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Use of lauryl diamine derivatives in preparation of drugs for treatment of cancer

A technology of lauryl diamine and derivatives, applied in the field of medicine

Inactive Publication Date: 2019-01-18
柴梦莹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no specific targeted small molecule drug that can effectively inhibit the growth of cancer cells against the carcinogenesis mechanism of colon cancer.

Method used

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  • Use of lauryl diamine derivatives in preparation of drugs for treatment of cancer
  • Use of lauryl diamine derivatives in preparation of drugs for treatment of cancer
  • Use of lauryl diamine derivatives in preparation of drugs for treatment of cancer

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0057] Experimental Example 1 Inhibition of Test Compounds Binding to 12G5 Antibody CXCR4 Receptor Experiment

[0058] CXCR4 is a cell membrane biomarker of cancer cell proliferation and malignant division, and SDF-1 is a natural chemokine and agonist of CXCR4. Therefore, by effectively inhibiting the binding of CXCR4 to SDF-1, the signal of CXCR4 can be inhibited, normal cell physiological functions can be maintained, and hematopoietic differentiated cells (immune cells and leukocytes) can be prevented from entering the malignant proliferation program. When CXCR4 is stimulated by a signal that is too strong, whether it is positive regulation or negative regulation will cause CXCR4 intracellular signal regulation disorders, resulting in imbalanced cell growth.

[0059] 12G5 is a general commercial antibody that recognizes CXCR4 as a murine monoclonal antibody. 12G5 antibody has strong binding affinity to CXCR4 and can be used to recognize CXCR4.

[0060] In this experiment, ...

experiment example 2

[0069] Experimental example 2 Specific recognition experiment of test compound to CXCR4

[0070] The CCR5 receptor is a specific chemokine receptor expressed by T lymphocytes in the activated state. For T lymphocytes, both CXCR4 and CCR5 are induced to express when they are activated or activated by various signals. CXCR4 and CCR5 sometimes aggregate into heterodimers, and the irregular combination will lead to changes in the signaling of membrane receptors and complete changes in cell physiological functions, which may produce unpredictable side effects, resulting in membrane receptors produced by them. Signaling mutagenic malignancy signaling for carcinogenesis. Therefore, in order to confirm the specific recognition ability of the three lauryl diamine derivatives in the present application to CXCR4, this experiment was carried out.

[0071] In order to confirm the binding specificity of the test compound to CXCR4 but not to CCR5, the inventors chose to use A3.01-R5T lymph...

experiment example 3

[0079] Experimental Example 3 The specific recognition experiment of the test compound to SDF-1 binding to CXCR4

[0080] The expression of CXCR4 and CXCR7 receptors is a molecular basis for lymphocyte migration, activation, clustering and effect. But in general, the expression of the receptor and the signaling effect of agonists on the receptor make the chemokine receptor a favorable signaling pathway for cancer or virus invasion. Using the CXCR4 and CXCR7 receptors expressed on the cell membrane as targets to specifically inhibit the binding of SDF-1 to CXCR4 or CXCR7 will be an important indicator for targeting CXCR4 antagonists.

[0081] SDF-1 can specifically recognize CXCR4 and CXCR7. In order to confirm that the lauryl diamine derivatives in the present application can specifically block the binding of SDF-1 to CXCR4, but not to CXCR7, the inventors proved by the following experiments.

[0082] 1. Experimental principle

[0083] SDF-1 will be coupled with Tebium reage...

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Abstract

The invention provides an application of a lauryl diamine derivative in preparing a medicine for treating cancer, belonging to the cancer field. A study by that inventor found that the three lauryl diamine derivatives represented by formulae I, II and III were potent regulators of SDF-1 Possible inducible CXCR4-stimulated carcinogenesis signal, inducible modulation of SDF-1 From a potent agonist to a partial or less potent agonist in physiological or pathological conditions. These three compounds can target CXCR4 specifically and kill cancerous cells efficiently. They can be used as therapeutic drugs for cancer and have a broad application prospect.

Description

technical field [0001] The present invention relates to the field of medicine, in particular, to the application of a lauryl diamine derivative in the preparation of a medicine for the treatment of cancer. Background technique [0002] The incidence of colorectal cancer in China ranks third in the incidence spectrum of malignant tumors, second only to lung cancer and gastric cancer; the mortality rate ranks fifth, after lung cancer, liver cancer, gastric cancer and esophageal cancer. The prolongation of survival is more obvious in middle-advanced colorectal cancer, which is mainly related to adjuvant therapy for middle-advanced colorectal cancer, such as preoperative radiotherapy and chemotherapy. Advances in imaging diagnosis have improved the detection rate and diagnostic accuracy of colorectal cancer liver metastases. The application of a series of targeted therapy drugs such as anti-EGFR and anti-VEGF has improved the survival rate of patients with advanced colorectal ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4178A61P35/00
CPCA61K31/4178A61P35/00
Inventor 周志诚柴梦莹
Owner 柴梦莹
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