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A class of substituted homopiperazine aminocarbamate bismuth complexes, pharmaceutically acceptable salts of the complexes, preparation methods and anti-tumor applications of the complexes

A technology of bismuth aminocarbamate and homopiperazine, which is applied in the field of antitumor drugs, can solve the problems of few antitumor cell lines, low clinical application value, and single structure, and achieve significant antitumor activity, good antitumor effect, and widespread The effect of applying the foreground

Inactive Publication Date: 2017-05-10
NANYANG NORMAL UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, there are problems of single structure, few anti-tumor cell lines, and low clinical application value, and there is still a long way to go before clinical application

Method used

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  • A class of substituted homopiperazine aminocarbamate bismuth complexes, pharmaceutically acceptable salts of the complexes, preparation methods and anti-tumor applications of the complexes

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Embodiment Construction

[0022] The present invention will be further described below through specific examples, but not as a limitation.

[0023] A, B, C, D, and E in the examples are used as numbers.

[0024] Implementation 1: Preparation of 4-methylhomopiperazine bismuth dicarbamate (A)

[0025] Add 0.571 g (5 mmol) of 1-methylhomopiperazine, 0.25 g (6 mmol) of sodium hydroxide, and 10-15 mL of anhydrous methanol into a 50 mL round bottom flask, and stir magnetically in a cold water bath at 0-5 °C After dissolving, add dropwise 0.76g (10 mmol) CS 2 , low temperature magnetic stirring reaction for 1 h, 10-50 ° C magnetic stirring reaction for 3 h.

[0026] 0.53 g (1.7 mmol) BiCl 3 Dissolve it in 5-15 mL of anhydrous methanol, drop it into the above reaction solution, add a certain amount of dichloromethane, and stir at room temperature for 3 h. After the reaction, a certain amount of water was added, the dichloromethane layer was separated, washed with water, dried over anhydrous sodium sulfate,...

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Abstract

The invention relates to substituted-homopiperzine dithiocarbamic acid bismuth complexes, and medicinal salts, preparation methods and antitumor application thereof. The condensed structural formula of the complexes is shown in the description, wherein R represents methyl, ethyl, benzyl, acetyl or benzyloxycarbonyl. The substituted-homopiperzine dithiocarbamic acid bismuth complexes have excellent antitumor activity, remarkable tumor inhibition activity on stomach cancer, lung cancer, liver cancer, colorectal cancer, ovarian cancer and other malignancies, and broad application prospects after being developed to novel anti-tumor drugs.

Description

technical field [0001] The invention relates to the technical field of antitumor drugs, in particular to a class of substituted homopiperazine bismuth complexes, pharmaceutically acceptable salts of the complexes, preparation methods and antitumor applications of the complexes. Background technique [0002] Malignant tumors (cancer) are a serious threat to human health and life. Every year, patients who die from cancer account for about a quarter of the total death toll, and the incidence rate is increasing year by year. Cancer prevention and treatment has become a major issue for medical and life science workers. one of the research topics. The incidence of cancer in my country is very alarming, and has become the second most cancer-incidence country in the world. Statistics (WHOGLOBOCAN 2008) show that all new cancer cases in China are 2.8 million, which is twice the number of new cancer cases in the United States (1.4 million in the United States). ; In the same year, the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/21A61K31/555A61P35/00
CPCC07D295/21
Inventor 郭应臣邱东方孙如中郭婷卓立宏
Owner NANYANG NORMAL UNIV
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