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Liver tumor cell inhibitor and preparation method thereof

A liver cancer cell and inhibitor technology, applied in chemical instruments and methods, platinum group organic compounds, organic chemistry, etc., can solve the problems of high toxicity and side effects of chemotherapy drugs, failure to achieve the expected effect of treatment, high cost of treatment, etc., to achieve inhibition Significant ability, enhanced cell transmembrane ability, and great application potential

Inactive Publication Date: 2017-04-26
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, the treatment methods for liver cancer include surgery, chemotherapy, radiotherapy, biological therapy, traditional Chinese medicine and other methods. Most of the drugs used in radiotherapy and chemotherapy are chemical drugs, although they can control the development of some cancer cells and relieve symptoms. , but due to the high toxicity and side effects of chemotherapy drugs, great harm to the body, and a series of complications due to low immunity, large adverse reactions, and high treatment costs, quite a few patients cannot tolerate adverse reactions and give up treatment
At the same time, cancer cells exposed to sub-lethal concentrations of chemotherapy drugs often develop drug resistance, and often cross-resistance to other anticancer drugs, so the drug resistance of chemotherapy drugs and the occurrence of cancer cell metastasis often make the treatment unreachable. to the desired effect

Method used

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  • Liver tumor cell inhibitor and preparation method thereof
  • Liver tumor cell inhibitor and preparation method thereof
  • Liver tumor cell inhibitor and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] One, preparation method of the present invention:

[0042](1) Preparation of compound 2: Weigh 2 mol of phenanthroline-5,6-dione (compound 1) and 2 mol of 2-hydroxy-3-methoxybenzaldehyde, add glacial acetic acid 16mL and ammonium acetate 3.1 g, under 120°C oil bath, heat to reflux for 6h, cool to room temperature; under ice bath conditions, stir, slowly add 16mL of concentrated ammonia water (25-28%) to neutrality to obtain 2-[2-(hydroxyl) - yellow precipitate of 3-(methoxy)-phenyl]imidazo[4,5-f][1,10]-phenanthroline (compound 2);

[0043] (2) Preparation of complex 3: Prepare potassium chloroplatinite solution in advance, add 0.8mL water to 2.4mmol potassium chloroplatinite, heat to dissolve at 60°C, add 2mL dimethyl sulfoxide, heat and stir at 60°C for 5min That's it.

[0044] Add 10mL of dimethyl sulfoxide to 2.4mmol of compound 2, heat the oil bath to 140°C to dissolve compound 2, slowly drop the pre-prepared potassium chloroplatinite solution into the compound 2 ...

Embodiment 2

[0066] One, preparation method of the present invention:

[0067] (1) Preparation of compound 2: Weigh 2 mol of phenanthroline-5,6-dione (compound 1) and 4 mol of 2-hydroxy-3-methoxybenzaldehyde, add glacial acetic acid 20mL and ammonium acetate 3.6 g, in an oil bath at 130°C, heat to reflux for 7 hours, and cool to room temperature; in an ice bath, stir, and slowly add 20 mL of concentrated ammonia water (25-28%) dropwise to neutral, and a yellow precipitate (compound 2) is obtained;

[0068] (2) Preparation of complex 3: Prepare potassium chloroplatinite solution in advance, add 1 mL of water to 2.4 mmol potassium chloroplatinite, heat to dissolve at 50 ° C, add 3 mL of dimethyl sulfoxide, heat and stir at 50 ° C for 10 min Can.

[0069] Add 12mL of dimethyl sulfoxide to 2.4mmol of compound 2, heat the oil bath to 150°C to dissolve compound 2, slowly drop the pre-prepared potassium chloroplatinite solution into the compound 2 solution, and a yellow precipitate precipitates ...

Embodiment 3

[0086] One, preparation method of the present invention:

[0087] (1) Preparation of compound 2: Weigh 2 mol of phenanthroline-5,6-dione (compound 1) and 4 mol of 2-hydroxy-4-methoxybenzaldehyde, add glacial acetic acid 18mL and ammonium acetate 3.6 g, in an oil bath at 125°C, heated to reflux for 5h, cooled to room temperature; in an ice bath, stirred, and slowly added 18mL of concentrated ammonia water (25-28%) dropwise until neutral, and a yellow precipitate (compound 2) was obtained;

[0088] (2) Preparation of complex 3: Prepare potassium chloroplatinite solution in advance, add 1 mL of water to 2.4 mmol potassium chloroplatinite, heat to dissolve at 55 ° C, add 2.5 mL of dimethyl sulfoxide, heat and stir at 55 ° C for 8 min That's it.

[0089] Add 11mL of dimethyl sulfoxide to 2.4mmol of compound 2, heat the oil bath to 145°C to dissolve compound 2, slowly drop the pre-prepared potassium chloroplatinite solution into the compound 2 solution, and a yellow precipitate pre...

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Abstract

The invention discloses a liver tumor cell inhibitor and a preparation method thereof. The inhibitor has chirality and is a complex named as dichloro-2-[2-(hydroxyl)-3-(methoxy)-phenyl]imidazo[4,5-f][1,10]-phenanthroline.S,S-cyclohexanediamine platinum (II). The preparation method comprises the following steps: preparing 2-[2-(hydroxyl)-3-(methoxy)-phenyl]imidazo[4,5-f][1,10]-phenanthroline from [1,10]-phenanthroline-5,6-dione and 2-hydroxyl-3-methoxybenzaldehyde; then adding potassium chloroplatinite to prepare 2-[2-(hydroxyl)-3-(methoxy)-phenyl]imidazo[4,5-f][1,10]-phenanthroline.dichloroplatinum (II); and finally adding cyclohexanediamine so as to obtain the liver tumor cell inhibitor. The complex provided by the invention has excellent antineoplastic activity and is applicable to anti-hepatoma drugs.

Description

technical field [0001] The invention relates to the technical field of anticancer drugs, in particular to an inhibitor of liver cancer cells and a preparation method. Background technique [0002] Liver cancer is a malignant tumor of the liver, which can be divided into two categories: primary and secondary. Primary liver malignant tumors originate from the epithelial or mesenchymal tissues of the liver. The former is called primary liver cancer, which is a malignant tumor with a high incidence in my country and is extremely harmful; the latter is called sarcoma. [0003] At present, the treatment methods for liver cancer include surgery, chemotherapy, radiotherapy, biological therapy, traditional Chinese medicine and other methods. Most of the drugs used in radiotherapy and chemotherapy are chemical drugs, although they can control the development of some cancer cells and relieve symptoms. However, due to the high toxicity and side effects of chemotherapy drugs, great harm...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0093
Inventor 杨燕罗旭健黎昌贵
Owner YULIN NORMAL UNIVERSITY
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