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Amphipathic polymer with main chain containing double anticancer drugs, as well as preparation method and nano-micelle of amphipathic polymer

A technology of amphiphilic polymers and anticancer drugs, which is applied in the field of preparation of amphiphilic polymers and nanomicelles containing double anticancer drugs in the main chain, which can solve the problems of high toxicity and side effects, low bioavailability, and easy metabolism And other issues

Active Publication Date: 2016-01-20
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no matter which of the above tetravalent platinum prodrug forms of combined chemotherapy, there are still problems such as wide distribution in the body, easy to be metabolized, low bioavailability, and sometimes more toxic and side effects.

Method used

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  • Amphipathic polymer with main chain containing double anticancer drugs, as well as preparation method and nano-micelle of amphipathic polymer
  • Amphipathic polymer with main chain containing double anticancer drugs, as well as preparation method and nano-micelle of amphipathic polymer
  • Amphipathic polymer with main chain containing double anticancer drugs, as well as preparation method and nano-micelle of amphipathic polymer

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preparation example Construction

[0048] The present invention also provides a method for preparing amphiphilic polymers containing double anticancer drugs in the main chain, including the following steps:

[0049] Step 1: reacting a platinum (II) compound with hydrogen peroxide to obtain a platinum (IV) compound;

[0050] Step 2: reacting the platinum (IV) compound obtained in step 1 with cantharidin or demethylcantharidin to obtain a platinum (IV) cantharidin complex or a platinum (IV) norcantharidin complex;

[0051] Step 3: react the platinum (IV) cantharidin complex or platinum (IV) demethylcantharidin complex obtained in step 2 with diamine and polyethylene glycol to obtain a main chain containing double anticancer drug with high amphipathic molecular.

[0052] According to the present invention, the platinum (II) compound is first reacted with hydrogen peroxide to obtain the platinum (IV) compound, the reaction temperature is preferably room temperature, the reaction time is preferably 12h, the platinu...

Embodiment 1c

[0067] Example 1c, c-[Pt(II)(CDA)(N 3 ) 2 ] preparation

[0068] (1) 1.57g (5mmol) of c,c-[Pt(II)(CDA)Cl 2 ] and 1.7g (10mmol) of silver nitrate were dissolved in 100ml of distilled water, stirred and reacted in the dark at room temperature for 12h, and the precipitate AgCl was removed by filtration to obtain divalent platinum hydrate nitrate c,c-[Pt 2+ (II)(CDA)(H 2 0) 2 ](NO 3 - ) 2 ;

[0069] (2) The above c,c-[Pt 2+ (II)(CDA)(H 2 0) 2 ](NO 3 - ) 2 The aqueous solution was reacted with 0.65g (10mmol) of sodium azide at room temperature for 4h to obtain the divalent platinum diazide complex c,c-[Pt(II)(CDA)(N 3 ) 2 ] Yellow precipitate.

Embodiment 2c

[0070] Example 2c, c-[Pt(II)(CHDA)(N 3 ) 2 ] preparation

[0071] (1) Dissolve 1.14g (10mmol) trans-1,2-cyclohexanediamine and 4.15g (10mmmol) potassium chloroplatinite in 100ml double-distilled water, and stir for 12 hours in the dark to obtain a complex of divalent platinum c,c-[Pt(II)(CHDA)Cl 2 ];

[0072] (2) 1.9 g (5 mmol) of c,c-[Pt(II)(CHDA)Cl 2 ] and 1.7g (10mmol) of silver nitrate were dissolved in 100ml of distilled water, stirred and reacted in the dark at room temperature for 12h, and the precipitate AgCl was removed by filtration to obtain divalent platinum hydrate nitrate c,c-[Pt 2+ (II)(CHDA)(H 2 0) 2 ](NO 3 - ) 2 ;

[0073] (3) The above c,c-[Pt 2+ (II)(CHDA)(H 2 0) 2 ](NO 3 - ) 2 The aqueous solution was reacted with 0.65g (10mmol) of sodium azide at room temperature for 4h to obtain the divalent platinum bis-azide complex c,c-[Pt(II)(CHDA)(N 3 ) 2 ] Yellow precipitate.

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Abstract

The invention provides an amphipathic polymer with a main chain containing double anticancer drugs, as well as a preparation method and a nano-micelle of the amphipathic polymer, and belongs to the technical field of chemical synthetic drugs. The structural formula of the amphipathic polymer is shown in the formula I. The amphipathic polymer is obtained by leading a quadrivalent platinum cantharidin complex or a quadrivalent platinum norcantharidine complex into the main chain of the polymer, wherein the quadrivalent platinum cantharidin complex or the quadrivalent platinum norcantharidine complex is taken as a main body, and is connected with the main chain through an amide bond to serve as a hydrophobic section, and a polyethylene glycol chain is taken as a hydrophilic section; the obtained polymer is relatively high in antineoplastic activity but relatively low in cytotoxicity. The invention further provides the preparation method of the mphipathic polymer, and the nano-micelle made of the amphipathic polymer.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis of medicines, and in particular relates to an amphiphilic macromolecule whose main chain contains double anticancer drugs, a preparation method and nano micelles thereof. Background technique [0002] Since Rosenberg accidentally discovered the anticancer activity of cisplatin in 1965, bivalent platinum drugs such as cisplatin, carboplatin, and oxaliplatin have been used as cancer chemotherapy drugs to treat more than half of cancers, such as testicular cancer, bladder cancer, and lung cancer. Wait. However, platinum drugs such as cisplatin are almost lack of selectivity, causing great toxic and side effects on normal tissues and organs, and reducing the patient's tolerance to the drug. What's more serious is that many cancers show innate resistance to platinum drugs such as cisplatin, or acquire drug resistance after repeated chemotherapy, which further limits the chemotherapeutic eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/00C08G65/337C08G65/333A61K9/107A61K33/24A61P35/00A61K31/365A61K31/282A61K31/194A61K31/44
Inventor 黄宇彬周东方丛雨微王明哲谢志刚景遐斌
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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