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甘草次酸硫代缩氨基脲衍生物的合成及抗肿瘤活性。

Synthesis and antitumor activity of liquiritigenin thiosemicarbazone derivatives.

机构信息

Faculty of Chemistry & Chemical Engineering, Jiangsu Polytechnic University, 1 Gehu Road, Changzhou, Jiangsu 213164, China.

出版信息

Eur J Med Chem. 2010 Aug;45(8):3453-8. doi: 10.1016/j.ejmech.2010.04.036. Epub 2010 May 6.

Abstract

In an attempt to develop potent and selective antitumor agents, a series of liquiritigenin thiosemicarbazone derivatives were designed and synthesized. The cytotoxicities of these compounds were evaluated in vitro against K562, DU-145, SGC-7901, HCT-116 and Hela cell lines. The pharmacological results showed that most of the prepared compounds displayed excellent selective cytotoxicity toward K562 and DU-145 cells. From the structure-activity relationships we may conclude that the introduction of a thiosemicarbazone functional group at the 4-position in the skeleton of liquiritigenin is associated with an increase in cytotoxicity.

摘要

为了开发高效、选择性的抗肿瘤药物,设计并合成了一系列甘草次酸硫代缩氨脲衍生物。这些化合物的体外细胞毒性在 K562、DU-145、SGC-7901、HCT-116 和 Hela 细胞系中进行了评估。药理结果表明,大多数所制备的化合物对 K562 和 DU-145 细胞表现出优异的选择性细胞毒性。从构效关系可以得出结论,在甘草次酸骨架的 4-位引入硫代缩氨脲官能团与细胞毒性的增加有关。

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