鬼臼毒素自旋标记衍生物的合成及其抗肿瘤活性
Synthesis and antitumor activity of spin labeled derivatives of podophyllotoxin.
作者信息
Tian X, Wang Y G, Yang M G, Chen Y Z
机构信息
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, P.R. China.
出版信息
Life Sci. 1997;60(8):511-7. doi: 10.1016/s0024-3205(96)00689-3.
Three new nitroxyl labeled derivatives of podophyllotoxin 4-6 have been synthesized and evaluated for their antitumor activity in vitro. Compounds 4-6 showed significant inhibitory activity against human nasopharyngeal carcinoma KB,lung cancer A549 and stomach carcinoma SGC-7901 cells, as well as mouse leukemia L1210 and P388 cells. Compounds 4 and 5 exhibited comparable or superior activity to clinically used etoposide (VP-16,2) in their inhibition of these cell lines.
已合成了三种新的鬼臼毒素4-6的硝酰基标记衍生物，并对其体外抗肿瘤活性进行了评估。化合物4-6对人鼻咽癌KB细胞、肺癌A549细胞和胃癌SGC-7901细胞以及小鼠白血病L1210和P388细胞均表现出显著的抑制活性。在对这些细胞系的抑制作用方面，化合物4和5表现出与临床使用的依托泊苷（VP-16,2）相当或更优的活性。
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