Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound

A boron compound and drug technology, applied in the field of boron-containing compounds and their preparation, can solve the problems of poor targeting and enrichment ability, and achieve the effects of inhibiting overexpression, good tumor targeting, and inhibiting growth

Active Publication Date: 2019-06-25
童永彭
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The main purpose of the present invention is to provide a boron-containing compound, aiming to improve the probl

Method used

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  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound
  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound
  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound

Examples

Experimental program
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Example Embodiment

[0041] In addition, the present invention also provides a method for preparing a boron-containing compound, which includes the following steps: mix the reactant and boric acid at a molar ratio of 1:15 to 1:10, add dimethyl sulfoxide to form a mixed solution, The synthesis device is heated at 110-150°C for 1.5-2h, the product is centrifuged and filtered, and the precipitate is obtained by recrystallization with ethanol, and dried at 80-90°C to obtain the boron-containing compound of the present invention with general structural formula (I). Among them, the reactant is adenosine di-sodium triphosphate, adenosine diphosphate or adenosine di-sodium monophosphate, and the reactant is preferably adenosine di-sodium triphosphate.

[0042] In addition, the present invention also provides a pharmaceutical composition comprising the above-mentioned boron-containing compound, and a pharmaceutically acceptable carrier, diluent or auxiliary agent.

[0043] Furthermore, the present invention als...

Example Embodiment

[0044] Example 1

[0045] The synthetic route of the boron-containing compound of this embodiment is:

[0046]

[0047] The preparation steps of the boron-containing compound in this embodiment are: mix 100 mg adenosine disodium triphosphate with 100 mg boric acid (the molar ratio is about 1:10), add 2000 μl dimethyl sulfoxide to form a mixed solution, and place it in an organic synthesis device 110-150 The reaction was heated at ℃ for 1.5 hours; the product was centrifuged and filtered, recrystallized with ethanol to obtain a precipitate, and dried at 80 ℃ to obtain the final product: adenosine disodium triphosphate borate, with a total yield of 32%. Among them, adenosine triphosphate disodium was purchased from BBI Life Science Co., Ltd., boric acid was purchased from Tianjin Damao Chemical Reagent Factory, and dimethyl sulfoxide was purchased from BBI Life Science Co., Ltd.

[0048] Infrared detection: Nicolet 6700 Fourier infrared spectrometer was used to detect the infrared spe...

Example Embodiment

[0051] Example 2

[0052] The synthetic route of the boron-containing compound in this example is the same as that in Example 1. The preparation steps of the boron-containing compound in this example are: mix 100 mg adenosine disodium triphosphate with 120 mg boric acid, add 2200 μl dimethyl sulfoxide to form a mixed solution, In the organic synthesis device, the reaction was heated at 110-150°C for 2 hours; the product was centrifuged and filtered, recrystallized with ethanol to obtain a precipitate, and dried at 90°C to obtain the final product: adenosine triphosphate disodium borate. Among them, adenosine triphosphate disodium was purchased from BBI Life Science Co., Ltd., boric acid was purchased from Tianjin Damao Chemical Reagent Factory, and dimethyl sulfoxide was purchased from BBI Life Science Co., Ltd. Using the same infrared detection, nuclear magnetic detection and mass spectrometry detection as in Example 1, the comprehensive analysis results show that the synthesize...

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Abstract

The invention discloses a boron-containing compound, a pharmaceutical composition and a preparation method and application of the boron-containing compound. The boron-containing compound has a generalstructural formula (I), and nucleotide substances serve as small molecules required by DNA synthesis and are easily taken up by rapidly proliferating tumor cells in a large amount, so that 10B atomscombined with the nucleotide substances enter the nucleus of tumor cells together, and the boron-containing compound can kill tumors more effectively after neutron irradiation. Secondly, the boron agent synthesized by the compound belongs to an epidermal growth factor receptor (EGFR) inhibitor, produces synergistic tumor growth inhibition effect with BNCT, competitively blocks ATP (adenosine triphosphate) and receptor tyrosine kinase domain to inhibit EGFR overexpression effect, prevents DNA repair of tumor cells, and further inhibits growth, migration, differentiation and survival of the tumor cells.

Description

technical field [0001] The invention relates to the field of boron-containing compounds, in particular to a boron-containing compound and its preparation method and application. Background technique [0002] At present, radiotherapy is a routine treatment for tumors, but it has poor effects on some special tumors that grow deep in the body, while Boron Neutron Capture Therapy (BNCT) has a better effect. BNCT is a 10 Unique particle radiation therapy of the B nuclear capture reaction, which in principle has significant advantages over conventional radiation therapy. The therapy mainly utilizes the high neutron capture cross-section 10 Molecules of element B react with neutrons to release particles to treat tumors. After injecting boron into the patient's body, 10 B will be selectively enriched in the tumor site, and the tumor will be irradiated with thermal neutrons, and the neutrons will interact with 10 B undergoes a neutron capture reaction, and the maximum energy of ...

Claims

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Application Information

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IPC IPC(8): C07H1/00C07H19/20A61K41/00A61P35/00
Inventor 童永彭王淼
Owner 童永彭
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