Benzimidazole derivative, preparation method thereof and application of benzimidazole derivative to tumor resistance

A technology of benzimidazoles and derivatives, which is applied in its preparation method and its application in anti-tumor. In the field of benzimidazole derivatives, it can solve the problems of limited application and limited types of topoisomerase inhibitors.
CN107698577AActive Publication Date: 2018-02-16GUANGDONG UNIV OF TECH
2 Cites 1 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
GUANGDONG UNIV OF TECH
Publication Date
2018-02-16

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention provides a benzimidazole derivative which is provided with a structure as shown in a formula (I). R1 and R2 are independently selected from one of hydrogen, halogen, alkyl, alkoxy, halogenated alkyl, nitryl and a nitrile group, R3 is carboxyl, alkyl, phenyl or a cyano group, the value range of m is 0-3, the value range of n is 0-3, X is CH or nitrogen, and Y is CH2 or carbonyl. The benzimidazole derivative has a strong inhibiting effect on activity of topoisomerase II, so that the benzimidazole derivative can serve as a topoisomerase II inhibitor. Research finds that the compoundis the catalytic inhibitor of Topo II, so that the compound can be used for preparing an anti-tumor drug taking the topoisomerase II as a target spot. Besides, the benzimidazole derivative has good anti-proliferative activity for a plurality of tumor cells, so that the benzimidazole derivative can be used for preparing the anti-tumor drug.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to the fields of medicine and chemical industry, in particular to a benzimidazole derivative, its preparation method and its application in antitumor. Background technique

[0002] Cancer seriously threatens human health and life safety. According to statistics, about 4 million people around the world are diagnosed with cancer every year. In China, 8,500 new cancer patients are added every day, and one in eight people dies of cancer. Therefore, the research and development of anti-tumor drugs has always been a hot spot in current scientific research, and anti-tumor drugs with high efficiency and low toxicity are one of the important directions of research and development.

[0003] Topoisomerase plays an important role in the process of DNA replication, transcription and repair. In tumor cells, topoisomerases are overexpressed. If the activity of topoisomerase is inhibited, it will cause the disorder of cellular nucleic acid me...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More