by MTT method against K562 and K562/AO2 in vitro. Results Seven derivatives were not reported by previous literature. The derivatives 5b,Sd exhibit superior anticancer activity compared to VP-16 against K562 in vitro. The derivatives 5b,5c,Sd and 5e may overcome MDR compared to VP-16 against K562/AO2 in vitro. Conclusion The results indicate that these compounds show high antitumor activity.