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5-fluorouracil copolymer with anti-tumor activity and preparation method of 5-fluorouracil copolymer

An anti-tumor activity, fluorouracil technology, applied in the field of polymer copolymers, can solve problems such as poor water solubility of pentafluorouracil, and achieve the effects of prolonging residence time, promoting inhibitory effect, and enhancing inhibitory effect.

Inactive Publication Date: 2014-08-06
NORTHWEST NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of pentafluorouracil, the selection of co-solvents (absolute ethanol, DMSO, etc.) will cause a variety of toxic and side effects

Method used

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  • 5-fluorouracil copolymer with anti-tumor activity and preparation method of 5-fluorouracil copolymer
  • 5-fluorouracil copolymer with anti-tumor activity and preparation method of 5-fluorouracil copolymer
  • 5-fluorouracil copolymer with anti-tumor activity and preparation method of 5-fluorouracil copolymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] (1) Preparation of pentafluorouracil monomer (a): Weigh 0.18 g (1.2 mmol) of pentafluorouracil and dissolve it in 2ml of DMSO, slowly add 0.12 g (1 mmol) of methacryloyl chloride dropwise at room temperature; After reacting for 24 hours, 0.30 g of anhydrous sodium carbonate was added, and after stirring for 6 hours, the sodium carbonate was removed by filtration, and the filtrate was precipitated with ethyl acetate to obtain a white solid, which was washed with acetone, filtered with suction, and dried in vacuum at 25°C for 12 hours to obtain a single Compound (a) 0.15 g, yield 60%.

[0055] 1 H NMR (400MHz, DMSO): δ 7.41 (s, 1H, Cycle-H), 5.86 (s, 1H, C=C-H), 5.48 (s, 1H, C=C-H), 1.65 (s, 3H, CH 3 ). 13 C NMR (400MHz, D 2 O): δ 171.8, 160.6, 151.7, 141.9, 139.7, 126.9, 110.0, 17.5.

[0056] (2) Preparation of pentafluorouracil polymer: First, dissolve 0.10 g (0.5 mmol, 20%) of monomeric compound (a) and 0.28 g (2 mmol, 80%) of HPMA in 1 ml of DMSO in a Shleck react...

Embodiment 2

[0059] (1) Preparation of pentafluorouracil monomer (a): same as Example 1.

[0060] (2) Preparation of pentafluorouracil polymer: First, dissolve 0.0396 g (0.2 mmol, 10%) of monomeric compound (a) and 0.2488 g (1.8 mmol, 90%) of HPMA in 1 ml of DMSO in a Shleck reaction flask , and then add 0.028 g (10%, wt) of azobisisobutyronitrile (AIBN). At this time, vacuumize and fill with nitrogen for 3 to 5 cycles. After sealing, keep the temperature at about 60°C and react for 24 hours. Precipitate the reaction solution with 10 ml of acetone to obtain a light yellow solid. After filtration, dissolve the precipitate with 1 ml of anhydrous methanol, and centrifuge with an ultrafiltration concentration centrifuge tube with a molecular weight of 3000 to remove small molecules. The liquid after centrifugation was dried to obtain a light yellow solid, which was 0.1106 g of the polymer expressed by the structural formula (1), and the yield was 38.7%.

[0061] Mn=1.49×10 4 , Mw / Mn=1.52. 1...

Embodiment 3

[0063] (1) Preparation of pentafluorouracil monomer (a): same as Example 1.

[0064] (2) Preparation of pentafluorouracil polymer: First, dissolve 0.0793 g (0.4 mmol, 15%) of monomeric compound (a) and 0.3123 g (2.26 mmol, 85%) of HPMA in 1 ml of DMSO in a Shleck reaction flask , and then add 0.039 g (10%, wt) of azobisisobutyronitrile (AIBN). At this time, vacuumize and fill with nitrogen for 3 to 5 cycles. After sealing, keep the temperature at about 60°C and react for 24 hours. Precipitate the reaction solution with 10 ml of acetone to obtain a light yellow solid. After filtration, dissolve the precipitate with 1 ml of anhydrous methanol, and centrifuge with an ultrafiltration concentration centrifuge tube with a molecular weight of 3000 to remove small molecules. The liquid after centrifugation was dried to obtain a light yellow solid, which was 0.1643 g of the polymer expressed by the structural formula (1), and the yield was 40.9%.

[0065] Mn=1.32×10 4 , Mw / Mn=1.41. ...

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Abstract

The invention provides a pentafluorouracil polymer with anti-tumor activity, which is formed by linking pentafluorouracil or pentafluorouracil and sulfadiazine to N-(2-hydroxypropyl)methacrylamide through polymerization High molecular copolymer with good biocompatibility. The polymer copolymer of the present invention connects pentafluorouracil and sulfadiazine with antitumor activity to N-(2-hydroxypropyl) methacrylamide as a tumor-targeting drug carrier, so that its antitumor activity is superimposed, and further It promotes the inhibitory effect of high molecular polymers on tumors, and at the same time greatly prolongs the residence time of anticancer drugs in tumors. Moreover, the polymer carrier HPMA also reduces the toxicity of anticancer drugs and reduces the damage to normal tissues, which provides a new idea for the preparation of new anticancer drugs.

Description

technical field [0001] The present invention relates to two novel polymer copolymers with antitumor activity (one of which also has tumor tendency), N-(2-hydroxypropyl)methacrylamide-pentafluorouracil copolymer and N-(2- The preparation method of hydroxypropyl) methacrylamide-pentafluorouracil-sulfadiazine copolymer, and their application and prospect in the preparation of antitumor drugs. Background technique [0002] Cancer has become one of the main threats to human health, and it is showing an obvious upward trend. Due to the lack of specific drugs to prevent and treat cancer or tumors, cancer has increasingly become the number one cause of human death. The main methods of treating cancer today include radiotherapy, chemotherapy, surgical therapy and gene therapy. Among them, radiotherapy and chemotherapy are extremely important non-surgical treatments, but while killing tumor cells, radiotherapy and chemotherapy also cause serious damage to normal cells in the body. E...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48C08F220/58C08F220/60A61P35/00
Inventor 袁建超苗承萍贾宗栗静宋凤英袁兵年王福州
Owner NORTHWEST NORMAL UNIVERSITY
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