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Chemical substance with anticancer activity and preparation method and application thereof

A technology for chemical substances and anti-cancer activity, which is applied to the field of chemical substances with anti-cancer activity and their preparation, can solve the problems that the anti-tumor activity needs to be further improved, the advantages of Satraplatin are not outstanding, achieves good killing effect, and the preparation method is simple and easy. line, low cytotoxicity

Active Publication Date: 2016-08-31
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in terms of curative effect, compared with cisplatin and carboplatin, Satraplatin has no outstanding advantages except oral activity, and its antitumor activity needs to be further improved

Method used

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  • Chemical substance with anticancer activity and preparation method and application thereof
  • Chemical substance with anticancer activity and preparation method and application thereof
  • Chemical substance with anticancer activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0037] The method for preparing the above-mentioned chemical substance with anticancer activity is as follows:

[0038] A) The platinum (II) compound and hydrogen peroxide are stirred and reacted under dark conditions, the reaction temperature is room temperature, and the reaction time is 5-10h. After the reaction is completed, purification (purification process generally involves filtration) to obtain yellow powder, which is platinum (IV) Compound;

[0039] Among them, platinum (II) compounds are Cisplatin, Oxaliplatin, pyAA-Pt-Cl 2 Or CHAA-Pt-Cl 2 The present invention has no special requirements for its source, and it can be generally commercially available; hydrogen peroxide has no special requirements, preferably 30% hydrogen peroxide; the molar ratio of the volume of hydrogen peroxide to the platinum (II) compound is preferably (5mL~15mL):( 1mmol~3mmol);

[0040] The reaction formula of step A) is as follows (where M 1 , M 2 , M 3 , M 4 Both represent substituents, which are s...

Embodiment 1

[0052] Put cisplatin (600mg, 2mmol) in the flask, then add 10mL of 30% hydrogen peroxide, stir at room temperature and avoid light for 8h, filter and remove hydrogen peroxide to obtain Cisplatin(IV)-(OH) 2 Yellow powder.

[0053] The resulting Cisplatin(IV)-(OH) 2 (334mg, 1mmol), N,N'-Dicyclohexylcarbodiimide (185.6mg, 0.9mmol) was placed in a dried polymerization bottle, ventilated three times, and then added 5ml of dried DMF, 20℃ After stirring for 0.5 h, artesunate (307.5 mg 0.8 mmol) was added, and the reaction was stirred at 10° C. for 16 h. Then the DMF in the system was drained, the remaining material was dissolved in acetone, and the insoluble material was filtered off, the filtrate was concentrated and the ether settled, the obtained solid was filtered and vacuum dried to obtain compound 1, which was 317.3 mg of white solid powder.

[0054] The reaction formula is as follows:

[0055]

[0056] The prepared compound 1 was characterized by infrared absorption spectroscopy, nu...

Embodiment 2

[0059] Put cisplatin (600mg, 2mmol) in a flask, add 10 mL of 30% hydrogen peroxide, stir at room temperature and avoid light for 8 hours, filter and remove hydrogen peroxide to obtain Cisplatin(IV)-(OH) 2 Yellow powder.

[0060] The resulting Cisplatin(IV)-(OH) 2 (334mg, 1mmol), N,N'-Dicyclohexylcarbodiimide (226.8, 1.1mmol) was placed in a dried polymerization flask, ventilated three times, and then 5ml dried DMF was added to it, at 20℃ After stirring for 1 h, artesunate (384.4 mg, 1 mmol) was added, and the reaction was stirred at 10° C. for 18 h. Then the DMF in the system was drained, the remaining material was dissolved in acetone, and the insoluble material was filtered off, the filtrate was concentrated and the ether was settled, the obtained solid was filtered and vacuum dried to obtain compound 1, which was 335 mg of white solid powder.

[0061] The reaction formula is as in Example 1.

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Abstract

The invention discloses a chemical substance with anticancer activity and a preparation method and application thereof, belongs to the technical field of chemically-synthesized medicine, and aims to provide the chemical substance with low cytotoxicity, low drug resistance and high anticancer activity. The chemical substance is a compound as shown in formula (I), a compound as shown in formula (II) or the mixture of the compound as shown in formula (I) and the compound as shown in formula (II). The chemical substance has the advantages that the chemical substance is obtained by the mating reaction of artesunate and a platinum (IV) compound, the cytotoxicity of the platinum (IV) compound is lowered by introducing the artesunate ligand, the anticancer cavity of the platinum (IV) compound is increased, and the chemical substance is low in drug resistance and widely applicable to the preparation of anticancer medicine.

Description

Technical field [0001] The invention relates to the technical field of chemically synthesized drugs, in particular to a chemical substance with anti-cancer activity and a preparation method and application thereof. Background technique [0002] Since people discovered that cisplatin has anticancer activity in 1967, the research and application of platinum metal anticancer drugs have been developed for a long time. At present, thousands of platinum series compounds have been screened, and dozens of them have entered clinical research. , Several have been approved to enter the market. [0003] Among them, platinum (II) (representing divalent platinum) has been widely used in chemotherapy. For example, cisplatin (II), also known as cisplatin, is a periodic non-specific Drugs are the most widely used bivalent platinum drugs in clinical use. They can combine with DNA to form cross bonds, thereby destroying the replication function of DNA. Clinical practice has proved that cisplatin ha...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0086C07F15/0093
Inventor 黄宇彬周东方景遐斌谢志刚
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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