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22-nor-stigmasta thiosemicarbazone compound and preparing method and application thereof

A technology of stigmaster thiosemicarbazone and compound, which can be applied in the field of medicine and can solve the problems of high toxicity, limited scope of use and the like

Inactive Publication Date: 2016-08-17
南宁师范大学
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, various types of anti-tumor drugs continue to emerge and have been applied clinically, but the clinically used anti-tumor drugs have greatly limited their scope of use due to their high toxicity to human tissues

Method used

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  • 22-nor-stigmasta thiosemicarbazone compound and preparing method and application thereof
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  • 22-nor-stigmasta thiosemicarbazone compound and preparing method and application thereof

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Embodiment 1

[0025] The present invention provides a kind of 22-nor-stigmasterol thiosemicarbazone compound, and its structural formula is formula (III):

[0026]

[0027] A preparation method of 22-nor-stigmasterol thiosemicarbazone compound, comprising the following steps:

[0028]Step 1. Add 1.206g stigmasterol into 10mL pyridine, after completely dissolving, add 5mL acetic anhydride, stir and react at room temperature for 24h, stop the reaction after the reaction is completed, add 30mL dilute hydrochloric acid with a concentration of 1mol / L, and transfer the product into a separate In the liquid funnel, use 15mL ethyl acetate to continuously extract 3 times (the amount of ethyl acetate is 15mL each time, after adding ethyl acetate for the first time, the solution is layered, and the organic layer is separated after layering, and placed in a conical bottle, then the water layer was extracted with ethyl acetate, after the water layer was extracted, the organic layer was separated, eth...

Embodiment 2

[0043] The present invention provides a kind of 22-nor-stigmasterol thiosemicarbazone compound, and its structural formula is formula (III):

[0044]

[0045] A preparation method of 22-nor-stigmasterol thiosemicarbazone compound, comprising the following steps:

[0046] Step 1. Add 1.206g stigmasterol into 10mL pyridine, after completely dissolving, add 5mL acetic anhydride, stir and react at room temperature for 24h, stop the reaction after the reaction is completed, add 30mL dilute hydrochloric acid with a concentration of 1mol / L, and transfer the product into a separate In the liquid funnel, use 15mL ethyl acetate to continuously extract 3 times (the amount of ethyl acetate is 15mL each time, after adding ethyl acetate for the first time, the solution is layered, and the organic layer is separated after layering, and placed in a conical bottle, then the water layer was extracted with ethyl acetate, after the water layer was extracted, the organic layer was separated, et...

Embodiment 3

[0061] The present invention provides a kind of 22-nor-stigmasterol thiosemicarbazone compound, and its structural formula is formula (III):

[0062]

[0063] A preparation method of 22-nor-stigmasterol thiosemicarbazone compound, comprising the following steps:

[0064] Step 1. Add 1.206g stigmasterol into 10mL pyridine, after completely dissolving, add 5mL acetic anhydride, stir and react at room temperature for 24h, stop the reaction after the reaction is completed, add 30mL dilute hydrochloric acid with a concentration of 1mol / L, and transfer the product into a separate In the liquid funnel, use 15mL ethyl acetate to continuously extract 3 times (the amount of ethyl acetate is 15mL each time, after adding ethyl acetate for the first time, the solution is layered, and the organic layer is separated after layering, and placed in a conical bottle, then the water layer was extracted with ethyl acetate, after the water layer was extracted, the organic layer was separated, et...

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Abstract

The invention discloses a 22-nor-stigmasta thiosemicarbazone compound and a preparing method and application thereof. The structural formula of the 22-nor-stigmasta thiosemicarbazone compound is shown in the description. In vitro cancer cell growth and proliferation activity inhibition tests show that the prepared 22-nor-stigmasta thiosemicarbazone compound has a remarkable inhibition effect on various tumor cell strains such as human nipple thyroid gland cancer cells, human oral cavity epidermoid carcinoma cells and cervical cancer. Meanwhile, the 22-nor-stigmasta thiosemicarbazone compound is free of cytotoxicity on human kidney epithelial cells (HEK293T) and can be used for preparing medicine for treating cancer.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, the present invention relates to a 22-nor-stigmasteryl thiosemicarbazone compound and its preparation method and application. Background technique [0002] Cancer is a major disease that endangers human health. Overcoming malignant tumors is a difficult problem in modern medicine, and it is also the biggest challenge for the pharmaceutical industry today. At present, various types of anti-tumor drugs are continuously emerging and used clinically, but the anti-tumor drugs used in clinical practice are highly toxic to human tissues, which greatly limits their scope of use. Therefore, finding anticancer drugs with high efficiency, high selectivity and small side effects is the main direction of anticancer drug development. [0003] Among the antineoplastic drugs, Finasteride is currently clinically used to treat benign prostatic hyperplasia, Estramustine phosphate sodium, abira...

Claims

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Application Information

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IPC IPC(8): C07J41/00A61P35/00
CPCC07J41/005
Inventor 甘春芳董新刘志平盛海兵黄燕敏崔建国
Owner 南宁师范大学
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