新型含丁烯内酯的二硫代氨基甲酸盐的合成及体外抗肿瘤活性研究。
Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates.
机构信息
New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):3074-7. doi: 10.1016/j.bmcl.2011.03.029. Epub 2011 Mar 17.
PMID:21486694
Abstract
Three series of butenolide-containing dithiocarbamates were designed and synthesized. Their anti-tumor activity in vitro was evaluated. Among them compound I-14 exhibited broad spectrum anti-cancer activity against five human cancer cell lines with IC(50) <30 μM. Structure-activity relationship analysis showed that the introduction of dithiocarbamate side chains on the C-3 position of butenolide was crucial for anti-tumor activity.
摘要
设计并合成了三系列含丁烯内酯的二硫代氨基甲酸盐。评估了它们的体外抗肿瘤活性。其中化合物 I-14 对五种人癌细胞系表现出广谱抗癌活性，IC50<30 μM。构效关系分析表明，在丁烯内酯的 C-3 位引入二硫代氨基甲酸盐侧链对于抗肿瘤活性至关重要。
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