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Application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as derivative thereof

A technology of acetylamino and benzoyloxy, which is applied in the field of biomedicine, can solve the problems of high preparation cost and high price of finished drugs, and achieve the effects of simple preparation method, good therapeutic effect and abundant sources

Pending Publication Date: 2018-11-23
江苏吉诺思美精准医学科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, almost all immune checkpoint inhibitor drugs on the market are monoclonal antibodies, which are expensive to prepare, resulting in high prices for finished drugs

Method used

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  • Application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as derivative thereof
  • Application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as derivative thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 checks the molecular activity of 1,3-bis(benzoyloxy)-4-(acetylamino)benzene

[0020] The materials used are 1,3-bis(benzoyloxy)-4-(acetylamino)benzene, BMS-202 (PD-L1 small molecule inhibitor published in recent years), PD-1 protein, PD-L1 protein and the HTRF kit.

[0021] Firstly, the relationship between the substrate protein concentration was tested, and the effect of different concentrations of PD-L1 on the 665 / 620nm absorbance ratio was determined under the condition of PD-1 concentration of 100nM, and the model was established.

[0022] The experimental results are shown in the table.

[0023] PDL1 (nM)

0

0.13

0.25

0.5

1.0

2.0

4.0

8.0

Absorbance ratio

0.11

0.30

0.32

0.42

0.49

0.53

0.54

0.54

[0024] After using the HTRF kit process to test the two inhibitors at the same concentration, use a microplate reader to detect the absorbance values ​​at 665nm and 620nm, and use...

Embodiment 2

[0026] Example 2 checks the molecular activity of 1,3-bis(benzoyloxy)-4-(acetylamino)benzene derivatives

[0027] Chemically modify 1,3-bis(benzoyloxy)-4-(acetylamino)benzene, and oxidize its only aldehyde group to a carboxyl group. The synthesis method is as follows: 5g of 1,3-bis(benzoyl Acyloxy)-4-(acetylamino)benzene was dissolved in 30mL of benzene, and 20mL of 4% KMnO was added 4 solution, then add 10mL 1M dilute sulfuric acid, and react at room temperature. After 10h, the target modification (ms: 391.4) was obtained by recrystallization.

[0028] The molecular activity test of Example 1 was carried out on the modified product. It was found that the inhibitory rate of modification 1 on the binding of PD-1 and PD-L1 was 62.61%, which proved that 1,3-bis(benzoyloxy)-4-(acetylamino)benzene can improve the activity through certain modifications .

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PUM

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Abstract

The invention provides application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as a derivative thereof to inhibition of a PD-1 / PD-L1 signal path. The invention provides application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as the derivative thereof as a PD-1 / PD-L1 immune checkpoint inhibitor. The invention provides application of 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as the derivative thereof to preparation of PD-1 / PD-L1 immune checkpoint inhibition medicines. The 1,3-bis(benzoyloxy)-4-(acetyl amino) benzene as well as the derivative thereof is simple in structure, simple in preparation method, rich in sources and excellent in treatment effect.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to the application of 1,3-bis(benzoyloxy)-4-(acetylamino)benzene and its derivatives in inhibiting PD-1 / PD-L1 signaling pathway. Background technique [0002] With the continuous development of science and technology, people's treatment of cancer is not limited to using all means to kill cancer cells, and restoring the body's own immunity against cancer cells is a popular treatment method recently. Immune checkpoint is an inhibitory signaling pathway in the immune system, which regulates the intensity and persistence of immune responses in peripheral tissues, prevents tissue damage, and plays a role in the process of maintaining self-antigen tolerance. [0003] The PD-1 / PD-L1 pathway is one of the inhibitory signaling pathways in the immune system. The PD-1 receptor is expressed on the surface of T cells in the human body. When activated, it will inhibit the life activities of T cells an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/235A61P35/00
CPCA61P35/00A61K31/235
Inventor 韩维
Owner 江苏吉诺思美精准医学科技有限公司