Synthesis and cytotoxic evaluation of novel symmetrical taspine derivatives as anticancer agents.
Synthesis and cytotoxic evaluation of novel symmetrical taspine derivatives as anticancer agents.
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DOI：
10.2174/157340611796150914
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发表时间：
2011-06
期刊：
影响因子：
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通讯作者：
Jie Zhang;Yanmin Zhang;Xiaoyan Pan;Sicen Wang;Langchong He
中科院分区：
文献类型：
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作者：
Jie Zhang;Yanmin Zhang;Xiaoyan Pan;Sicen Wang;Langchong He
已证明塔斯品衍生物具有抗癌作用，因此我们设计并合成了一类新型对称联苯衍生物。我们评估了联苯对五种人类肿瘤和正常细胞系的细胞毒性和抗肿瘤活性。结果表明，大多数化合物表现出相当于或大于阳性对照的抗癌活性。化合物(11)和(12)表现出最有效的细胞毒活性，IC50值在19.41 µM和29.27 µM之间。这些化合物对 ECV304 人转化内皮细胞的有效抗增殖能力表明这些联苯有可能作为抗血管生成剂。我们还根据实验结果回顾了结构和活性之间的关系。我们的研究结果为进一步开发对称联苯衍生物作为潜在的新型抗癌剂提供了良好的起点。
It has been demonstrated that taspine derivatives act as anticancer agents, thus we designed and synthesized a novel class of symmetrical biphenyl derivatives. We evaluated the cytotoxicity and antitumor activity of biphenyls against five human tumor and normal cell lines. The results indicated that the majority of the compounds exhibited anticancer activity equivalent to or greater than the positive control. Compounds (11) and (12) demonstrated the most potent cytotoxic activity with IC₅₀ values between 19.41 µM and 29.27 µM. The potent antiproliferative capabilities of these compounds against ECV304 human transformed endothelial cells indicated that these biphenyls could potentially serve as antiangiogenic agents. We also reviewed the relationship between structure and activity based on the experimental results. Our findings provide a good starting point for further development of symmetrical biphenyl derivatives as potential novel anticancer agents.