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A kind of jatrorrhizine platinum (ii) complex targeting human bladder cancer and its synthesis method and application

A bladder cancer, jatrorrhizine technology, applied in platinum-based organic compounds, platinum-based organic compounds, drug combinations, etc., can solve problems such as no related reports, achieve high yield, superior in vitro and in vivo antitumor activity and target The effect of tropism, mild reaction conditions

Active Publication Date: 2021-08-27
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There have been no related reports on the synthesis of metal complexes and their mechanism of action using jatrorrhizine derivatives as active ligands of traditional Chinese medicine.

Method used

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  • A kind of jatrorrhizine platinum (ii) complex targeting human bladder cancer and its synthesis method and application
  • A kind of jatrorrhizine platinum (ii) complex targeting human bladder cancer and its synthesis method and application
  • A kind of jatrorrhizine platinum (ii) complex targeting human bladder cancer and its synthesis method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Weigh 1.0 mol of derivative 1, 0.8 mol of potassium iodide and 1.50 mol of lutidine amine in a round-bottomed flask, add 5.0 ml of acetonitrile, the added solvent is just enough to dissolve the solid, and make the reaction more fully. After reacting for 4 hours, the J-TFA ligand was obtained as a yellow solid powder with a yield of 88.9%.

[0037] Add 1.0 mol ligand J-TFA and 1.0 mol dichlorobis(dimethylsulfoxide) platinum(II) into a 100.0 mL round bottom flask, dissolve in 25.0 mL acetonitrile solution, and carry out at 60°C After the coordination reaction for 4.0 h, the product was washed with acetonitrile and dried under vacuum at 45° C. to obtain the yellow target product Pt1. The yield was 93.0%.

[0038] The synthetic route of the jatrorrhizine platinum (II) complex targeting human bladder cancer of the present invention is as follows:

[0039]

Embodiment 2

[0041] The difference from Example 1 is that 1.0mol of ligand J-TFA and 1.0mol of dichlorobis(dimethylsulfoxide)platinum(II) were added to a 100.0mL round-bottomed flask, dissolved in 50.0 In mL acetonitrile solution, the coordination reaction was carried out at 60°C for 4.0h, washed with acetonitrile and then vacuum-dried at 45°C to obtain the yellow target product Pt1. The yield was 85.2%.

Embodiment 3

[0043] The difference from Example 1 is that 1.0mol of ligand J-TFA and 1.0mol of dichlorobis(dimethylsulfoxide)platinum(II) were added to a 100.0mL round bottom flask, dissolved in 5.0 In mL acetonitrile solution, the coordination reaction was carried out at 60°C for 4.0h, washed with acetonitrile and then vacuum-dried at 45°C to obtain the yellow target product Pt1. The yield was 90.0%.

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Abstract

The invention relates to a quatrorrhizine platinum (II) complex targeting human bladder cancer, its synthesis method and the application of the complex in the preparation of antitumor drugs. The synthesis method of the jatrorrhizine platinum (II) complex targeting human bladder cancer comprises the following steps: (1) dissolving jatrorrhizine bromide derivatives, potassium halide and lutidine amine in a solvent, and Reaction at ~90°C to obtain J-TFA ligand (2) Dissolve the J-TFA ligand prepared in step (1) and dichlorobis(dimethylsulfoxide) platinum (II) in acetonitrile solution, and carry out The coordination reaction takes 4 to 6 hours, and the product is washed and dried to obtain the product. In the present invention, the novel jatrorrhizine derivative J-TFA is used as the active ligand for the first time to synthesize its platinum complex, which exhibits superior anti-tumor activity and targeting in vivo and in vitro, has potential medicinal value, and is expected to be used in various Preparation of an antitumor drug. The structural formula of the jatrorrhizine platinum (II) complex targeting human bladder cancer is as follows:

Description

technical field [0001] The invention relates to a platinum-based highly active complex and a synthesis method, in particular to a jatrorrhizine platinum (II) complex targeting human bladder cancer and a synthesis method thereof. The invention also relates to the application of the quatrorrhizine platinum (II) complex targeting human bladder cancer in the preparation of antitumor drugs. Background technique [0002] Malignant tumors are recognized as one of the most serious diseases to human health in the world, second only to cardiovascular diseases. Therefore, strengthening the research and development of tumor drugs and the research of tumor treatment methods is one of the major problems that clinicians and scientists urgently need to solve. In tumor treatment, chemotherapy is one of the important methods of current tumor treatment. Among many chemotherapeutic drugs, platinum complexes are a kind of drugs with strong anti-tumor effect and wide anti-tumor spectrum. Howeve...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 覃其品黄小玲王振凤
Owner YULIN NORMAL UNIVERSITY
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