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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。
Purpose: To find new anticancer compounds. METHODS: Ten 5 (or 6) heterocyclic substituted 1,2-diphenyl-1-ene compounds were designed and synthesized by different routes. Their inhibitory effects on human nasopharyngeal carcinoma (KB) and human cervical carcinoma ) Cell proliferation activity and to study the relationship between its structure and anti-cancer activity. Results: The target substance was found to inhibit the proliferation of KB and Hela cells, and the inhibition of Hela cell activity was stronger than that of KB cells. The quantitative structure-activity relationship (QSAR) results showed that the induction effect index (I) Activity has a certain impact. Conclusion: Compounds with calmodulin antagonist have anticancer activity.