4-S-(5"-烃基-4"-氨基-1",2",4"-三唑-3"-基)-4-去氧-4'-去甲基表鬼臼毒素衍生物的合成及抗肿瘤活性

SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4β S (5″ ALKYL 4″ AMINO 1″,2″,4″ TRIAZOLE 3″ YL) 4 DEOXY 4′ O DEMETHYL EPIPODOPHYLLOTOXIN DERIVATIVES

许多有显著抗肿瘤活性的鬼臼毒素类化合物，其母核Ｃ４侧链上往往连接有刚性较强的脂环或芳香环结构，而且侧链多含有一定数量的杂原子［１～３］。另外，三氮唑类化合物大都有广泛的生物活性，如抗菌［４～５］、抗病毒［６］、抗肿瘤［７］等，据此，我们设计并合成了...

AIM: In order to search for podophyllotoxin analogue agents with fewer side effects and improved activity, the podophyllotoxin derivatives are to be synthesized. METHODS: Eight 4′ demethyl podophyllotoxin analogues with 4β S triazoles have been synthesized from 4′ demethyl podophyllotoxin. RESULTS: Eight 4′ demethyl podophyllotoxin derivatives possessing 4β S triazoles have been synthesized and their antitumor activities were screened in vitro against HL 60, BGC 823, BcaP, KB and K 562 cells. CONCLUSION: The results indicated that these compounds showed high biological activity only towards K 562 cells.