Synthesis and antitumor activity of 6- and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones.
Synthesis and antitumor activity of 6- and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones.
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DOI：
10.1016/j.ejmech.2008.09.039
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发表时间：
2009-04
影响因子：
6.7
通讯作者：
Li-Ming Zhao;Tianxin Xie;Yu-Qin He;Defeng Xu;Shaoshun Li
中科院分区：
文献类型：
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作者：
Li-Ming Zhao;Tianxin Xie;Yu-Qin He;Defeng Xu;Shaoshun Li
为了开发有效的选择性抗肿瘤药物，设计并合成了一系列6-和2-(1-取代-硫代-4-甲基戊-3-烯基)-5,8-二甲氧基萘-1,4-二酮。在体外针对 BEL-7402、HT-29 和 SPC-A1 细胞系评估了这些化合物的细胞毒性。药理结果表明，所制备的大多数化合物对HT-29细胞表现出优异的选择性细胞毒性。从构效关系我们可以得出结论，在紫草素侧链1′位引入硫醚官能团与细胞毒性的增加有关。
In an attempt to develop potent and selective antitumor agents, a series of 6- and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones were designed and synthesized. The cytotoxicities of these compounds were evaluated in vitro against BEL-7402, HT-29 and SPC-A1 cell lines. The pharmacological results showed that most of the prepared compounds displayed the excellent selective cytotoxicity toward HT-29 cells. From the structure–activity relationships we may conclude that the introduction of a thioether functional group at the 1′-position in the side chain of shikonin is associated with an increase in cytotoxicity.