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A kind of organic selenium compound and its preparation method and application

A compound and organic selenium technology, applied in the field of biomedicine, can solve problems such as side effects, and achieve the effects of inhibiting tumor growth, improving tumor cell inhibition, and excellent anti-tumor effect.

Active Publication Date: 2021-11-30
JIANGHAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is known that the toxicity of anticancer drugs not only acts on cancer cells, but also acts on normal cells of patients, causing side effects

Method used

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  • A kind of organic selenium compound and its preparation method and application
  • A kind of organic selenium compound and its preparation method and application
  • A kind of organic selenium compound and its preparation method and application

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preparation example Construction

[0046] According to another typical implementation of the embodiments of the present invention, the preparation method of the organoselenium compound is provided, the method comprising:

[0047]

[0048] S1. Compound III is reacted with a chlorination reagent through chlorine substitution to obtain compound II;

[0049] As an optional embodiment, the chlorination reagent includes one of thionyl chloride, chlorosulfonic acid and tert-butyl hypochlorite. The ratio of the compound of formula III to thionyl chloride is 1:(1-6), the reaction temperature is 0-60° C., and the reaction time is 2-12 hours; these reaction conditions are favorable for complete chlorine substitution reaction.

[0050] S2, reacting the compound II with potassium selenocyanate to obtain compound I;

[0051] specifically:

[0052] The compound II is dissolved in an organic solvent, and potassium selenocyanate and catalyst potassium iodide are added for a heating reaction, followed by purification to obt...

experiment example 2

[0085] Experimental example 2: in vivo antitumor activity of the compound of formula I

[0086] The experimental animals were SPF-grade male Kunming mice with a body weight of 19-22 g, provided by the Animal Experiment Center of Wuhan University. The tumor strain mouse S180 sarcoma was introduced by the Institute of Materia Medica, Chinese Academy of Medical Sciences. The S180 cells used in the experiment were the cell suspension of passage 4 after resuscitation, and 5-fluorouracil was selected as the positive control drug.

[0087] The establishment of the S180 tumor-bearing mouse model was aseptically extracted ascites from S180-bearing mice, the cell suspension was counted under a microscope, and the cell concentration was adjusted to 2.0×10 7 0.2 mL / mL of the above-mentioned S180 ascites tumor fluid was aseptically inoculated subcutaneously in the right axilla of the mice, and 20 healthy mice were randomly divided into groups according to body weight.

[0088] Dosing meth...

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Abstract

The invention discloses an organoselenium compound and its preparation method and application. The organoselenium compound includes a compound represented by formula I. The compound represented by formula I has unexpected biological activity of preventing and / or treating tumors. It can be effectively used for the prevention and / or treatment of various cancers. The compound represented by formula I has cytotoxic activity to different tumor cells, especially to SW480 cell line, which is better than the control drug 5-fluorouracil, and can play a better inhibitory effect on tumor cells. The results of animal experiments showed that Compound I had a significant effect of inhibiting tumor growth in S180-bearing mice, and the anti-tumor effect at the same dose (5 mg / kg) was better than that of the control compound 5-fluorouracil. Therefore, the compound represented by formula I exhibits higher tumor growth inhibition efficiency than 5-fluorouracil.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to an organic selenium compound and its preparation method and application. Background technique [0002] Malignant tumors have become a prominent public health problem in the world today. Currently, cancer treatment methods mainly include surgical treatment, radiotherapy, chemotherapy, and biological therapy, among which chemical drug therapy is still the main treatment method. [0003] Cancer occurs as an abnormal mass of tissue in a living host organism, which receives nutrients from the host, overproliferates independently of the host, and destroys the host organism. Human organs are composed of a large number of cells. Cancer occurs when normal cells of the body become abnormal and the abnormal cells divide and multiply without check. Although genetic factors are closely related to the incidence of cancer, environmental factors also have an important impact on whether an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/16A61K31/52A61P35/00
CPCA61P35/00C07D473/16
Inventor 贺贤然钟敏
Owner JIANGHAN UNIVERSITY
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