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Long-life fluorescein derivative with hypoxia targeting function, synthesis method of derivative and biological application of derivative

A derivative and long-life technology, applied in the field of fluorescein derivatives, can solve the problems of high tumor recurrence rate, systemic side effects, damage to normal tissues, etc., and achieve the effect of wide application prospects

Inactive Publication Date: 2018-04-24
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Compared with traditional cancer treatment methods, surgical resection of tumors is often accompanied by a higher recurrence rate, radiation therapy is limited by radiation dose and damage to normal tissues, and chemotherapy can easily induce systemic side effects

Method used

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  • Long-life fluorescein derivative with hypoxia targeting function, synthesis method of derivative and biological application of derivative
  • Long-life fluorescein derivative with hypoxia targeting function, synthesis method of derivative and biological application of derivative
  • Long-life fluorescein derivative with hypoxia targeting function, synthesis method of derivative and biological application of derivative

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthetic route to long-lived fluorescein derivative N2 with hypoxia targeting:

[0039]

[0040] (1) Synthesis of Intermediate III

[0041] Under normal temperature transformation, Ⅱ (1.0g, 2.5mmol) and urotropine (1.752g, 12.5mmol) were dissolved in a 25mL trifluoroacetic acid round bottom flask. Heated to 90°C and refluxed for 24 hours. After the mixture became viscous, 2M hydrochloric acid aqueous solution was added, and the solid was precipitated after cooling in the refrigerator. The filter cake was suction-filtered in a Buchner funnel to obtain compound III, which was washed three times with water and dried to obtain an orange-red solid. The next reaction was carried out directly without purification.

[0042] (2) Synthesis of intermediate DCF-MPYM

[0043] In a nitrogen atmosphere, compound III (0.456g, 1mmol) was dissolved in 15mL of absolute ethanol as a solvent, and R 1(0.688g, 4mmol) intermediate, the mixture was stirred uniformly, piperidine (0.4mL) w...

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Abstract

The invention discloses a long-life fluorescein derivative with a hypoxia targeting function as shown in a structural formula I, a synthesis method of the derivative and a biological application of the derivative. In the formula, L is -CH2-O-CH2-, CO-O-CO- or -COO-CH2-, and R is a symmetric C10H8N2O, C8H8O or C6H6OS structure. The long-life fluorescein derivative I can be used for detecting nitroreductase (NTR) in hypoxic tumor tissues. With long triplet-state life, the derivative I can produce a singlet state for photodynamic therapy of hypoxic tumors. The fluorescein derivative based on traditional stains has integrated diagnosis and treatment effects and has the potential of playing a role in biological application.

Description

technical field [0001] The present invention relates to a class of long-lived fluorescein derivatives with hypoxia targeting, its preparation method and biological application. The compound has a longer lifespan and better ability to generate singlet oxygen, and can be used as an excellent photosensitizer Targeted and photodynamic therapy for tumors. Background technique [0002] Cancer has become one of the major diseases that threaten human life and health. How to effectively detect and treat cancer is an important topic that has been concerned all over the world. The tumor microenvironment is often used as a tumor detection target because it has characteristics significantly different from normal tissues. The so-called tumor microenvironment refers to the unique physiological environment caused by the rapid reproduction of tumors during the growth process. In the tumor microenvironment, hypoxia is an important physiological feature. The hypoxic microenvironment of the ...

Claims

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Application Information

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IPC IPC(8): C07D407/14C09K11/06A61K41/00A61P35/00
CPCA61K41/0057C07D407/14C09K11/06C09K2211/1007C09K2211/1088
Inventor 宋锋玲刘致玮彭孝军
Owner DALIAN UNIV OF TECH
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