Abstract: Disclosed in the present invention are a bis-?-carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis-?-carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis-?-carboline compound is prepared through the condensation of ?-carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis-?-carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis-?-carboline compound in preparing drugs resistant to tumors such as melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer.

Abstract: This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumor activity and lower nervous system toxicity by structurally modification of the parent structure of ?-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumor medicines and medicines used in treatment of tumor diseases in combination of light or radiation therapy.