BIS-B-CARBOLINE COMPOUND AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF

摘要

Disclosed in the present invention are a bis-β-carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis-β-carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis-β-carboline compound is prepared through the condensation of β-carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis-β-carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis-β-carboline compound in preparing drugs resistant to tumours 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.;

主权项

1. An bis-β-carboline compound and a pharmaceutical salt thereof are described as general formula Iwherein,
R1 is substituent selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 linear or branched alkyl, hydroxyl, substituted or unsubstituted C1-6 linear or branched alkoxy, sulfonate group, substituted or unsubstituted C1-6 linear or branched alkylthio, C1-6 alkoxy C1-6 alkyl group, amino group, substituted or unsubstituted C1-6 linear or branched alkylamino group wherein the alkylamino group include mono- and bis-alkylamino, halogen, nitro, cyano, substituted or unsubstituted five-six membered aryl, substituted or unsubstituted five-six membered aryl containing 1-4 heteroatoms selected from N, O, or S; Substituents on the substituted or unsubstituted five-six membered aryl are selected from the group consisting of hydroxy, mercapto, amino, aldehyde, carboxyl, carbamoyl, halogen, nitro, cyano, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylamino, C1-6 alkylamino group and C1-6 alkoxy C1-6 alkyl group; Substituents on the substituted or unsubstituted five-six membered aryl containing 1-4 heteroatoms selected from N, O, or S; are selected from the group consisting of hydroxy, mercapto, amino, aldehyde, carboxyl, carbamoyl, halogen, nitro, cyano, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylamino, C1-6 alkylamino group and C1-6 alkoxy C1-6 alkyl group; R3 is substituent selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 linear or branched alkyl carconby, carboxyl; substituted or unsubstituted C1-6 linear or branched alkoxy carconby, substituted or unsubstituted C1-6 linear or branched alkyl carbonyloxy, amino-carbonyl, substituted or unsubstituted C1-6 linear or branched alkylamino carbonyloxy, substituted or unsubstituted C1-6 linear or branched alkyl acyl amido; R6 is substituent selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 linear or branched alkyl, hydroxyl, substituted or unsubstituted C1-6 linear or branched alkoxy, sulfonate group, substituted or unsubstituted C1-6 linear or branched alkylthio, C1-6 alkoxy C1-6 alkyl group, amino group, substituted or unsubstituted C1-6 linear or branched alkylamino group wherein the alkylamino group include mono- and bis-alkylamino, aldehyde, substituted or unsubstituted C1-6 linear or branched alkyl acyl, substituted or unsubstituted C1-6 linear or branched alkyloxy acyl, carboxyl, substituted or unsubstituted C1-6 linear or branched alkyl acyloxy, carbamoyl, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, C2-6 olefins, halogen, nitro, cyano; R7 is substituent selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 linear or branched alkyl, hydroxyl, substituted or unsubstituted C1-6 linear or branched alkoxy, sulfonate group, substituted or unsubstituted C1-6 linear or branched alkylthio, C1-6 alkoxy C1-6 alkyl group, amino group, substituted or unsubstituted C1-6 linear or branched alkylamino group wherein the alkylamino group include mono- and bis-alkylamino, aldehyde, substituted or unsubstituted C1-6 linear or branched alkyl acyl, substituted or unsubstituted C1-6 linear or branched alkyloxy acyl, carboxyl, substituted or unsubstituted C1-6 linear or branched alkyl acyloxy, carbamoyl, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, C2-6 olefins, halogen, nitro, cyano; R8 is substituent selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 linear or branched alkyl, hydroxyl, substituted or unsubstituted C1-6 linear or branched alkoxy, sulfonate group, substituted or unsubstituted C1-6 linear or branched alkylthio, C1-6 alkoxy C1-6 alkyl group, amino group, substituted or unsubstituted C1-6 linear or branched alkylamino group wherein the alkylamino group include mono- and bis-alkylamino, aldehyde, substituted or unsubstituted C1-6 linear or branched alkyl acyl, substituted or unsubstituted C1-6 linear or branched alkyloxy acyl, carboxyl, substituted or unsubstituted C1-6 linear or branched alkyl acyloxy, carbamoyl, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, substituted or unsubstituted C1-6 linear or branched alkyl acylamino group, C2-6 olefins, halogen, nitro, cyano; Substituents on the substituted or unsubstituted C1-6 linear or branched alkyl are selected from the group consisting of hydroxy, mercapto, amino, aldehyde, carboxyl, carbamoyl, halogen, nitro, and cyano; n is selected from the group consisting of the natural numbers from 2 to 12.