Synthesis of zinc phenanthroline aminopolycarboxylate complex and application of complex in anti-tumor drugs

An aminopolycarboxylic acid, o-phenanthroline technology, applied in antitumor drugs, zinc organic compounds, drug combinations, etc. Problems such as drug resistance and poor water solubility of drugs are generated, and the effects of simple preparation method, small toxic and side effects, and fast precipitation time are achieved.

Inactive Publication Date: 2015-04-29
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, platinum complexes also have many disadvantages: the drug has poor water solubility; it can only be administered by injection, and the remission period is short, accompanied by severe nephrot...

Method used

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  • Synthesis of zinc phenanthroline aminopolycarboxylate complex and application of complex in anti-tumor drugs
  • Synthesis of zinc phenanthroline aminopolycarboxylate complex and application of complex in anti-tumor drugs
  • Synthesis of zinc phenanthroline aminopolycarboxylate complex and application of complex in anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Add 1.5mmol o-phenanthroline, 2.5mmol iminodiacetic acid, and 2.5mmol zinc nitrate to a 50mL round-bottomed flask in sequence, stir and react at 80°C for 0.5h, and adjust the pH value to 4.0; filter, and place the filtrate in In a beaker, naturally volatilize to obtain the zinc complex of o-phenanthroline iminodiacetic acid ( Zn-ida complex ) as white crystals, the compound yield was 61%.

[0020] The product is analyzed by infrared spectroscopy, and the structure is as follows: IR (KBr, cm -1 ): V as (CO 2 ) 1625 vs, 1597 vs , 1518 m; V s (CO 2 ) 1426 m, 1387 s, 1297 m

[0021] The product was analyzed by elements, and the data are as follows: Experimental value (%): C, 47.30; H, 3.90; N, 12.33. Calculated value (%): C, 47.26; H, 3.87; N, 12.40.

Embodiment 2

[0022] Example 2: Add 1.0mmol o-phenanthroline, 1.5mmol iminodiacetic acid, and 1.0mmol zinc chloride successively to a 50mL round-bottomed flask, stir and react at 80°C for 1.0h, and adjust the pH value to 4.0; filter, and place the filtrate in into a beaker, naturally volatilized to obtain white crystals, and the compound yield was 56%.

Embodiment 3

[0023] Example 3: Add 2.0mmol o-phenanthroline, 1.5mmol iminodiacetic acid, and 1.5mmol zinc sulfate to a 50mL round bottom flask in sequence, stir and react at 80°C for 1.5h, and adjust the pH value to 2.0; filter, and place the filtrate in In the beaker, white crystals were obtained by natural volatilization, and the compound yield was 55%.

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Abstract

The invention discloses a zinc phenanthroline aminopolycarboxylate complex as well as a preparation method and an application thereof in anti-tumor drugs, and belongs to the field of an anti-tumor technology. The zinc phenanthroline aminopolycarboxylate complex disclosed by the invention is prepared by mixing, heating and reacting zinc salt, aminopolycarboxylic acid and phenanthroline in an aqueous phase. The complex is relatively strong in anti-tumor activity, and can be used as a raw material for preparing liver cancer and breast cancer treating drugs; compared with platinum-based anti-tumor drugs which are commonly used at present, the complex disclosed by the invention has the characteristics of high anti-tumor activity, low toxic and side effects, short crystallization and separation time, good water solubility, high purity, low raw material cost, simple preparation method and the like.

Description

technical field [0001] The invention relates to the technical field of anti-cancer, in particular to an amino polycarboxylic acid o-phenanthroline zinc complex for anti-cancer. Background technique [0002] In today's society, malignant tumors with a high fatality rate have become the number one killer threatening human life and health. Therefore, countries all over the world attach great importance to cancer prevention and treatment. At present, chemotherapy, surgery, and radiation therapy are commonly used to treat tumors clinically. However, due to the serious side effects, tumor drug resistance, and incomplete surgical treatment of chemotherapy drugs, the development of high-efficiency, low-toxicity, and broad-spectrum , highly selective anticancer drugs have become a long-term strategic goal. [0003] In 1969, American chemist Rosenberg first discovered that cisplatin (cisplatin) has anti-tumor activity, and then in 1979, the US Food and Drug Administration (FDA) appro...

Claims

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Application Information

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IPC IPC(8): C07F3/06A61K31/555A61P35/00
CPCC07F3/06
Inventor 倪鲁彬刁国旺孙云王娟刘畅
Owner YANGZHOU UNIV
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