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Nitroxyl radical anti-tumor medicaments

A drug and selected technology, applied in the field of medicine, can solve problems such as large toxic and side effects

Active Publication Date: 2011-05-25
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drugs currently used for tumor treatment lack specificity to tumor cells, and often have problems such as high toxicity and side effects

Method used

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  • Nitroxyl radical anti-tumor medicaments
  • Nitroxyl radical anti-tumor medicaments
  • Nitroxyl radical anti-tumor medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the synthetic method of compound 1

[0020]

[0021] Add 3.0 g (30 mmol) prolinol, CH 2 Cl 2 100 mL, 4.4 mL of triethylamine were magnetically stirred in an ice bath, and then added dropwise to 50 mL of CH containing 5.57 g (30 mmol) p-nitrobenzoyl chloride 2 Cl 2 solution. After the dropwise addition, the ice bath was removed, stirred at room temperature for 24 h, the organic phase was separated, washed twice with water, dried, and purified by column chromatography to obtain 6.4 g of the product.

[0022] The above product 1.0 g (4.0 mmol), 0.93 g (4.0 mmol) TCCA and 20 mL CH 2 Cl 2 , stirred at 0 °C for 5 min, then added 0.006 g (0.04 mmol) TEMPO. Stirring was continued at room temperature for 20 min. Filter, combine the organic phases, and wash with saturated Na 2 CO 3 Wash with 0.1 mol·L -1 The organic phase was washed with HCl and saturated brine. The organic phase was dried and purified by column chromatography to obtain 0.69 g of t...

Embodiment 2

[0024] Embodiment 2: the synthetic method of compound 2

[0025]

[0026] Add 3.0 g (30 mmol) prolinol, CH 2 Cl 2 100 mL, 4.4 mL of triethylamine were magnetically stirred in an ice bath, and then added dropwise to 50 mL of CH containing 4.74 g (30 mmol) p-fluorobenzoyl chloride 2 Cl 2 solution. After the dropwise addition, the ice bath was removed, stirred at room temperature for 24 h, the organic phase was separated, washed twice with water, dried, and purified by column chromatography to obtain 5.5 g of the product.

[0027] 0.89 g (4.0 mmol) of the above product, 0.93 g (4.0 mmol) TCCA and 20 mL CH 2 Cl 2 , stirred at 0 °C for 5 min, then added 0.006 g (0.04 mmol) TEMPO. Stirring was continued at room temperature for 20 min. Filter, combine the organic phases, and wash with saturated Na 2 CO 3 Wash with 0.1 mol·L -1 The organic phase was washed with HCl and saturated brine. The organic phase was dried and purified by column chromatography to obtain 0.69 g...

Embodiment 3

[0029] Embodiment 3: the synthetic method of compound 3

[0030]

[0031] Add 3.0 g (30 mmol) prolinol, CH 2 Cl 2 100 mL, 4.4 mL of triethylamine were magnetically stirred in an ice bath, and then added dropwise to 50 mL of CH containing 4.68 g (30 mmol) p-chlorobenzoyl chloride 2 Cl 2 solution. After the dropwise addition, the ice bath was removed, stirred at room temperature for 24 h, the organic phase was separated, washed twice with water, dried, and purified by column chromatography to obtain 5.8 g of the product.

[0032] 0.88 g (4.0 mmol) of the above product, 0.93 g (4.0 mmol) TCCA and 20 mL CH 2 Cl 2 , stirred at 0 °C for 5 min, then added 0.006 g (0.04 mmol) TEMPO. Stirring was continued at room temperature for 20 min. Filter, combine the organic phases, and wash with saturated Na 2 CO 3 Wash with 0.1 mol·L -1 The organic phase was washed with HCl and saturated brine. The organic phase was dried and purified by column chromatography to obtain 0.78 g...

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Abstract

The invention discloses a novel anti-tumor medicament structure represented by a structural general formula (I), wherein R1 to R5 are independently selected from H, OH, OCH3, NO2 and halogen. A synthesis method for the medicaments is simple and convenient, the molecules of the medicaments contain nitroxyl radical structural units, and proliferation of liver cancer, gastric cancer, breast cancer and other tumor cells can be effectively suppressed.

Description

technical field [0001] The invention provides a novel nitrogen oxide free radical antitumor drug structure, which belongs to the technical field of medicine. Background technique [0002] Due to the impact of environmental pollution and bad living habits such as drinking and smoking, malignant tumors have become common and frequently-occurring diseases that seriously threaten human health. At present, about 7 million people die of malignant tumors every year in the world. According to the results of the third national resident cause of death survey, the death rate caused by tumors in my country ranks second among all causes, and the incidence rate is still on the rise. The treatment of malignant tumors is an urgent problem to be solved in our country. [0003] Drug therapy is an important means of tumor treatment. Governments, research institutions and pharmaceutical companies have long attached great importance to and invested heavily in the research and development of an...

Claims

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Application Information

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IPC IPC(8): C07D403/04A61K31/4178A61P35/00
Inventor 文爱东孙晓莉向卓高鹏田敏
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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