新型鬼臼毒素类似物作为抗肿瘤药物的合成及生物学评价
Synthesis and biological evaluation of novel podophyllotoxin analogs as antitumor agents.
作者信息
Zhang Zhong-Heng, Zhang Li-Ming, Luo Gang, Zhang Shi, Chen Hong, Zhou Jing
机构信息
a Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics , School of Pharmacy, Tianjin Medical University , Tianjin 300070 , China.
出版信息
J Asian Nat Prod Res. 2014;16(5):527-34. doi: 10.1080/10286020.2014.913578.
A series of 4β N-indole-substituted podophyllotoxin derivatives were synthesized. Nine target compounds were evaluated against human cancer cell lines (HeLa, K562, and K562/A02) using MTT assay including three imine derivatives 8, 9, and 10 in vitro. The result showed that the three compounds had higher antitumor activity than their reduced forms. Among them, compounds 8, 9, 11, and 16 were superior to the positive control VP-16.
合成了一系列4β-N-吲哚取代的鬼臼毒素衍生物。采用MTT法对9种目标化合物进行了体外抗人癌细胞系（HeLa、K562和K562/A02）活性评价，其中包括3种亚胺衍生物8、9和10。结果表明，这3种化合物的抗肿瘤活性均高于其还原形式。其中，化合物8、9、11和16优于阳性对照药VP-16。
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