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Water-soluble conjugated polymers for photothermal therapy, polymerized monomers, preparation methods and applications thereof

A technology of conjugated polymers and photothermal therapy, which is applied in the field of antitumor drugs, can solve the problems of high biological toxicity and poor water solubility, and achieve the effects of high solubility, mild synthesis conditions and wide absorption range

Active Publication Date: 2022-03-29
SOUTH CHINA UNIV OF TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The biological system is a complex water-soluble environment, and organic photothermal materials containing oil-soluble groups have poor water solubility and high biological toxicity

Method used

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  • Water-soluble conjugated polymers for photothermal therapy, polymerized monomers, preparation methods and applications thereof
  • Water-soluble conjugated polymers for photothermal therapy, polymerized monomers, preparation methods and applications thereof
  • Water-soluble conjugated polymers for photothermal therapy, polymerized monomers, preparation methods and applications thereof

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Embodiment Construction

[0051] The present invention will be further described in detail below with reference to the examples and drawings, but the implementation of the present invention is not limited thereto.

[0052] 1. Preparation of polymerized monomer (HM1)

[0053] (1) Preparation of 2,6-dibromo-4,4-bis(6-bromohexyl)-4H-cyclopenta[2,1-b:3,4-b']dithiophene (1)

[0054] Under an argon atmosphere, 2,6-dibromo-4H-cyclopenta[2,1-b:3,4-b']dithiophene (6.68g, 20mmol), 1,6 -dibromohexane (12.1g, 50mmol), 50% sodium hydroxide aqueous solution (1g / mL deionized water 4mL, 100mmol), tetrabutylammonium iodide (0.74g, 2.0mmol), 100 °C for 24 hours. The reaction was stopped, quenched with water, extracted with dichloromethane and dried with anhydrous magnesium sulfate. After the solution was concentrated, it was purified by silica gel column chromatography with petroleum ether as eluent, and the yield was 89%. 1 H NMR, 13 CNMR, MS and elemental analysis results show that the obtained compound is the tar...

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Abstract

The invention discloses a water-soluble conjugated polymer for photothermal therapy, its polymer monomer, preparation method and application. The chemical structure of the water-soluble conjugated polymer of the present invention is shown in formula (II). The water-soluble conjugated polymer of the present invention has good solubility in aqueous solution, has excellent biocompatibility, can be directly used in photothermal therapy without coating treatment, and is easy to operate; it has a nanometer size and is easy to enter cells; the side chain contains Polar groups, with targeting, can locate intracellular organelles; have excellent photostability and chemical properties, and also have high photothermal conversion efficiency, which can realize photothermal therapy in the first or second near-infrared region, and treat High efficiency and few side effects. The preparation method of the water-soluble conjugated polymer of the present invention has easy-to-obtain raw materials, mild synthesis conditions, simple preparation method, convenient purification, easy realization, and great application prospects.

Description

technical field [0001] The invention belongs to the technical field of antineoplastic drugs, and in particular relates to a water-soluble conjugated polymer for photothermal therapy, a polymerized monomer thereof, a preparation method and an application thereof. Background technique [0002] Cancer is one of the important diseases that threaten human health and life. According to the "World Cancer Report" published by the World Health Organization in 2018, there were 18.1 million new cancer cases (9.5 million men and 8.6 million women) and 9.6 million deaths (5.4 million men and 4.2 million women) in the world in 2018. The burden of cancer has further increased. Among them, China, as a country with a large population, accounts for a large part of the global cancer incidence and death. Therefore, cancer has become one of the major diseases that our country must overcome independently. [0003] Photothermal therapy uses photothermal materials to selectively heat the cancer ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04C09K11/06C08G61/12A61K41/00A61P35/00
CPCC07D495/04C09K11/06C08G61/126C08G61/124A61K41/0052A61P35/00C08G2261/411C08G2261/124C08G2261/3243C08G2261/18C08G2261/594C08G2261/147C08G2261/143C08G2261/1452C08G2261/312C08G2261/3142C08G2261/3162C09K2211/1092C08G61/12A61K31/795C07D519/00A61K47/59
Inventor 应磊胡黎文郭婷彭俊彪曹镛
Owner SOUTH CHINA UNIV OF TECH
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