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Osalmid and pterostilbene based cyclic coupling molecule DCZ0801 compound and preparation method and application thereof

A technology for coupling compounds, salivamol, which is applied in the field of ring-forming molecular coupling compounds and their pharmaceutical compositions, can solve problems such as limiting drug applications and lowering blood cholesterol

Inactive Publication Date: 2020-08-25
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Osalmid and pterostilbene based cyclic coupling molecule DCZ0801 compound and preparation method and application thereof
  • Osalmid and pterostilbene based cyclic coupling molecule DCZ0801 compound and preparation method and application thereof
  • Osalmid and pterostilbene based cyclic coupling molecule DCZ0801 compound and preparation method and application thereof

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Experimental program
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Effect test

preparation Embodiment 1

[0045]

[0046] 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 compound 2-1 (1.145 g, 5.0 mmol) and triethylamine (1.70 mL, 12.0 mmol) in acetone (10 mL) were added, stirred and reacted for 10 hours, and samples were taken to monitor the completion of the reaction. Dilute with water, extract the reaction liquid with dichloromethane, separate the organic phase, wash with water, wash with saturated sodium chloride, dry over anhydrous sodium sulfate, evaporate to dryness under reduced pressure, and the residue is separated by silica gel column (PE / EA(v:v) = 1:1;CH 2 Cl 2 / MeOH (v:v)=20:1), the white solid product DCZ0801 was obtaine...

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Abstract

The invention discloses an osalmid and pterostilbene based cyclic coupling molecule compound as shown in a formula I or pharmaceutically acceptable salts thereof. R is selected from hydrogen, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C5-C12 aryl, substituted or unsubstituted C1-C6 alkoxy, C1-C6 alkylthio, C5-C12 aryloxy and C5-C12 arylthio; and substituent for substitution is one or more of hydroxyl, amino, sulfydryl, halogen, C5-C12 aryl and C1-C6 alkyl. The invention also provides a preparation method and application of the compound.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a ring-forming 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. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K31/609A61P35/00A61K31/09
CPCA61K31/09A61K31/609A61K47/55A61P35/00A61K2300/00
Inventor 李波施菊妹贺湾徐志建余丹丹张勇蔡婷婷张鑫贲朱维良
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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