New compound having anthracycline antibiotic structure, and preparation method and application thereof

A technology of antibiotics and anthracyclines, which is applied in the field of new compounds containing anthracycline antibiotics structure and its preparation and application, can solve the problems of low solubility, decreased pharmacodynamic function of doxorubicin, and application limitations, etc., and achieve easy dissolution Effect

Active Publication Date: 2014-07-09
张雅珍
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Anthracycline antibiotics are currently widely used, but they often need to be turned into salts from a clinical point of view, such as doxorubicin. The common medicinal form is doxorubicin hydrochloride, which needs to be turned into hydrochloride. Its solubility is very low, it cannot be converted into salt form, so it cannot be used
After becoming hydrochloride, the pharmacodynamic function of doxorubicin is greatly reduced, so this brings great difficulties to clinical application.
[0004] Another disadvantage of anthracycline antibiotics is that due to their strong cytotoxicity, they are very toxic. They often have obvious bone marrow suppression about 10 days after use. After a week of use, they can show very obvious gastrointestinal tract Adverse reactions and cardiotoxicity, so the drug must be accurately calculated before it can be used, and the half-life of the drug is very short, which also limits the application

Method used

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  • New compound having anthracycline antibiotic structure, and preparation method and application thereof
  • New compound having anthracycline antibiotic structure, and preparation method and application thereof
  • New compound having anthracycline antibiotic structure, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] 1) A mixture of 2 g of sebacic acid in 25 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0052] 2) 5 g of compound A, 60 mg of compound B, 200 mg of dicyclohexylcarbodiimide and 10 mg of pyridine were mixed with 30 ml of dichloromethane, stirred at room temperature overnight; then washed with ether and dried under vacuum to obtain a polymer;

[0053] 3) Mix the products of step 1) and step 2) into a flask, and react at 150°C for 1 hour; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried;

[0054] 4) Put doxorubicin and the polymer of step 3) into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven for 2 hours; minutes; the product was put into 5% cholic acid solution and stirred at 400 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

Embodiment 2

[0056] 1. Mix 2.5g of compound A, 47mg of compound B, 200mg of dicyclohexylcarbodiimide and 8mg of pyridine, add 20ml of dichloromethane, and stir overnight at room temperature;

[0057] It was then washed with ether and dried under vacuum;

[0058] 2. Mix 1 g of acetyl-sebacic acid (commercially available) and the product of step 1 into a flask, and react at 120°C for 1.5 hours; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried to obtain a polymer thing;

[0059] 3 Put pirarubicin and the polymer into a solution mixed with 5ml of methanol and 5ml of dichloromethane; then put it in an oven for 4 hours; at minus 10-20 degrees, ultrasonic for 20 minutes; put the product in 3% Stir in the cholic acid solution at 400 rpm for 2 hours; collect by centrifugation and freeze-dry to obtain the final product.

Embodiment 3

[0061] A mixture of 2 g of sebacic acid in 20 ml of acetic anhydride was refluxed to form acetyl-sebacic acid;

[0062] 2 Compound A 2.5g, Compound B 42mg, dicyclohexylcarbodiimide 150mg and tetrahydrofuran were mixed with 15ml of chloroform, stirred at room temperature overnight; then washed with ether and dried under vacuum to obtain a polymer;

[0063] 3 Mix the products of step 1 and step 2 into a flask, and react at 150°C for 1 hour; when the polymer is cooled to room temperature, dissolve it in chloroform, wash with petroleum ether and dry;

[0064] 4 Put arubicin and the polymer of step 3 into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven for 8 hours; at minus 20-30 degrees, ultrasonic for 20 minutes The product was put into 5% cholic acid solution and stirred at 400 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

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Abstract

The invention discloses a new compound having an anthracycline antibiotic structure, and a preparation method and an application thereof. The anthracycline antibiotic coupled nonlinear multi-block copolymer has better effects on treatment of oculopathy compared with other forms of drugs or medicaments.

Description

technical field [0001] The invention discloses a new compound containing anthracycline antibiotic structure, a preparation method and application of the compound. Background technique [0002] Anthracyclines are antimitotic and extremely cytotoxic drugs. Doxorubicin can successfully inhibit a variety of malignancies, including acute leukemia, lymphoma, soft tissue and osteosarcoma, childhood malignancies, and adult solid tumors. Its mechanism of action is that the drug can penetrate into the cell and bind to the chromosome. The planar loop in the drug structure is inserted between base pairs to form a complex with DNA, which seriously interferes with DNA synthesis, DNA-dependent RNA synthesis, and protein synthesis. However, the concentration of doxorubicin required to produce an antiproliferative effect through this mechanism is higher than the concentration of the drug at the tumor site in clinical treatment. In addition, anthracycline antibiotics are also related to th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C08G63/91C08G63/685A61K47/48A61K31/704A61P27/02
Inventor 张雅珍李铁力白毅
Owner 张雅珍
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