Bladder cancer cell inhibitor and preparation method thereof

A technology of bladder cancer cells and inhibitors, applied in chemical instruments and methods, platinum group organic compounds, organic chemistry, etc., can solve problems such as severe adverse reactions, low immunity, and serious physical damage, and achieve enhanced cell transmembrane ability , stable molecular structure, strong anti-tumor activity

Inactive Publication Date: 2017-05-10
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drugs usually used in radiotherapy and chemotherapy are mostly chemical drugs. Although they can control the development of some cancer cells and relieve symptoms, they are harmful to the body due to the large toxic and side effects of chemotherapy drugs. The reaction is large, and the cost of treatment is expensive at the same time. 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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  • Bladder cancer cell inhibitor and preparation method thereof
  • Bladder cancer cell inhibitor and preparation method thereof
  • Bladder cancer cell inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1. The preparation method of the present invention:

[0043] (1) Preparation of compound 2: Weigh 1 mol of o-phenanthroline-5,6-dione (compound 1) and 1 mol of 4-methoxybenzaldehyde, add 1000 mL of ethanol, and heat to 80°C to make the o-phenanthrene Rholine-5,6-dione was dissolved, then 3850g of ammonium acetate was added in batches, heated to reflux in a water bath at 80℃ for 4h, and cooled to room temperature; under ice bath conditions, stirring, slowly adding concentrated ammonia (25-28%) Until the solution is neutral, a yellow precipitate (compound 2) of 2-[4-(methoxy)-phenyl]imidazo[4,5-f][1,10]-phenanthroline (compound 2) is obtained, and the precipitate is filtered , Ethanol washing, vacuum drying;

[0044] (2) Preparation of complex 3: Prepare potassium chloroplatinate solution in advance, add 0.8 mL of water to 2.4 mmol potassium chloroplatinate, heat to dissolve at 60°C, add 2 mL of dimethyl sulfoxide, heat and stir at 60°C for 5 min That's it.

[0045] Add 400 m...

Embodiment 2

[0067] 1. The preparation method of the present invention:

[0068] (1) Preparation of compound 2: Weigh 2 mol of o-phenanthroline-5,6-dione (compound 1) and 3 mol of 4-methoxybenzaldehyde, and add 2L Ethanol And 4000g of ammonium acetate, Under 80℃ water bath , Heating to reflux for 4h, and cooling to room temperature; under ice bath conditions, stirring, slowly adding 200 mL of concentrated ammonia (25-28%) to neutrality to obtain a yellow precipitate (compound 2);

[0069] (2) Preparation of complex 3: Prepare a potassium chloroplatinate solution in advance, add 1 mL of water to 2.4 mmol potassium chloroplatinate, heat to dissolve at 50°C, add 3 mL of dimethyl sulfoxide, and heat and stir at 50°C for 10 minutes. can.

[0070] Add 9.6mL to 2.4mmol compound 2 Ethanol , water The bath is heated to 85°C and heated for 20 minutes to dissolve compound 2. The pre-prepared potassium chloroplatinite solution is slowly dropped into the compound 2 solution, and a yellow precipitate is qu...

Embodiment 3

[0086] 1. The preparation method of the present invention:

[0087] (1) Preparation of compound 2: Weigh 2 mol of o-phenanthroline-5,6-dione (compound 1) and 2.5 mol of 4-methoxybenzaldehyde, and add 1.5L of Ethanol , And 3900g of ammonium acetate, Under 85℃ water bath , Heated to reflux 4 h, cooling to room temperature; stirring in an ice bath, slowly adding 180 mL of concentrated ammonia (25-28%) to neutrality to obtain a yellow precipitate (compound 2);

[0088] (2) Preparation of complex 3: Prepare potassium chloroplatinate solution in advance, add 5 mL of water to 2.4 mmol potassium chloroplatinate, heat at 55°C to dissolve, add 2.5 mL of dimethyl sulfoxide, heat at 55°C and stir for 8 min That's it.

[0089] Add 10 mL of 2.4 mmol compound 2 Ethanol , water Heat the bath to 80°C to dissolve compound 2, slowly drop the pre-prepared potassium chloroplatinate solution into the compound 2 solution, and quickly precipitate a yellow precipitate, continue to reflux and stir for 1.5...

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Abstract

The invention discloses a bladder cancer cell inhibitor and a preparation method thereof. The complex dichloro.2.[4.(methoxy).phenyl]imidazo[4, 5.f][1, 10].phenanthroline.R, R.platinum cyclohexanediamine (II) has chirality. With 1,10-phenanthroline.5,6.dione and 4.methoxybenzaldehyde as raw materials, 2.[4.(methoxy).phenyl]imidazo[4, 5.f][1, 10].phenanthroline is prepared; potassium chloroplatinite is added to prepare 2.[4.(methoxy).phenyl]imidazo[4, 5.f][1, 10].phenanthroline.dichloro platinum (II); and finally, cyclohexanediamine is added to obtain the product bladder cancer cell inhibitor. The complex has excellent anti-tumor activity and can be applied to the drugs against bladder cancer and human large-cell lung cancer cells.

Description

Technical field [0001] The invention relates to the technical field of anticancer drugs, in particular to a bladder cancer cell inhibitor and a preparation method. Background technique [0002] Bladder cancer is a malignant tumor that occurs on the bladder mucosa. It is the most common malignant tumor in the urinary system and one of the ten most common tumors in the whole body. It accounts for the first place in the incidence of urogenital tumors in my country. Bladder cancer can occur at any age, even in children, and its incidence increases with age, with a high incidence of 50 to 70 years old. The incidence of bladder cancer in men is 3 to 4 times that of women. [0003] There are many treatment methods for bladder cancer, mainly surgical treatment, among which radiotherapy, chemotherapy and biological treatment play an auxiliary role. Bladder cancer has the characteristics of easy recurrence and invasion. However, most of the drugs commonly used in radiotherapy and chemothe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0093
Inventor 罗旭健杨燕黎昌贵
Owner YULIN NORMAL UNIVERSITY
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