Fat soluble dual-core cobalt (III) anti-tumor coordination compound and preparation method thereof

A complex and fat-soluble technology, which is applied in the preparation of hydrazone, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of severe toxicity and side effects, and achieve the effect of simple chemical reaction process and good anti-tumor activity

Inactive Publication Date: 2010-11-17
YUNNAN UNIV
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Problems solved by technology

However, platinum-based anticancer drugs have relatively large toxic and side effects, and cancer patients receiving treatment usually have severe toxic and side effects such as bone marrow suppression, such as thrombocytopenia, nausea and vomiting, kidney and nerve damage, so research on non-platinum-based complexes with less toxicity is still necessary. It is one of the main directions of anticancer drug research

Method used

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  • Fat soluble dual-core cobalt (III) anti-tumor coordination compound and preparation method thereof
  • Fat soluble dual-core cobalt (III) anti-tumor coordination compound and preparation method thereof
  • Fat soluble dual-core cobalt (III) anti-tumor coordination compound and preparation method thereof

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Embodiment Construction

[0025] (-) The preparation of complex N of the present invention, N'-disalicylaldehyde diamine and cobalt (III)

[0026] (1) Synthesis of ligand N, N'-salicylaldehyde diamine

[0027] The synthetic reference document [B.Sreenivasulu, J.J.Vittal, [J].Angew.Chem.Int.Ed., 2004,43:5769-5772] of N,N'-salicylaldehyde diamine of the present invention: Hydrazine 50mmol (2.5g), slowly dropwise added 20mL salicylaldehyde 50mmol (6.1g) in anhydrous methanol solution, stirring while adding, the solution turned yellow. Afterwards, after sufficient reaction at room temperature, a large amount of yellow precipitate was obtained, which was filtered by suction and recrystallized from THF (tetrahydrofuran) to obtain 12 g of a yellow solid of N,N'-salicylaldehyde diamine, which was vacuum-dried for later use.

[0028] N, N'-salicylaldehyde diamine yield: 85%. The characteristic structural parameters are: elemental analysis (%): theoretical value: C, 69.99; H, 5.03; N, 11.66; experimental value...

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Abstract

The invention discloses a fat soluble dual-core cobalt (III) anti-tumor coordination compound and a preparation method thereof. The fat soluble dual-core cobalt (III) anti-tumor coordination compound belongs to lipophilic cobalt anti-tumor coordination compounds. The coordination compound of the invention has a chemical name of N,N'-bis(salicylidene)diamine cobalt (III) ([Co2(C14H12N2O2)3] for short), a molecular formula of C42H33Co2N6O6 and a molecular weight FW of 834.63, and is prepared by using CoAc2.4H2O as a raw material and by the steps of performing a quantitative reaction of the CoAc2.4H2O and ligand N,N'-bis(salicylidene)diamine in a solvent of dimethyl formamide and separating out products. The anti-tumor activity of the coordination compound is 1.6 times that of cis-platinum and 5 times that of carboplatin; an anti-tumor G150 value is 0.35mu g / mL; the activity is higher than those of the cis-platinum and carboplatin; and the coordination compound is low in toxicity and high in fat solubility and is used for clinical tumor treatment.

Description

technical field [0001] The invention belongs to lipophilic cobalt anti-tumor complexes. Background technique [0002] Chemotherapy is currently one of the three major methods for humans to deal with cancer, and it is widely used clinically. The main drugs of chemotherapy are all cytotoxic compounds, which lack selectivity and specificity to cancer cells. While killing cancer cells, they also greatly damage normal tissue cells and cause serious side effects [Edited by Han Rui. Tumor Chemoprevention And Drug Treatment. Beijing Medical University, China Union Medical University Press. Beijing, 1991]. Chemotherapy is based on chemotherapeutic drugs, and countries all over the world invest a lot of manpower, material and financial resources in the research of anticancer drugs every year. [0003] Cobalt is an essential trace element in the human body, and exists in the form of complexes in living organisms. Because it can be used as an excellent probe ion to replace Zn(II), Mn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C251/88C07C249/16A61K31/295A61P35/00
Inventor 谢明进赵琦华陈红雁金毅
Owner YUNNAN UNIV
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