杂环取代的二苯乙烯类化合物抗癌活性研究

Studies of anticancer activties of heterocyclic substituted-1,2-bipheylenes

目的 :寻找新的抗癌化合物。方法 :设计并用不同路线合成了 10个 5 (或 6 )杂环取代的 1,2 二苯基 1 烯类目的化合物 ,分别测定了它们抑制人鼻咽癌 (KB)和人宫颈癌 (Hela)细胞增殖的活性 ,并研究了其结构与抗癌活性之间的关系。结果 :发现目的物对KB和Hela细胞增殖均有一定的抑制作用 ,且抑制Hela细胞的活性较抑制KB细胞强 ;定量构效关系 (QSAR)研究结果认为取代基的诱导效应指数 (I)对活性有一定的影响。结论 :具有钙调素拮抗剂类型的化合物具有抗癌活性。

Objectives: Search for new anticancer compounds. Methods: Ten compounds of 5-(or 6-) heterocyclic substituted-1,2-biphenyl-pet-1-enes were synthesized. The inhibitory activities on KB and Hela cancer cells and the relationship of structure-anticancer activity of these compounds were studied.Results:It is discovered that all these compounds showed inhibitory activities on KB and Hela cells in some extents.Furthermore,the inhibitory activity on Hela cells is more stronger than that on KB cells.The results of QSAR study showed that the inductive effect index of substituents have influences on their anticancer activities.Conclusions:Compounds with calmoduline antagonists'structure show anticancer activities and further studies should be conducted.