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Application of 10-arylmethenyl anthrones in the preparation of antitumor drugs

A technology of arylmethylenyl anthrone and anti-tumor drugs, which is applied in the field of application of 10-arylmethylenyl anthrone compounds in the preparation of anti-tumor drugs, and can solve problems such as difficult-to-cure malignant tumors

Active Publication Date: 2015-08-05
湖南康立成生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although great progress has been made in the research and development of anti-tumor drugs, malignant tumors are still difficult to cure diseases, and the incidence of tumors is still increasing year by year. Therefore, there is still an urgent need to develop more effective anti-tumor drugs

Method used

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  • Application of 10-arylmethenyl anthrones in the preparation of antitumor drugs
  • Application of 10-arylmethenyl anthrones in the preparation of antitumor drugs
  • Application of 10-arylmethenyl anthrones in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～8

[0019] Embodiments 1-8: Anti-human ovarian cancer activity test

[0020] Test method: in vitro anti-tumor activity test method

[0021] A. Principle: Cells decompose thiazolidine (MTT) into water-insoluble blue-purple crystals through mitochondrial hydrolase and deposit them in cells. The light absorption value is measured at the place, which indirectly reflects the proliferation and quantity changes of cells.

[0022] B. Cell: HO, human ovarian cancer cell line;

[0023] C. Experimental steps

[0024] (1) Sample preparation: For soluble samples, dissolve each 1 mg with 40 μL DMSO, take 2 uL and dilute with 1000 μL culture medium to make the concentration 50 μg / mL, and then serially dilute with culture medium to the use concentration.

[0025] (2) Cell culture

[0026] Preparation of culture medium: every 1000 mL of culture medium contains 800,000 units of penicillin, 1.0 g of streptomycin, and 10% inactivated fetal bovine serum.

[0027] Cell culture: Inoculate tumor cel...

Embodiment 9～16

[0037] Examples 9-16: Anti-human pancreatic cancer activity test

[0038] Test method: in vitro anti-tumor activity test method

[0039] A. Principle: Cells decompose thiazolidine (MTT) into water-insoluble blue-purple crystals through mitochondrial hydrolase and deposit them in cells. The light absorption value is measured at the place, which indirectly reflects the proliferation and quantity changes of cells.

[0040] B. Cell: PANC-1, human pancreatic cancer cell line;

[0041] C. Experimental steps

[0042] (1) Sample preparation: For soluble samples, dissolve each 1 mg with 40 μL DMSO, take 2 uL and dilute with 1000 μL culture medium to make the concentration 50 μg / mL, and then serially dilute with culture medium to the use concentration.

[0043] (2) Cell culture

[0044] Preparation of culture medium: every 1000 mL of culture medium contains 800,000 units of penicillin, 1.0 g of streptomycin, and 10% inactivated fetal bovine serum.

[0045] Cell culture: Inoculate t...

Embodiment 17～24

[0055] Examples 17-24: Anti-human lung cancer activity test

[0056] Test method: in vitro anti-tumor activity test method

[0057] A. Principle: Cells decompose thiazolidine (MTT) into water-insoluble blue-purple crystals through mitochondrial hydrolase and deposit them in cells. The light absorption value is measured at the place, which indirectly reflects the proliferation and quantity changes of cells.

[0058] B. Cell: NCI, human lung cancer cell line;

[0059] C. Experimental steps

[0060] (1) Sample preparation: For soluble samples, dissolve each 1 mg with 40 μL DMSO, take 2 uL and dilute with 1000 μL culture medium to make the concentration 50 μg / mL, and then serially dilute with culture medium to the use concentration.

[0061] (2) Cell culture

[0062] Preparation of culture medium: every 1000 mL of culture medium contains 800,000 units of penicillin, 1.0 g of streptomycin, and 10% inactivated fetal bovine serum.

[0063] Cell culture: Inoculate tumor cells in ...

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Abstract

The invention provides an application of 10-arylmethylideneanthrone compounds to preparing antitumor drugs. The 10-arylmethylideneanthrone compounds are preferably selected from compounds represented by formula (I-3), formula (I-4), formula (I-5), formula (I-7) or formula (I-8), and most preferably selected from compounds represented by formula (I-3) or formula (I-7). The invention provides the application of the 10-arylmethylideneanthrone compounds to preparing the antitumor drugs, especially the compounds represented by formula (I-3) or formula (I-7) have substantial effect on various different tumors, and a foundation is provided for screening of new drugs.

Description

(1) Technical field [0001] The invention relates to the application of a 10-arylmethylenyl anthrone compound in the preparation of antitumor drugs. (2) Background technology [0002] Malignant tumor (cancer) has become a major disease that seriously endangers human life and health. According to the latest data released by the World Health Organization (WHO), in recent years, the number of new cancer cases in the world has reached 12 million each year, and the number of deaths due to cancer has reached 7 million, accounting for 13% of the global death toll. In China, there are about 2.4 million new cancer patients every year, and about 1.7 million cancer deaths, of which cancer deaths account for 20% of the total deaths. Moreover, according to WHO estimates, on a global scale, new cancer cases and the death rate of cancer patients will also increase at a rate of 1% per year, and the growth rate will be faster in countries such as China, Russia and India. In some countries a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61K31/136A61K31/167A61K31/404A61P35/00
Inventor 周卫胡惟孝
Owner 湖南康立成生物科技有限公司
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