A kind of radiotherapy-sensitized antitumor drug and preparation method thereof

A technology of anti-tumor drugs and rare earth complexes, which is applied in the direction of anti-tumor drugs, drug combinations, and pharmaceutical formulations, and can solve the problem of few rare earth complexes, and achieve the effects of low raw material cost, good application prospects, and simple and convenient preparation process

Active Publication Date: 2020-09-04
JINAN UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

据文献检索发现,稀土配合物还应用于开发发光材料(如专利WO2018047951、RU2645513、CN107619661、CN107384369、CN107903279)、催化剂(如专利CN107474063、CN107417510、CN107376891、CN107312026、CN107286280)、造影剂(如专利WO2016058066、 WO2016058066), etc., but there are few patents on the anti-tumor activity of rare earth complexes

Method used

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  • A kind of radiotherapy-sensitized antitumor drug and preparation method thereof
  • A kind of radiotherapy-sensitized antitumor drug and preparation method thereof
  • A kind of radiotherapy-sensitized antitumor drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Dy(Hpbc) 2 Preparation of Cl

[0041] 2‐(pyridine‐2‐yl)‐1H‐benzo[d]imidazole‐6‐carboxylic acid (abbreviated as H 2 pbc), DyCl 3 , dissolved in a mixed solution of water and acetonitrile, stirred with a magnetic stirrer in the air, and then transferred to a polytetrafluoroethylene-lined hydrothermal reaction vessel, heated to 170°C and maintained for 48 hours, and then slowly cooled to room temperature. Filtration and washing gave large light yellow blocky crystals. Through elemental analysis, it can be seen that the synthesized crystal material contains a molecule of crystal water, and the molecular formula can be abbreviated as Dy(Hpbc) 2 Cl.H 2 O. (The elemental analysis data are as follows: Found: C, 44.17; H, 2.86; N, 11.67.Calc.for Dy(Hpbc) 2 Cl.H 2 O: C, 43.96; H, 2.84; N, 11.83).

Embodiment 2

[0042] Example 2 Gd(Hpbc) 2 Preparation of Cl

[0043] 2-(pyridin-2-yl)-1H-benzo[d]imidazole-6-carboxylic acid (abbreviated as H 2 pbc), GdCl 3 , dissolved in a mixed solution of water and acetonitrile, stirred with a magnetic stirrer in the air, and then transferred to a polytetrafluoroethylene-lined hydrothermal reaction vessel, heated to 170°C and maintained for 48 hours, and then slowly cooled to room temperature. Filtration and washing gave large light yellow blocky crystals. Through elemental analysis, it can be seen that the synthesized crystal material contains four molecules of crystal water, and the molecular formula can be abbreviated as Gd(Hpbc) 2 Cl.4H 2 O. (The elemental analysis data are as follows: Found: C, 42.62; H, 2.93; N, 11.30.Calc.for Gd(Hpbc) 2 Cl.4H 2 O: C, 42.13; H, 3.26; N, 11.34).

Embodiment 3

[0044] Example 3 Eu(Hpbc) 2 Preparation of Cl

[0045] 2-(pyridin-2-yl)-1H-benzo[d]imidazole-6-carboxylic acid (abbreviated as H 2 pbc), EuCl 3 , dissolved in a mixed solution of water and acetonitrile, stirred with a magnetic stirrer in the air, and then transferred to a polytetrafluoroethylene-lined hydrothermal reaction vessel, heated to 170°C and maintained for 48 hours, and then slowly cooled to room temperature. Filtration and washing gave large light yellow blocky crystals. Through elemental analysis, it can be seen that the synthesized crystal material contains a molecule of crystal water, and the molecular formula can be abbreviated as Eu(Hpbc) 2 Cl.H 2 O. (Found: C, 45.93; H, 3.18; N, 12.26. Calc. for Eu (Hpbc) 2 Cl.H 2 O: C, 45.80; H, 2.66; N, 12.33).

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Abstract

The invention discloses radiotherapy-sensitized anti-tumor drugs and a preparation method thereof. The anti-tumor drugs are nano-scale rare earth complexes, and are low-toxic or non-toxic; the molecular formula of the rare earth complexes is Dy(Hpbc)2Cl, Gd(Hpbc)2Cl and Eu(Hpbc)2Cl. The preparation method comprises the steps of dissolving 2-(pyridine-2-yl)-1H-benzo[d]imidazole-6-carboxylic acid and LnCl3 in a mixed solution of water and acetonitrile, uniformly stirring the obtained mixed solution in the air, carrying out a hydrothermal reaction, cooling to the room temperature, filtering, washing, performing vacuum drying, and grinding into powder; dispersing the obtained powder into an organic solvent, carrying out ultrasonic treatment, centrifuging to remove the precipitate, and then centrifuging again to obtain the radiotherapy-sensitized antitumor drugs. The radiotherapy-sensitized anti-tumor drugs can be induced by X-ray so as to generate singlet oxygen, can be used for imaging while resisting tumors, and can be applied in the aspects such as light, electricity, magnetism and biology; the preparation method is simple in process, easy to operate, large in quantity of sample preparation, short in time consumption and good in reproducibility.

Description

technical field [0001] The invention relates to a class of new anti-tumor drugs, in particular to providing a new anti-tumor drug with radiotherapy sensitization and magnetic imaging, and belongs to the field of biotherapeutic drugs. Background technique [0002] According to the "Global Cancer Report 2014" issued by the World Health Organization, in 2012, the number of cancer patients and deaths worldwide increased to about 14 million, and nearly half of the new cancer cases occurred in Asia, most of which were in China. In 2012, the number of cancer cases in China was 3.065 million, accounting for about one-fifth of the global incidence; the number of cancer deaths was 2.205 million, accounting for about one-quarter of the global cancer deaths. The World Health Organization predicts that in the next hundred years, cancer will continue to rank first in the list of human killers. [0003] At present, metal complexes have been widely used as antitumor drugs in the treatment ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F5/00C09K11/06C08G83/00A61K31/555A61K41/00A61P35/00H01F1/42
CPCA61K31/80A61K41/0038A61P35/00C07B2200/13C07F5/003C08G83/008C09K11/06C09K2211/182H01F1/42
Inventor 陈填烽马丽黄小婷陈鸿达
Owner JINAN UNIVERSITY
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