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Natural active molecular coupling compound based on salaminol and pterostilbene and use thereof

A technology for coupling compounds and active molecules, applied in the fields of medicinal chemistry and pharmacotherapeutics, can solve problems such as lowering blood cholesterol and limiting drug applications

Active Publication Date: 2021-04-16
SHANGHAI TENTH PEOPLES HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at the same time, there are still the following deficiencies: first, the single-drug effective rate of these drugs in relapsed and refractory patients is only 25% to 50%; second, although the disease-free survival time is prolonged, most patients will eventually relapse, and Significant drug resistance appears; third, some serious side effects such as neuritis limit the application of drugs
In addition, it has the effect of lowering blood cholesterol

Method used

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  • Natural active molecular coupling compound based on salaminol and pterostilbene and use thereof
  • Natural active molecular coupling compound based on salaminol and pterostilbene and use thereof
  • Natural active molecular coupling compound based on salaminol and pterostilbene and use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0035]

[0036] Phosphorus oxychloride (0.50mL, 5.5mmol) was dissolved in dichloromethane (60mL), under nitrogen protection, cooling in an ice bath, compound 1 (1.28g, 5.0mmol) and triethylamine (0.85mL, 6.0mmol) were added dropwise dichloromethane (15mL) solution, stirred for 2 hours, and took a sample to monitor that the reaction was complete. The reaction solution was cooled in an ice bath again, then N-methylpiperazine 3a (0.55mL, 5.0mmol) and triethylamine (0.85mL, 6.0mmol) in dichloromethane (10mL) were added, stirred for 5 hours, and monitored by sampling The response is complete. The reaction solution was cooled in an ice bath again, and compound 2 (1.145g, 5.0mmol), N,N-dimethylaminopyridine (122mg, 1.0mmol) and triethylamine (0.85mL, 6.0mmol) in dichloromethane were added dropwise (10mL) solution, stirred and reacted for 10 hours, and took a sample to monitor that the reaction was complete. Diluted with water, extracted the reaction solution with dichloromethane...

preparation Embodiment 2

[0039]

[0040] Phosphorus oxychloride (0.50mL, 5.5mmol) was dissolved in dichloromethane (60mL), under nitrogen protection, cooling in an ice bath, compound 1 (1.28g, 5.0mmol) and triethylamine (0.85mL, 6.0mmol) were added dropwise dichloromethane (15mL) solution, stirred for 2 hours, and took a sample to monitor that the reaction was complete. The reaction solution was cooled in an ice bath again, and then 3-fluoro-4-morpholinoaniline 3b (0.98g, 5.0mmol) and triethylamine (0.85mL, 6.0mmol) in dichloromethane (10mL) were added, and the reaction was stirred for 5 Hours, sampling monitoring reaction is complete. The reaction solution was cooled in an ice bath again, and compound 2 (1.145g, 5.0mmol), N,N-dimethylaminopyridine (122mg, 1.0mmol) and triethylamine (0.85mL, 6.0mmol) in dichloromethane were added dropwise (10mL) solution, stirred and reacted for 10 hours, and took a sample to monitor that the reaction was complete. Diluted with water, extracted the reaction solut...

preparation Embodiment 3

[0043]

[0044] Phosphorus oxychloride (0.50mL, 5.5mmol) was dissolved in dichloromethane (60mL), under nitrogen protection, cooling in an ice bath, compound 1 (1.28g, 5.0mmol) and triethylamine (0.85mL, 6.0mmol) were added dropwise dichloromethane (15mL) solution, stirred for 2 hours, and took a sample to monitor that the reaction was complete. The reaction solution was cooled in an ice bath again, and then a solution of L-proline methyl ester hydrochloride 3 (825 mg, 5.0 mmol) and triethylamine (0.85 mL, 6.0 mmol) in dichloromethane (10 mL) was added, and the reaction was stirred for 5 hours , Sampling to monitor the reaction is complete. The reaction solution was cooled in an ice bath again, and compound 2 (1.145g, 5.0mmol), N,N-dimethylaminopyridine (122mg, 1.0mmol) and triethylamine (0.85mL, 6.0mmol) in dichloromethane were added dropwise (10mL) solution, stirred and reacted for 10 hours, and took a sample to monitor that the reaction was complete. Diluted with water...

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Abstract

The present invention relates to a natural active molecular coupling compound based on salaminol and pterostilbene shown in formula 1 and a pharmaceutically acceptable salt thereof, wherein the definition of each substituent is as described in the description; the present invention also provides The preparation method of the natural active molecule coupling compound represented by formula 1, and its use in the preparation of drugs for preventing or treating tumors or cancers.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a natural active molecular coupling compound based on salaminol and pterostilbene for treating tumors or cancers, as well as its pharmaceutical composition, preparation method and medical application. Background technique [0002] Malignant tumors, as one of the largest public health problems in the world, have greatly endangered human health and will become the number one killer of human beings in the new century. Malignant tumors are no longer just a serious disease in developed industrial countries, and developing countries are facing a greater burden of disease. Malignant tumors include solid tumors (such as lung cancer, colorectal cancer, liver cancer, gastric cancer, etc.) and blood tumors (such as myeloma, lymphoma, etc.). [0003] Multiple myeloma (multiple myeloma, MM) is a malignant disease of abnormal proliferation of clonal plasma cells. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6509C07F9/6533C07F9/572C07F9/24A61P35/00A61P35/02A61K31/675A61K31/685
Inventor 施菊妹朱维良贺湾李波胡亮凝徐志建张勇
Owner SHANGHAI TENTH PEOPLES HOSPITAL