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Benzimidazole zinc complex and preparation method thereof

A technology of zinc benzimidazole and benzimidazole, which is applied in the field of metal complex antitumor drugs, can solve the problems of being difficult to meet the clinical needs of the treatment of esophageal cancer, prone to drug resistance, and many adverse reactions, and achieves the inhibition of esophageal cancer cells. Growth, good esophageal cancer cell growth inhibitory activity, easy post-treatment effect

Inactive Publication Date: 2014-09-24
ZHANJIANG NORMAL UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, platinum complexes such as cisplatin have the disadvantages of low selectivity, many adverse reactions, and easy drug resistance, which have been difficult to meet the clinical needs of esophageal cancer treatment.

Method used

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  • Benzimidazole zinc complex and preparation method thereof
  • Benzimidazole zinc complex and preparation method thereof
  • Benzimidazole zinc complex and preparation method thereof

Examples

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Effect test

Embodiment 1

[0025] (1) Ligand 2-(2-(1H-benzimidazole-2-)benzyl)-1H-benzimidazole synthesis method

[0026] 2-(Carboxymethyl)benzoic acid (1.80g, 0.010mol) and o-phenylenediamine (2.16g, 0.020mmol) were mixed in phosphoric acid (20mL), heated at 180°C for 3 hours, and the reactant was cooled to room temperature, then Distilled water was added and a yellow solid was obtained after neutralization with ammonia water. Washed 3 times with distilled water, then filtered, and recrystallized from ethanol to obtain yellow-green solid 2-(2-(1H-benzimidazole-2-)benzyl)-1H-benzimidazole, the yield was 2.16g, and the yield was 62.4 %.

[0027] Elemental Analysis: C 21 h 20 N 4 o 2 (bbb·CH 3 CH 2 OH·H 2 O), the theoretically calculated value is C, 71.11%; H, 6.23%; N, 14.42%, the experimental value is C, 71.48%; H, 6.I1%; N, 14.33%; Infrared spectrum: IR (KBr, cm -1 ): 3406, 3058, 1627, 1534, 1437, 1379, 1310, 1271, 1155, 839, 799, 724; Proton NMR spectrum: 1 HNMR: (300MHz, CDCl 3 ):1.26(m, ...

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Abstract

The invention relates to a benzimidazole zinc complex and a preparation method thereof. A chemical name of the benzimidazole zinc complex is dichloro-2-(2-(1H-benzimidazole-2-)benzyl)-1H-benzimidazole zinc complex. The preparation method includes following steps: mixing 2-(carboxymethyl)benzoic acid with o-phenylenediamine, placing the mixture in phosphoric acid, performing a heating process at 180 DEG C for 3 hours to obtain a purple-green reactant, cooling the reactant to room temperature, adding distilled water, performing a neutralization reaction to obtain a yellow-green solid, performing a washing process through distilled water for three times, carrying out a filtering process, carrying out a recrystallization process through alcohol to obtain a yellow-green solid 2-(2-(1H-benzimidazole-2-)benzyl)-1H-benzimidazole, namely a ligand, dissolving ZnCl2 and the ligand 2-(2-(1H-benzimidazole-2-)benzyl)-1H-benzimidazole in a proper amount of a DMF solvent to obtain a mixture, stirring the mixture uniformly at room temperature, performing a volatilization process for seven days to obtain a slight yellow-green block-shaped complex monocrystal. The complex employs biological non-toxic element zinc as a metal ion, can be used for preparing antitumor drugs, can inhibit generation of esophagus cancer cells, and is free from remaining in human body and causing poisoning in human body due to metal accumulation. The complex is simple in the preparation method, is high in yield, is low in cost and is suitable for an industrial production.

Description

technical field [0001] The invention relates to a complex and a preparation method thereof, in particular to a benzimidazole zinc complex with antitumor effect and a preparation method thereof, belonging to the technical field of metal complex antitumor drugs. Background technique [0002] Esophageal cancer is a malignant tumor occurring in the esophageal epithelium, which seriously threatens human health. Esophageal cancer is the fourth most deadly tumor in my country, accounting for 5.5% of the death toll (Chen Wanqing, Zhang Siwei, Zheng Rongshou et al. China Oncology, 2011, 03: 162-9). Since most patients in the early stage have no obvious symptoms, more than 95% of the first clinically diagnosed esophageal cancer patients are in the middle and advanced stages. At present, chemotherapy is the main and most effective method for the treatment of advanced esophageal cancer. [0003] At the end of the 20th century, research on inorganic drugs has become a worldwide hotspot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F3/06A61P35/00A61P3/02
Inventor 刘生桂李国璧苏文义
Owner ZHANJIANG NORMAL UNIV
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