The present invention provides a novel aryl-substituted and methyl group attached bisindole acetic acid derivatives represented by Formula I, a method of preparing the same and an application thereof. The aryl-substituted and methyl group attached bisindole acetic acid derivatives of the present invention has a function of inhibiting tumor cells with low toxic side effects, and thus is able to be used as anticancer drugs for clinical application.本發明提供了通式I代表的新穎的芳基取代甲基連接的雙吲哚乙酸衍生物及其製備方法和應用。本發明的芳基取代甲基連接的雙吲哚乙酸衍生物具有抑制腫瘤細胞功效且毒副作用弱,可作為臨床用的抗腫瘤藥物。