Biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle and preparation method thereof

A biodegradable and macromolecular technology, applied in the field of chemical synthesis of new drugs and their preparations, can solve problems such as lack of photoactivity

Active Publication Date: 2012-04-18
吉林市博禹祥实工贸有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the problem that the prior art polymer-platinum (IV) bonded drug does not have photoactivity, and provide a biodegradable polymer bonded photoactive Pt (IV) anticancer drug micelle and a preparation method

Method used

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  • Biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle and preparation method thereof
  • Biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle and preparation method thereof
  • Biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle and preparation method thereof

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preparation example Construction

[0078] The present invention also provides a method for preparing a biodegradable polymer-bonded photoactive Pt(IV) anticancer drug, the preparation of the anticancer drug shown in formula 1 includes the following steps:

[0079] (1) Axial dihydroxy photoactive tetravalent platinum complex Pt(IV)-(OH) 2 React with an acid anhydride, introduce a ligand with a carboxylic acid in the axial direction of tetravalent platinum, and obtain a photoactive Pt(IV) complex with a carboxyl group in the axial direction. The reaction products are collectively referred to as "photoactive Pt(IV) with a carboxyl group". as "Pt(IV)-(OH) 2-x (COOH) x , with the following structure:

[0080]

[0081] In the formula, 1≤x≤2, wherein R is the part of the acid anhydride molecule that removes the carboxyl group, which can be an alkane, cycloalkane or aromatic structure, and the acid anhydride is succinic anhydride, glutaric anhydride, adipic anhydride, phthalic anhydride One of formic anhydride, c...

Embodiment 1

[0122] Example 1: Axial dihydroxy photoactive tetravalent platinum complexes c, c, t-[Pt(IV)(CHDA)(N 3 ) 2 (OH) 2 ] preparation

[0123] (1) 1.14g (10mmol) trans-1,2-cyclohexanediamine and 4.15g (10mmmol) potassium chloroplatinite were dissolved in 100ml twice-distilled water, and stirred and reacted in the dark for 12 hours to obtain the complex of divalent platinum Substance c, c-[Pt(II)(CHDA)Cl 2 ]3.5g;

[0124] (2) 1.9 g (5 mmol) of c, c-[Pt(II)(CHDA)Cl obtained in the above step (1) 2 ] and the silver nitrate of 1.7g (10mmol) were dissolved in the distilled water of 100ml, at room temperature avoid light stirring reaction 12 hours, filter method removes precipitate AgCl, obtains divalent platinum hydrate nitrate c, c-[Pt 2+ (II)(CHDA)(H 2 O) 2 ](NO 3 - ) 2 ;

[0125] (3) c, c-[Pt obtained by the above step (2) 2+ (II)(CHDA)(H 2 O) 2 ](NO 3 - ) 2 The aqueous solution was reacted with 0.65g (10mmol) of sodium azide at room temperature for 4h to obtain the d...

Embodiment 2

[0128] Example 2: Photoactive platinum (IV) complex CDA-Pt(IV)-(OH) with carboxyl groups in the axial direction 2-x (COOH) x preparation of

[0129] 200mg (0.576mmol) CDA-Pt(IV)-(OH) 2 Dissolve in 16mL DMSO, add the succinic anhydride of the listed weight in Table 1, stir and react at room temperature for 12 hours to obtain a mixed solution, the mixed solution is precipitated with 200mL acetone, the precipitate is washed with acetone and ether successively, and vacuum-dried at room temperature to obtain CDA-Pt(IV)-(OH) 2-x (COOH) x , the results are shown in Table 1.

[0130] Table 1. CDA-Pt(IV)-(OH) 2 - Preparation of succinic anhydride complex

[0131]

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Abstract

The invention provides a biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle and a preparation method thereof, which relate to the field of novel chemical synthesis medicaments and preparations thereof and are used for solving the problem that a high-polymer-platinum (IV) bonded medicament does not have optical activity in the prior art. In an anticancer medicament, ethylene glycol-b-polyester-b-polylysine serving as a biodegradable triblock copolymer or polyethylene glycol-b-poly(ester-co-carbonic ester) serving as a diblock copolymer is taken as a carrier polymer, and Pt (IV) is a photoactive tetravalent platinum composition coordinated with dihydroxyl in the axial direction. The invention further provides a preparation method of the biodegradable high-polymer bonded photoactive Pt (IV) anticancer medicament micelle. The anticancer medicament prepared with the method has remarkable optical activity; under the irradiation of UV (Ultraviolet) of 365 nanometers, Pt (IV) is reduced into Pt (II); a cis-platinum or oxaliplatin antitumor active part is contained; and the mass content of platinum can be up to 10-20 percent.

Description

technical field [0001] The invention belongs to the field of chemically synthesized new drugs and preparations thereof, in particular to a biodegradable macromolecular bonded photoactive Pt (IV) anticancer drug micelle and a preparation method. Background technique [0002] Since the discovery of cisplatin's anticancer activity in 1967, the research and application of platinum-based metal anticancer drugs have been greatly developed. Thousands of platinum series compounds have been screened successively, dozens of them have entered clinical research, and several have been approved to enter the market. [0003] Cis-dichlorodiammine platinum (II), also known as cisplatin (cisplatin), is a cell cycle non-specific drug and the most clinically used divalent platinum drug, which can combine with DNA to form cross-links. Thereby disrupting the replication function of DNA. Clinical practice has proved that cisplatin has a broad anticancer spectrum, strong effect, synergistic effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/282A61K9/19A61P35/00
Inventor 景遐斌肖海华郑勇辉胡秀丽黄宇彬周东方柳时齐若谷
Owner 吉林市博禹祥实工贸有限公司
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