4-去氧-4β-芳甲磺酰胺基-4′-去甲鬼臼脂素的合成及体外抑制肿瘤细胞活性

SYNTHESIS AND ACTIVITIES OF 4-DEOXY-4β-ARYLMEHTYLENE SULFONYLAMIDO-4′-DEMETHYLPODOPHYLLOTOXINS

摘要: 目的　寻找高效低毒的鬼臼脂素类抗肿瘤药物。方法和结果　设计合成了4-增碳侧链的磺酰胺基鬼臼脂素衍生物(1-15),均为新化合物。并对这些化合物进行了体外抑制KB细胞和L1210白血病细胞活性试验。结论　化合物2，3，8，9，11和12有显著的体外抑制肿瘤细胞活性。

Abstract: AIM　To find new anticancer drug based on the structure of podophyllotoxin. METHODS AND RESULTS　4-Deoxy-4β-arylmethylenesulfonylamido-4′-demethylpodophyllotoxins were (1-15) synthesized and their antitumour activities against KB cells and L1210 leukemia cells were tested. CONCLUSION　These compounds are new compounds. Among them, compounds 2, 3, 8, 9, 11 and 12 showed antitumour activities. When halides exist on the aryl ring of substituted sulfonyl group, the corresponding compound has relatively higher activities. The stereo factor is important for the activities.