The present invention discloses the use of substituted diphenylamine compounds in preparing anti-tumor drugs, represented by the general formula I. In the formula, each substituent is defined in the specification. The compounds of general formula I have good anti-tumor activity, especially suitable for treating or relieving cancers caused by tumor cells in tissues and organs in a human body. The cancers are preferably selected form colon cancer, liver cancer, lymphoma, lung cancer, esophagus cancer, breast cancer, central nervous system tumor, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostate cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, pharyngeal cancer, gastric cancer, etc.本發明公開了一種如通式I所示的取代二苯胺類化合物作為製備抗腫瘤藥物的應用,式中各取代基的定義見說明書。通式I化合物具有很好的抗腫瘤活性,尤其適用於治療或緩解人體組織或器官腫瘤細胞引起的癌症。所指癌症優選結腸癌、肝癌、淋巴瘤、肺癌、食管癌、乳腺癌、中樞神經系統腫瘤、黑色素瘤、卵巢癌、宮頸癌、腎癌、白血病、前列腺癌、胰腺癌、膀胱癌、直腸癌、骨肉瘤、鼻咽癌或胃癌等。