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Anti-bacterial and anti-cancer active compound

An anti-cancer activity and compound technology, applied in the field of medical drugs, can solve problems such as the inability to effectively improve the survival rate of patients with advanced liver cancer, developed and produced by Bayer in Germany in 2008, and has large toxic and side effects, achieving good clinical application value, good The effect of killing activity

Active Publication Date: 2013-11-20
宁夏蓝博思化学技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason for the high mortality rate of liver cancer is that most liver cancer patients are already in the middle and late stage of cancer when they are diagnosed, and the existing treatment methods, including surgical resection, interventional therapy, and radiotherapy, cannot effectively improve the survival rate of patients with middle and late stage liver cancer ( 5-year survival rate is about 20%)
However, chemotherapy drugs that are more effective in the treatment of other cancers, such as fluorouracil (fluorouracil), doxorubicin (doxorubicin), cisplatin (cisplatin), etc., have unsatisfactory therapeutic effects and large toxic and side effects in liver cancer.
Nexavar (Sorafenib), developed and produced by Bayer AG in 2008, is the only oral drug approved so far for the treatment of advanced liver cancer, but it can only temporarily delay the development of liver cancer

Method used

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Experimental program
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preparation example Construction

[0019] The preparation method of antibacterial and anticancer active compound of the present invention, the preparation method of this antibacterial and antitumor active compound comprises the following steps:

[0020] Under ice bath cooling, compound HRB-1365-0, compound HRB-1365-1, and water were stirred and reacted under alkaline conditions, and filtered to obtain a white solid, which was compound HRB-1365-2;

[0021] Under ice-bath cooling, compound HRB-1365-2, compound HRB-1365-1, and triethylamine were stirred and reacted in methanol. After the reaction was completed, the methanol was concentrated under reduced pressure, the residue was washed with water, and filtered to obtain a yellow solid that was is compound HRB-1365;

[0022] The ethanol solution of the compound HRB-1365 was cooled and stirred in an ice bath, and the dried hydrogen chloride gas was passed into it. When the hydrogen chloride gas was saturated, the stirring was continued, and the product was filtered...

Embodiment 1

[0052] Embodiment 1 Reaction equation:

[0053]

[0054] The present invention is further described in conjunction with the anticancer activity test:

[0055] Human liver cancer cell line SMMC7721, human lung cancer cell line A549, and human gastric and pancreatic cancer cell line SGC7901 were provided by Ningxia University.

[0056] Cytotoxicity was evaluated by the MTT method. Cells were inoculated in a 96-well plate at an appropriate concentration, with a total volume of 192 μL per well. After 24 hours of culture, 8 μL of compounds of different concentrations were added. A solvent control group was set up at the same time. Drug culture solution, wash the well plate once with PBS, add 100 μL MTT solution to the culture solution again, and continue to cultivate for 4 hours, remove the culture solution, add DMSO, and after the color is completely dissolved, use an enzyme-linked instrument with a dual wavelength of 540 / 655nm Determine the absorbance value and calculate the ...

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Abstract

The invention discloses an anti-bacterial and anti-cancer active compound. The anti-bacterial and anti-cancer active compound or an addition product thereof is shown in the specification, wherein substituent groups of R1, R2, R3 and R4 are selected from a hydroxyl, an amino group, a nitryl, a halogen atom, a hydrogen atom, a C1-6 alkyl, a C2-6 alkenyl, a C6-10 aryl, a C1-6 alkyl acylamino group or a C1-6 alkoxy carbonyl. A novel compound is prepared by a hydrochloride salt, has an anti-bacterial effect and significant anti-cancer activity, and has good clinical application values.

Description

technical field [0001] The invention belongs to the technical field of medical drugs, and in particular relates to an antibacterial and anticancer active compound. Background technique [0002] Tumor is a new organism formed by the body under the action of various carcinogenic factors when a certain cell in a local tissue loses normal regulation of its growth at the gene level, resulting in abnormal clonal proliferation. It is generally believed that tumor cells are monoclonal, that is, all tumor cells in a tumor are descendants of a mutant cell. Tumors are generally divided into benign and malignant. All malignant tumors are collectively called cancer. At present, the death caused by malignant tumor is the second leading cause of human death after cardiovascular disease. [0003] my country is a big country with liver cancer. There are about 350,000 newly discovered cases of liver cancer every year, accounting for about 50% of the new cases in the world. There are 300,00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/18A61P35/00A61P31/04
Inventor 葛瑞武
Owner 宁夏蓝博思化学技术有限公司