Application of 4-benzothiopheneaminoquinazoline derivative in preparing tumor treatment medicine

A benzothiophene aminoquinazoline, tumor drug technology, applied in the research field of anti-tumor drugs, can solve the problems of difficulty, no anti-tumor activity evaluation, impossible application and the like

Inactive Publication Date: 2010-09-22
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For the application in pharmaceuticals, the technical scheme only provides the single-concentration inhibition rate of the three tumor cell lines, and there is no research on the target and mechanism of action of these compounds, let alone the evaluation of an...

Method used

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  • Application of 4-benzothiopheneaminoquinazoline derivative in preparing tumor treatment medicine
  • Application of 4-benzothiopheneaminoquinazoline derivative in preparing tumor treatment medicine
  • Application of 4-benzothiopheneaminoquinazoline derivative in preparing tumor treatment medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Compound 1-20 inhibits receptor tyrosine kinase

[0046] EGFR, HER-2, c-MET and other kinase detection kits from Cell Signaling Technology were used to measure the effects of various concentrations of compounds 1-20 and two positive control compounds Gefitinib and Erlotinib on the above receptor tyrosine according to the product instructions. Inhibitory activity of amino acid kinase (inhibition rate and half inhibitory concentration IC50, figure 1 ). Table 2 lists the inhibitory rates of 10.0 μM compounds 1-20 and two positive control compounds on three kinases, and the data are the average values ​​of two independent experiments. As can be seen from the experimental results, the inhibitory activity of compounds 11-20 (except compound 16) to HER-2 is equivalent to or better than the positive control compound, and the inhibitory activity to c-MET is better than the positive control compound; Compound 12 , 15, 17, 18 and 19 had slightly less inhibitory activit...

Embodiment 2

[0047] Example 2 Compound 1-20 inhibits tumor cell growth

[0048] Six different human tumor cell lines were treated with compounds 1-20 and two positive control compounds Gefitinib and Erlotinib. Two human pancreatic cancer cells, Miapaca2 and Panc1, two human prostate cancer cells, DU145 and PC3, and two human lung cancer cells, A549 and NCI-H661, were seeded in 96-well cell culture plates, and compound 1-20 and Two positive control compounds. At 37°C, 5% CO 2 After culturing in an incubator for 72-96 hours, the survival rate of the cells was detected with WST-8 reagent. The half maximal inhibitory concentrations (IC50) of 22 compounds on 6 kinds of human cell lines are shown in Table 2, and the data are the average value of three independent experiments. It can be seen from the experimental results that most of the compounds exhibit tumor cell growth inhibitory activity superior to the positive control compounds.

[0049] HER-2-negative breast cancer cells MCF-7 and HER...

Embodiment 3

[0050] Example 3 Compounds 15 and 17 Induce Pancreatic Cancer Cell Miapaca2 Apoptosis

[0051] Pancreatic cancer cells Miapaca2 were inoculated in 6-well cell culture plates, and the cells were treated with different concentrations of compounds 15, 17 and Gefitinib for 48 hours, then the cells were collected, stained with propidium iodide (PI), and analyzed by flow cytometry. dead cells. The experimental results showed that the percentage of apoptosis in Miapaca2 cells increased with the concentration of compounds 15 and 17, and 10.0 μM of compounds 15 and 17 could induce about 25% of the apoptosis, while Gefitinib at the same concentration could hardly induce apoptosis ( image 3 ).

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PUM

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Abstract

The invention discloses application of 4-benzothiopheneaminoquinazoline derivative and salt thereof in preparing tumor treatment medicine. The in vitro and in vivo activities of the 4-benzothiopheneaminoquinazoline derivative are evaluated; and the derivative kills tumor cells by means of inducing tumor cell apoptosis and autophagy to inhibit the growth of tumor cells and provide the application in preparing medicaments for treating cancers, especially pancreatic cancer, prostate cancer, lung cancer or breast cancer. In the invention, the action mechanism and the action target of the 4-benzothiopheneaminoquinazoline derivative are studied, and the derivative has stronger inhibitory activity to a plurality of receptortyrosinekinases and provides the application of acting as an inhibitor of receptortyrosinekinase, especially polyreceptortyrosinekinase.

Description

technical field [0001] The invention relates to the application of an antitumor compound, which belongs to the research field of antitumor drugs. Specifically, the present invention relates to a kind of 4-benzothiophene aminoquinazoline derivative and its salt, its application in the preparation of various tumor medicines for treating pancreatic cancer, prostate cancer, lung cancer or breast cancer, and its application in the preparation of Applications of Multiple Receptor Tyrosine Kinase Inhibitors Background technique [0002] Tumors seriously endanger human health. With the development of molecular biology, cell biology and other disciplines, the pathogenesis of tumors has been further clarified. Studies have shown that overexpression or activation of different receptor tyrosine kinases (receptortyrosinekinases, RTK) can be seen in many tumors, such as overexpression of the epidermal growth factor receptor (EGFR) family in epithelial cell tumors. The activation of thes...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K31/517A61P35/00
Inventor 吉民吴晓晴徐良郑友广李铭东
Owner SOUTHEAST UNIV
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