Application of fluoro-thiosemicarbazone compound in antitumor drug

An anti-tumor drug, thiosemicarbazide technology, applied in the field of medicine, can solve the problem of no fluorinated thiosemicarbazide compound, etc.

Inactive Publication Date: 2017-08-08
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The present invention relates to the application of fluorothiosemicarbazide compound (I) in the field of medicine, there is no report of fluorothiosemicarbazide compound (I) provided by the present invention and its medicine as an active ingredient in the prior art, and there is no such Reports on the application of the compound or its pharmaceutical composition in the preparation or treatment of drugs for diseases such as tumors caused by various factors

Method used

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  • Application of fluoro-thiosemicarbazone compound in antitumor drug
  • Application of fluoro-thiosemicarbazone compound in antitumor drug
  • Application of fluoro-thiosemicarbazone compound in antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Study on the Cell Proliferation Activity of 2-(3,4-Difluorobenzylidene) Thiosemicarbazide (I)

[0017] 1. Experimental drugs

[0018] Weigh 1mmol 3,4-difluorobenzaldehyde (3.07g) and 1.1mmol thiosemicarbazide (2.16g) and place in a 200mL reaction flask, add 20mL ethanol (95%) and stir evenly, then add 1mL glacial acetic acid dropwise, and then Reflux and stir at 65-70°C for about 10 hours, evaporate most of the ethanol under reduced pressure, add 20 ml of ice water, filter to obtain a precipitate, wash the precipitate with ice water (20 mL for three times), and recrystallize from ethanol to obtain 2-(3,4-difluorobenzene Methylene) thiosemicarbazide, white solid. 2-(3,4-Difluorobenzylidene)thiosemicarbazide is dissolved in DMSO, and prepared as a 50mg / ml storage solution for long-term storage. The maximum concentration for the experiment is 12.5, 25, and 50μg / ml.

[0019] 2. Cell lines

[0020] Human non-small cell lung cancer cells (A549) were purchased fro...

Embodiment 2

[0025] Example 2 Study on the apoptosis of A549 by 2-(3,4-difluorobenzylidene)thiosemicarbazide (I)

[0026] 1. Experimental cells:

[0027] Same as Example 1

[0028] 2. Experimental drugs:

[0029] Same as Example 1

[0030] 3. Experimental method:

[0031] Apoptosis was detected by AnnexinV / PI staining. Take A549 cells in the logarithmic phase and adjust the cell concentration to 5×10 5 / mL, seeded in a six-well plate, at 37°C, 5% CO 2 Cultivate in an incubator for 24 hours, add different concentrations of compound 2-(3,4-difluorobenzylidene)thiosemicarbazide (I) (5, 10, 20 μg / mL) for 48 hours, and set a blank group (PBS). The cells were digested with EDTA-free trypsin, washed three times with PBS, and collected 1-5×10 5 Add 500 μL of Binding Buffer to suspend the cells to form a cell suspension, then add 5 μL Annexin V-FITC and 5 μL Propidium Iodide, mix well, react at room temperature in the dark for 15 minutes, and perform detection on a flow cytometer.

[0032]...

Embodiment 3

[0033] Example 3 Morphological study on apoptosis of A549 by 2-(3,4-difluorobenzylidene)thiosemicarbazide (I)

[0034] 1. Experimental cells:

[0035] Same as Example 1

[0036] 2. Experimental drugs:

[0037] Same as Example 1

[0038] 3. Experimental method:

[0039] Hoechst staining was used to detect the morphology of apoptosis. Take A549 cells in the logarithmic phase and adjust the cell concentration to 5×10 5 / mL, seeded in a six-well plate, at 37°C, 5% CO 2 After culturing in the incubator for 24 hours, add different concentrations of 2-(3,4-difluorobenzylidene)thiosemicarbazide (I) (5, 10, 20 μg / mL) for 48 hours, and set a blank group (PBS). The cells were washed three times with PBS, fixed with 4% paraformaldehyde at room temperature for 15 min, washed three times with PBS, stained with Hoechst33258 dye in the dark for 15 min, and observed under a fluorescent microscope.

[0040] The results showed that after 2-(3,4-difluorobenzylidene)thiosemicarbazide (I) a...

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PUM

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Abstract

The invention relates to an medicinal application of a fluoro-thiosemicarbazone compound 2-(3,4-difluorobenzylidene)thiosemicarbazide (I). Experiments such as cell proliferation, cell apoptosis, cell period proves that the compound can effectively inhibit the proliferation of tumor cells, can induce the apoptosis of the tumor cells, can influence the period of the tumor cells and has significant antitumor activity. The 2-(3,4-difluorobenzylidene)thiosemicarbazide (I) can be used as a drug active ingredient and can be prepared with a carrier acceptable on pharmacology into an antitumor drug composition. (The formula structure is shown in the description.).

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to 2-(3,4-difluorobenzylidene)thiosemicarbazide compound (I) and its pharmacological activity and pharmaceutical use. The compound can be used for preventing and / or treating diseases such as tumors or cancers caused by various factors. Background technique [0002] Tumor seriously affects people's health and is the second leading cause of human death. According to the statistics of the World Health Organization, more than 10 million cancer patients are newly diagnosed every year in the world, and the total number of cancer deaths worldwide reaches 7 million people every year. In 2012, China had 3.07 million new cancer patients and caused about 2.2 million deaths, accounting for 21.9% and 26.8% of the global total respectively. Cancer has become the leading cause of death among urban and rural residents in my country. Tumors not only seriously threaten the health of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/175A61P35/00
CPCA61K31/175
Inventor 史大永郭传龙王立军赵越江波李祥乾
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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