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

作　　者：何勇[1] 马维勇[1] 陈秀华[1] 张椿年[1] 

机构地区：[1]上海医药工业研究院,上海200040

出　　处：《药学学报》2001年第2期105-107,共3页Acta Pharmaceutica Sinica

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L12 10白血病细胞活性试验。结论　化合物 2 ,3 ,8,9,11和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.

关 键 词：鬼臼脂素 鬼臼脂素衍生物 抗肿瘤 

分 类 号：R979.1[医药卫生—药品] TQ463.4[医药卫生—药学]