Benzimidazole derivatives, and preparation method and pharmaceutical applications thereof

A technology of benzimidazole derivatives, applied in the field of benzimidazole derivatives and pharmaceutical compositions containing such compounds, which can solve the problems of poor selectivity and easy drug resistance

Inactive Publication Date: 2015-07-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Most of these inhibitors act on the ATP-binding pocket of PLK1 and are ATP-competitive inhibitors, which have side effects such as poor selectivity to different kinases and easy drug resistance common to kinase inhibitors

Method used

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  • Benzimidazole derivatives, and preparation method and pharmaceutical applications thereof
  • Benzimidazole derivatives, and preparation method and pharmaceutical applications thereof
  • Benzimidazole derivatives, and preparation method and pharmaceutical applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Synthesis of 1-(3-chloropropyl)-1H-benzo[d]imidazole (c-1):

[0031] In a 100ml single-necked flask, add 3.0g benzimidazole, 6g of 1-bromo-3-chloropropane, 4.2g of anhydrous potassium carbonate and 30ml of acetone, stir and heat to reflux for about 12 hours, filter the reaction solution, and spin the filtrate Dries to a brownish-red liquid. Cast directly to the next step without separation.

Embodiment 2

[0033] Synthesis of 1-(3-chloro-2,2-dimethylpropyl)-1H-benzo[d]imidazole (c-2):

[0034] The target compound was prepared by a method similar to Example 1, and it was a brownish-red liquid. Cast directly to the next step without separation.

Embodiment 3

[0036] Synthesis of 1-(3-chloro-2-methyl-2-hydroxypropyl)-1H-benzo[d]imidazole (c-3):

[0037] The target compound was prepared by a method similar to Example 1, and it was a brownish-red liquid. Cast directly to the next step without separation.

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PUM

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Abstract

The invention belongs to the field of pharmaceutical chemistry, and specifically relates to novel N<1>-substituted benzimidazole compounds (I), wherein R1, R2, and R3 are defined by the patent specification. It is shown by results of in vitro tumor cell growth inhibitory activity tests that the novel N<1>-substituted benzimidazole compounds possess relatively high tumor cell growth inhibitory activity, and some of the novel N<1>-substituted benzimidazole compounds possess extremely high tumor cell growth inhibitory activity. The invention also discloses a preparation method of the novel N<1>-substituted benzimidazole compounds.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a class of benzimidazole derivatives, a preparation method thereof and its medical application as a tumor therapeutic agent, and a pharmaceutical composition containing the compound. Background technique [0002] At present, malignant tumors are still one of the major diseases that threaten people's lives. Although the currently marketed anticancer drugs have certain curative effects, most of them are cytotoxic drugs with serious toxic and side effects. Therefore, how to start from effective anti-tumor drug targets to study targeted new anti-cancer drugs has become a top priority. [0003] As an important target in the research of targeted anti-tumor drugs, protein kinase has always been the focus of drug researchers. At present, kinase inhibitors of various structural types have been developed, many small molecule inhibitors have entered the clinical research sta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/06A61P35/00
CPCC07D235/06
Inventor 江程陈东星徐云根刘孟李志裕
Owner CHINA PHARM UNIV
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