Tumor targeted nuclide diagnosis and treatment molecular probe, preparation method and application

A molecular probe and targeting technology, applied in the chemical field, can solve problems such as limited tissue penetration, inability to inhibit tumor cell growth, and difficult quantification of fluorescence imaging, and achieve strong tissue penetration and strong targeting in vivo

Active Publication Date: 2021-09-17
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, G1 and G2 fluorescence imaging is not easy to quantify, tissue penetration is limited, and neither G1 nor G2 fluorescent probes can inhibit the growth of tumor cells

Method used

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  • Tumor targeted nuclide diagnosis and treatment molecular probe, preparation method and application
  • Tumor targeted nuclide diagnosis and treatment molecular probe, preparation method and application
  • Tumor targeted nuclide diagnosis and treatment molecular probe, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1: A labeled precursor of a biotin-targeted molecular probe

[0080] This embodiment provides a biotin-targeted molecular probe 18 F-Bim-H 1 The labeled precursor of Bim-H 1 , the labeled precursor Bim-H 1 Has the following structure:

[0081]

Embodiment 2

[0082] Example 2: A method for preparing labeled precursors of biotin-targeted molecular probes

[0083] This example provides the biotin-targeted molecular probe described in Example 1 18 F-Bim-H 1 The labeled precursor of Bim-H 1 The preparation method, described method comprises the steps:

[0084] the CuSO 4 ·5H 2 O (6.3mg, 0.025mmol, 0.5eq), L-ascorbate sodium salt (9.9mg, 0.05mmol, 1eq) and THPTA ligand (THPTA, 10.84mg, 0.025mmol, 0.5eq) were dissolved in H 2 O (200 μL) to obtain a solution; add G to the solution 1 (G 1 The synthesis reference patent of a fluorescent imaging probe and its preparation method and application, application number: 2020112181003) (55.95mg, 0.05mmol, 1eq) and AmBF 3 (2-azidoethyl-N,N-dimethylaminomethyl-trifluoroborate) (29.4mg, 0.15mmol, 3eq) to obtain a mixture; to the mixture was added DMF (dimethylmethylmethane) amide), the solvent ratio of the control mixture is DMF:H 2 After O=5:1, under the protection of nitrogen, stir at 25 °C...

Embodiment 3

[0094] Example 3: A labeled precursor of a biotin-targeted molecular probe

[0095] This embodiment provides a biotin-targeted molecular probe 131 I-RT-H 2 The labeled precursor RT-H 2 , the labeled precursor RT-H 2 Has the following structure:

[0096]

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Abstract

The invention relates to a tumor targeted nuclide diagnosis and treatment molecular probe, a preparation method and application, and belongs to the technical field of chemistry. The preparation method comprises the following steps of: firstly, performing a ring formation reaction on alkynyl of a compound G1 and azide of AmBF3 through a CuAAC reaction to obtain a labeled precursor Bim-H1; and then, successfully synthesizing an NIRF/PET bimodal probe 18F-Bim-H1 through an isotope exchange method, wherein the probe contains radionuclide 18F and has the advantages of easiness in quantification and high tissue penetrating power. According to the preparation method, the ring formation reaction is performed on the alkynyl of the compound G1 and the azide of the AmBF3 through the CuAAC reaction to obtain a labeled precursor RT-H2, and then an NIRF/Cherenkov bimodal probe 131I-RT-H2 is successfully synthesized by selecting Iodogen as an oxidant; the probe can effectively inhibit proliferation of HeLa cells and has a therapeutic effect on tumors.

Description

technical field [0001] The invention relates to a molecular probe for tumor-targeting radionuclide diagnosis and treatment, a preparation method and application, and belongs to the technical field of chemistry. Background technique [0002] Tumors refer to diseases caused by abnormal cell growth caused by various factors in organisms. They are divided into malignant tumors and benign tumors according to their characteristics and harm to the organism. Malignant tumors, also known as cancers, are metastatic and invasive. Cancer is a serious threat to human health. Under the combined effect of aging population, tense life rhythm, bad living habits and air pollution, the incidence of cancer is getting higher and higher, and the age of onset is getting younger and younger. How to achieve early and accurate diagnosis of cancer has become an urgent problem to be solved. [0003] Biotin is a water-soluble vitamin, also known as vitamin H. Biotin can promote the metabolism of fat ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00A61K51/04A61K101/02A61K101/00
CPCA61K49/0002A61K49/0032A61K51/0453Y02P20/55
Inventor 林建国邱玲谢敏浩李珂刘清竹吕高超彭莹
Owner JIANGSU INST OF NUCLEAR MEDICINE
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