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New trans-stilbene-type antitumor agent

A technology for anti-tumor activity and stilbene compounds, which is applied in the field of novel trans-stilbene compounds and anti-tumor agents, and can solve the problems of reduced yield, difficulty in obtaining active stilbene compounds, and difficulty in product separation.

Inactive Publication Date: 2017-11-07
NORTHEAST FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In such a synthetic reaction, the types of compounds are limited by the number and types of substituents, and it is difficult to obtain stilbene compounds with better activity; secondly, most coupling reactions will generate cis-trans isomers, resulting in difficulty in product separation. also lead to lower yield

Method used

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  • New trans-stilbene-type antitumor agent
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  • New trans-stilbene-type antitumor agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: 10# stilbene compounds are synthesized

[0016] (1) One-pot preparation of α-carbonyl dithioketene: 5 mmol of morpholine was added into a round bottom flask and dissolved in 7 mL of DMF, the temperature was lowered to -10°C using an ice-salt bath, and 5 mmol of diketene was slowly added dropwise. After 10 minutes of dropwise addition, continue to react for 20 minutes and monitor the reaction status using a TLC plate. After the substrate reaction is complete, directly add 10 mmol of weak base potassium carbonate, activate the reaction for 30 minutes, then add 6 mmol of carbon disulfide, the solution turns red, and continue the reaction for 1 hour. Slowly Add 10mmol methyl iodide dropwise, after 30min, slowly rise to room temperature and react for 2-2.5h, use TLC to detect the reaction progress, when the substrate reaction is complete, add distilled water to stop the reaction, and extract with ethyl acetate. The organic layer was collected, washed with water...

Embodiment 2

[0019] Embodiment 2: 13# stilbene compounds are synthesized

[0020] (1) One-pot preparation of α-carbonyl dithioketene: Add 5 mmol of cyclohexylamine to a round bottom flask and dissolve in 7 mL of DMF, use an ice bath to lower the temperature to -10°C, and slowly add 5 mmol of diketene dropwise, After 10 minutes of dropwise addition, continue to react for 20 minutes and monitor the reaction status using a TLC plate. After the substrate reaction is complete, directly add 10 mmol of weak base potassium carbonate, activate the reaction for 30 minutes, then add 6 mmol of carbon disulfide, the solution turns red, and continue the reaction for 1 hour. Slowly Add 10mmol methyl iodide dropwise, after 30min, slowly rise to room temperature and react for 2-2.5h, use TLC to detect the reaction progress, when the substrate reaction is complete, add distilled water to stop the reaction, and extract with ethyl acetate. The organic layer was collected, washed with water three times, and dr...

Embodiment 3

[0023] Embodiment 3: 23# stilbene compounds are synthesized

[0024] (1) One-pot preparation of α-carbonyl dithioketene: 5 mmol of diethylamine was added into a round bottom flask and dissolved in 7 mL of DMF, the temperature was lowered to -10°C using an ice bath, and 5 mmol of diketene was slowly added dropwise. After 10 minutes of dropwise addition, continue to react for 20 minutes and monitor the reaction status using a TLC plate. After the substrate reaction is complete, directly add 10 mmol of weak base potassium carbonate, activate the reaction for 30 minutes, then add 6 mmol of carbon disulfide, the solution turns red, and continue the reaction for 1 hour. Slowly Add 10mmol methyl iodide dropwise, after 30min, slowly rise to room temperature and react for 2-2.5h, use TLC to detect the reaction progress, when the substrate reaction is complete, add distilled water to stop the reaction, and extract with ethyl acetate. The organic layer was collected, washed with water th...

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Abstract

The present invention provides a novel trans-stilbene antineoplastic agent, the structure of which is represented by the general formula I, II or III, which has significant inhibitory effect on various cancer cell lines. Its pharmaceutically acceptable salts, derivatives, tautomers or solvates thereof, and combinations of the above compounds are used in the prevention or treatment of tumors and other tumor-related diseases.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and specifically relates to a class of novel trans-stilbene compounds with antitumor activity, pharmaceutical compositions containing the compounds and their use as antitumor agents. Background technique [0002] Cancer is a major disease that seriously threatens human life and social development. In recent years, the number of cancer patients has increased day by day. According to the data of three national surveys on causes of death in China, in the past 30 years, the proportion of cancer among the causes of death in China has increased from 1970s to 1970s. 10.13% rose to 22.32%, and the death rate rose from 73.99 / 100,000 to 135.88 / 100,000. The top ten cancers in my country are: lung cancer, liver cancer, esophageal cancer, female breast cancer, pancreatic cancer, lymphatic cancer, bladder cancer and thyroid cancer, and there is a growing trend. Therefore, it can be seen that the di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C323/62C07D295/192A61K31/235A61K31/166A61K31/40A61K31/5375A61P35/00
CPCC07C323/62C07D295/192
Inventor 付玉杰焦骄洪丽高畅赵春建韩盈枝盖庆岩
Owner NORTHEAST FORESTRY UNIVERSITY
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