| abstract |
The invention provides a carbazole derivative, its preparation method and its application in anti-tumor. The carbazole derivative has the structure of formula I , and R1 and R2 are independently selected from hydrogen , halogen, alkoxy, C1～ One or more of C4 alkyl, haloalkyl, nitro and nitrile; R3 is selected from carboxyl, methyl, phenyl or cyano; X is CH2 or carbonyl; m=0～3; n= 0~3. The derivative significantly inhibits the activity of topoisomerase II; it is a non-intercalated Topo II catalytic inhibitor and can be used to prepare antitumor drugs targeting topoisomerase II; it can inhibit multiple tumor cell lines Proliferation can be used to prepare anticancer drugs. Carbazole derivatives have a strong inhibitory effect on topoisomerase II at 2.5-20 μmol/L; they have strong inhibitory effects on cervical cancer cells, human lung cancer cells, human leukemia cells and human prostate cancer cells. |