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Epidermal growth factor receptor tyrosine kinase inhibitors NXGF and NXGH with antineoplastic activity and preparing method and application thereof

An epidermal growth factor and tyrosine kinase technology, applied in the field of biomedicine, can solve the problems of not significantly prolonging the survival period of patients, treatment failure, etc., achieving excellent anti-tumor activity and inhibiting proliferation.

Inactive Publication Date: 2016-06-08
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, reversible and irreversible EGFRTKI have significant curative effect on mutated EGFR non-small cell lung cancer in a short period of time, but eventually all of them failed due to acquired drug resistance, and did not significantly prolong the survival of patients

Method used

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  • Epidermal growth factor receptor tyrosine kinase inhibitors NXGF and NXGH with antineoplastic activity and preparing method and application thereof
  • Epidermal growth factor receptor tyrosine kinase inhibitors NXGF and NXGH with antineoplastic activity and preparing method and application thereof
  • Epidermal growth factor receptor tyrosine kinase inhibitors NXGF and NXGH with antineoplastic activity and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The preparation of embodiment 1EGFRTKI-NXGF and EGFRTKI-NXGH

[0050] The molecular structural formula of described NXGF is as shown in formula I, and the molecular structural formula of described NXGH is as shown in formula II:

[0051]

[0052] The preparation flow chart is as figure 1 and figure 2 As shown, the specific preparation method is as follows:

[0053] (1) Under the protection of nitrogen, mix 60g of 2-amino-4 chlorobenzoic acid and 315ml of formamide and react at 160°C for 10h, pour into ice water after cooling, filter with suction, wash the filter cake with water and methanol respectively, and finally wash with ether and n-hexane Each of the alkanes was washed once, and dried to obtain 43.0 g of a light brown solid (compound 1), with a yield of 68.%;

[0054] (2) Add 38ml of concentrated sulfuric acid into a single-necked bottle, cool down to below 0°C, add 36ml of concentrated nitric acid dropwise, keep the temperature below 5°C, add 12.0g of comp...

Embodiment 2

[0075] Example 2 Inhibition test of NXGF and NXGH of the present invention on mutant EGFR non-small cell lung cancer cell line HCC827

[0076] 1. Compounds to be tested: NXGF, NXGH, prepared by the method of Example 1

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Abstract

The invention discloses epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) NXGF and NXGH with antineoplastic activity and a preparing method and application thereof, and belongs to the field of biological medicine. The brand new EGFR TKI are obtained by optimizing and improving the chemical structure of Pelitinib and named NXGF (the formula I) and NXGH (the formula II) respectively. It is shown through research that the synthesized EGFR TKI-NXGF and the synthesized EGFR TKI-NXGH can effectively inhibit proliferation of tumor cells, have a higher proliferation inhibiting effect on the mutation EGFR lung cancer cell line HCC827 compared with Pelitinib, and thus can be clinically applied as an antineoplastic agent. The invention further discloses the preparing method of the EGFR TKI NXGF and NXGH with antineoplastic activity. By proposing the EGFR TKI NXGF and NXGH with antineoplastic activity, and the preparing method and application thereof, an effective technical means is provided for treating tumors and especially non-small cell lung cancer.

Description

technical field [0001] The invention relates to quinazoline compounds, in particular to EGFRTKI-NXGF and NXGH with anti-tumor activity and their preparation methods. The invention also relates to the application of the drugs as anti-tumor agents, which belongs to the field of biomedicine. Background technique [0002] The currently discovered EGFR tyrosine kinase (EGFRTK) can catalyze the transfer of high-energy phosphate bonds of ATP to several tyrosine sites of EGFR to phosphorylate them, thereby activating downstream PI3K / Akt, Ras / MAPK and other signaling pathways, Promote cell growth, proliferation, metabolism, and inhibit cell apoptosis. When EGFR is overexpressed and mutated in cells, it will hinder the programmed death of cells, make the growth regulation of cells out of control, and obtain unlimited proliferation and invasion ability, that is, develop into malignant tumor cells. EGFRTKI competes with ATP for the binding site of intracellular tyrosine kinase, prevent...

Claims

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Application Information

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IPC IPC(8): C07D239/94A61P35/00
CPCC07D239/94
Inventor 申宝忠孙夕林杨丽丽王颖奕韩兆国桂媛朱玉军葛正兴徐志红
Owner HARBIN MEDICAL UNIVERSITY
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