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Modification method of antitumor drug

An anti-tumor drug and modification technology, which is applied in the field of organic polymer synthesis and drug preparation, and the field of organic synthesis modified anti-tumor drugs, can solve the problems of complicated drug carrier modification process, easy destruction of drug structure, and reduced drug efficacy. , to achieve the effect of helping dissolution and transportation, avoiding toxic and side effects, and improving solubility

Active Publication Date: 2018-12-18
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method also has some obvious disadvantages
For example: the drug-loaded carrier has potential risks of toxic and side effects, the modification process of the drug carrier is cumbersome, and the drug structure is easily destroyed during operation, resulting in a decrease in drug efficacy

Method used

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  • Modification method of antitumor drug
  • Modification method of antitumor drug
  • Modification method of antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0026] Mitoxantrone is a new type of drug for treating tumors. Compared with traditional anticancer drugs, its antitumor activity is equivalent to or slightly higher than that of doxorubicin, and significantly higher than that of cyclophosphamide, fluorouracil and other drugs. For malignant lymphoma The treatment of breast cancer, acute leukemia, lung cancer and other diseases has a good therapeutic effect. At the same time, because mitoxantrone has no amino sugar structure, does not generate free radicals, and has the effect of inhibiting lipid peroxidation, it is less toxic to the heart. These advantages make mitoxantrone a new drug with great development potential for treating tumors.

[0027] (1) Functionalized Mitoxantrone

[0028] Dissolve 88.2 mg of RAFT agent (4-cyano-4-ethyltrithiovaleric acid) and 50 mg of mitoxantrone in 5 mL and 3 mL of N,N-dimethyldiamide, respectively, and dissolve 42.8 mg of bicyclo Hexylcarbodiimide (DCC) and 3.3mg 4-dimethylaminopyridine (DM...

Embodiment 1-2～1-4

[0032] Same as Example 1-1, just change the molar ratio (i.e. feed ratio) of functionalized mitoxantrone and monomer PEG-A in step (2), respectively 1:50, 1:75, 1:150 .

[0033] Table 1 The relationship between feed ratio and degree of polymerization

[0034] Feeding ratio

Embodiment 2-1

[0036] Hydroxytyrosol has a variety of biological and pharmacological activities, has a safe and excellent antioxidant effect, and can be used for anti-cancer and anti-cancer.

[0037] (1) Functionalized hydroxytyrosol

[0038] Dissolve 6.4 mg of RAFT reagent (4-cyano-4-ethyltrithiovaleric acid) and 25 mg of hydroxytyrosol in 5 mL and 3 mL of N,N-dimethyldiamide, respectively, and dissolve 61.8 mg of dicyclohexyl Carbodiimide (DCC) and 4.76mg 4-dimethylaminopyridine (DMAP) were dissolved in 5mL N,N-dimethyldiamide, and the three solutions were mixed uniformly in a round bottom flask, and the resulting mixed solution was dissolved at 30 The reaction was stirred at ℃ for 24 hours, then 5 mL of tetrahydrofuran was added, and dried by rotary evaporation at 85 ℃. The obtained solid was chromatographically separated on a silica gel column (dichloromethane: ethyl acetate = 1:12 as the eluent) to obtain functionalized Hydroxytyrosol, and the solvent was removed by rotary evaporation ...

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Abstract

The invention belongs to the field of organic macromolecular synthesis and drug preparation, in particular to a modification method and product of an antitumor drug with alcoholic hydroxyl group. An RAFT reagent with carboxyl is used for esterified modification to obtain a functional drug, then PEG-A molecules are polymerized onto the functional drug by adopting an RAFT polymerization method, so that the modification of the antitumor drug can be realized; the hydrophilic performance can be greatly improved, and the dissolution and transportation of the drug in the water can be facilitated; andmeanwhile, the functional drug enters the human body after being subjectedto polymerizationed modificationed, under the enzyme catalytic effect, the RAFT reagent and the PEG-A can be degraded and reduced to active drug to play the curative effect, the drug effect can be completely reserved, and the toxicity and side effects of the drug can be avoided.

Description

technical field [0001] The invention belongs to the field of organic polymer synthesis and drug preparation, in particular to the field of organic synthesis modified antitumor drugs, specifically a method for modifying antitumor drugs with alcoholic hydroxyl groups by esterification reaction and RAFT polymerization reaction. Background technique [0002] In recent years, many new drugs that can be used to treat stubborn diseases have been discovered and have been applied in clinical trials. These drugs not only have higher anticancer properties than traditional drugs, but also have lower cytotoxicity, such as mitoxantrone, Hydroxytyrosol has become a new type of tumor treatment drug with great development potential. However, despite their good efficacy, antitumor drugs such as mitoxantrone and hydroxytyrosol have extremely low water solubility, which seriously affects the dosage and absorption efficiency of the drug. Therefore, finding a simple and biocompatible method for ...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K31/136A61K31/05A61P35/00
CPCA61K31/05A61K31/136A61K47/60A61P35/00
Inventor 刘敬权王慧宁陈涛
Owner QINGDAO UNIV
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