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Application of quinoline derivative of N isostere tectoridin in anti-hepatoma drugs

An isostere and irisin technology, applied in the application field of quinoline derivatives in anti-liver cancer drugs, to achieve the effects of improving the generation of ROS, less drug resistance and adverse reactions, and remarkable therapeutic effect

Inactive Publication Date: 2018-02-09
GUANGZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned molecular targeted drugs also have their own limitations.

Method used

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  • Application of quinoline derivative of N isostere tectoridin in anti-hepatoma drugs
  • Application of quinoline derivative of N isostere tectoridin in anti-hepatoma drugs
  • Application of quinoline derivative of N isostere tectoridin in anti-hepatoma drugs

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Experimental program
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Embodiment

[0033] The application of the quinoline derivative of N electron isostere irisin in anti-liver cancer drugs.

[0034] The quinoline derivative of the N-electron isostere irisin, its chemical structural formula is:

[0035] .

[0036]The quinoline derivatives of the N-electron isostere irisin inhibit the proliferation of liver cancer cells by inhibiting the RAF / MEK / ERK pathway and the JAK / STAT pathway; the quinoline derivatives of the N-electron isostere irisin inhibit the proliferation of P13K / The AKT / mTOR pathway promotes the apoptosis of liver cancer cells; the quinoline derivative of the N electron isostere irisin promotes the apoptosis of liver cancer cells by up-regulating the anti-apoptosis signal P53 and the anti-apoptosis signal PTEN gene.

[0037] The quinoline derivative of the N-isostere irisin increases the expression level of the anti-apoptotic signal p53, increases the generation of ROS, increases the permeability of the mitochondrial membrane and causes the ...

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Abstract

The invention discloses an application of a quinoline derivative of N isostere tectoridin in anti-hepatoma drugs. The chemical structural formula of the quinoline derivative of the N isostere tectoridin is shown as Formula (as shown in the description); and the invention also provides an application of the quinoline derivative, namely New Tectorigenin, of the N isostere tectoridin in preparing drugs for inhibiting hepatic carcinoma HepG2 cells. According to the invention, the proliferation of the hepatic carcinoma HepG2 cells can be inhibited by inhibiting an RAF / MEK / ERK pathway and a JAK / STATpathway. The anti-hepatoma drugs provided by the invention are obvious in therapeutic effect, and cannot cause drug resistance and adverse reactions easily.

Description

technical field [0001] The invention relates to an isostere of irisaxanthin, in particular to the application of a quinoline derivative of an isostere of irisin in anti-liver cancer drugs. Background technique [0002] Primary liver cancer (primary hepatic carcinoma, PHC) refers to cancer that occurs in hepatic parenchymal cells or intrahepatic bile duct epithelial cells. It is a malignant tumor with high malignancy, rapid progression, poor prognosis, and short survival period. The survival rate is only 3% to 5%. Globally, the morbidity and mortality of primary liver cancer rank seventh and third among all tumors, respectively. my country is a country with a large incidence of liver cancer, accounting for 45% of the global incidence. In recent years, the incidence of liver cancer in my country has been on the rise, and the mortality rate has also risen accordingly, accounting for the third place in the national cancer mortality rate. The 2010 national census population in...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61P35/00A61P35/04
CPCA61K31/47A61P35/00A61P35/04C07D215/20
Inventor 陈鲲肖竹平马咏思黎裕麟黎慧杰刘碧君陈裕华朱海亮张建华
Owner GUANGZHOU UNIVERSITY
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