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Novel arylurea-containing 4-arylpyran derivative and application thereof

A technology of arylpyrans and aryl urea, which is applied in the field of medicine, can solve the problems of poor compound activity, poor druggability, structural modification, etc., and achieve the effect of preventing colon cancer and lung cancer and having significant anti-tumor activity

Active Publication Date: 2019-12-20
SHAANXI SCI TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These isolated natural products often have poor druggability and require further structural modification
At present, there are relatively few reports on artificially synthesized 4-arylpyran compounds in the field of anti-tumor, and the activity of these compounds is relatively poor, and further structural modification is needed

Method used

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  • Novel arylurea-containing 4-arylpyran derivative and application thereof
  • Novel arylurea-containing 4-arylpyran derivative and application thereof
  • Novel arylurea-containing 4-arylpyran derivative and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Example 1: Compound 1 6-amino-5-cyano-2-(2-methoxy-2-oxoethyl)-4-[3-(3-phenylureido)phenyl)-4H- Methyl pyran-3-carboxylate

[0047]

[0048] Preparation of step A 2-(3-nitrobenzylidene) malononitrile

[0049]

[0050] Take a 250mL reaction flask, add 3-nitrobenzaldehyde (15.00g, 99.3mmol), dissolve it with 100mL ethanol, add malononitrile (7.20g, 109.2mmol) in 60mL ethanol solution to the above dissolution, add triacetate Amine 2.0mL, stirred at room temperature for 2h, a large amount of solids precipitated during the reaction, filtered, the filter cake was washed three times with cold ethanol, and dried to obtain 17.6g of yellow solid, namely 2-(3-nitrobenzylidene) propane Nitrile.

[0051] Step B of 6-amino-5-cyano-2-(2-methoxy-2-oxoethyl)-4-(3-nitrophenyl)-4H-pyran-3-carboxylic acid methyl ester preparation

[0052]

[0053] Get a 250mL reaction bottle, add 2-(3-nitrobenzylidene) malononitrile (13.00g, 65.3mmol) respectively, dimethyl acetone dicarboxyla...

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Abstract

The invention belongs to the field of medicines, and particularly relates to a novel arylurea-containing 4-arylpyran derivative of a structure as shown in a general formula (I) as shown in the specification and application of the novel arylurea-containing 4-arylpyran derivative of the structure as shown in the general formula (I) as shown in the specification. The derivative is as shown in the general formula (I) as shown in the specification, and can be used medicinally when salts are formed by adding acids into the derivative, wherein R and Ar are defined in the specification. Results of pharmacological activity screening of the compound show that the compound has significant inhibiting effects on human colon cancer cells HT-29, human lung adenocarcinoma cell A549 and human large cell lung cancer cells H460, and has good anti-tumor medicine development and application prospects.

Description

technical field [0001] The invention belongs to the field of medicine, and specifically relates to a novel arylurea-containing 4-arylpyran derivative with a structure of general formula (I) and its application. Background technique [0002] Cancer is currently one of the diseases that kill the most human beings in the world, and it is also the most difficult scientific problem to overcome. In recent years, with the increasingly serious problem of population aging, the continuous increase of population, and the neglect of unhealthy lifestyles, the problem of people dying from cancer has become increasingly serious. In 2015, nearly 8.8 million people died of cancer worldwide, accounting for about one-sixth of the global death toll. Among them, lung cancer, colon cancer, stomach cancer, liver cancer and breast cancer are the main culprits of most cancer deaths every year. The number of cancer deaths worldwide will continue to increase, and the number of cancer deaths is expec...

Claims

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Application Information

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IPC IPC(8): C07D309/32A61P35/00
CPCC07D309/32A61P35/00
Inventor 卢久富靳玲侠季晓晖于小虎葛红光赵蔡斌宋娟
Owner SHAANXI SCI TECH UNIV
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