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Application of diaryl ketone compounds in preparation of antitumor drug

A technology of diaryl ketones and anti-tumor drugs, which is applied in the field of application of diaryl ketone compounds in the preparation of anti-tumor drugs, and can solve problems such as evaluation of biological activity

Active Publication Date: 2017-05-10
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its biological activity has not been evaluated

Method used

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  • Application of diaryl ketone compounds in preparation of antitumor drug
  • Application of diaryl ketone compounds in preparation of antitumor drug
  • Application of diaryl ketone compounds in preparation of antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] In the following, unless otherwise specified, the materials and methods of operation used in the present invention are well known in the art. [Example 1] Evaluation of in vitro antitumor activity of compounds

[0023] Tested tumor cells: human hepatoma cell HepG2, human lung cancer cell A549, human breast cancer cell MCF-7, doxorubicin-resistant human breast cancer cell (MCF-7 / ADR), human gastric cancer cell SGC-7901, human cervical cancer Cell Hela, human glioma cell C6.

[0024] Cell culture: GIBCO DMEM medium, 10% fetal bovine serum and 0.01% L-glutamine were formulated into culture medium. Cultured cell lines were placed at 37°C, 5% CO. 2 The cells were routinely cultured and passaged under saturated humidity, and the cells in the logarithmic growth phase were used in the experiments.

[0025] In vitro antitumor activity evaluation (MTT method):

[0026] The above tumor cells were plated in 96-well plates, and after they were cultured in a 37°C, 5% CO2 incubator...

Embodiment 2

[0036] [Example 2] Tumor cytopathic effects caused by compounds

[0037] We further recorded the cytopathic effect of Hela, C6, HepG2, MCF-7, MCF-7 / ADR tumor cells induced by representative compounds M131 and M15 by microscopy. The specific implementation method is as follows:

[0038] Hela, C6, HepG2, MCF-7, MCF-7 / ADR tumor cells in logarithmic growth phase were plated in 24-well plates, and the cell culture medium was discarded after culturing at 37°C in a 5% CO2 incubator. , respectively, adding 20 μg / mL M131 and 40 μg / mL M15 test compound cell maintenance solution to continue culturing, and 48 hours later, the cytopathic conditions were observed and photographed by microscope.

[0039] Compound-induced tumor cytopathic effects such as image 3 shown. Under the microscope, untreated tumor cells grew well, adhered firmly, with plump shapes and clear borders. Treatment of 20μg / mL M131 and 40μg / mL M15 for 48h resulted in apoptosis of all tumor cells, and the cells became r...

Embodiment 3

[0040] [Example 3] Evaluation of tumor cell apoptosis activity induced by compounds

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Abstract

The invention relates to the field of antitumor drugs and provides application of diaryl ketone compounds in preparation of the antitumor drug. The diaryl ketone compounds are compounds shown as formulas M11, M13, M14, M15, M-126, M128, M130, M131, M132 and M149. By antitumor activity research experiments, the compounds show anti-tumor cell proliferation activity with a certain degree, and most compounds show strong inhibition effect; the compounds can strongly inhibit the growth of tumor cells, can promote apoptosis at relatively-low concentration and show stronger inhibition effect compared with positive contrast compounds. The preparation process of the compounds is simple and feasible; raw materials are low in price and easy to obtain; an antitumor effect target of the compounds can be found by researching a structure-function relationship, and a valuable guiding function is provided for further research and development of the drugs. The diaryl ketone compounds disclosed by the invention provide a basis for screening new drugs.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, in particular to the application of diaryl ketone compounds in the preparation of antitumor drugs. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. The human mortality rate caused by malignant tumor ranks second among all diseases and becomes the second "killer" after cardiovascular disease. In early 2013, a version of the "2012 China Cancer Registration Annual Report" released by the National Cancer Registry indicated that there were about 3.12 million new cancer cases in China each year and more than 2 million deaths due to cancer, which means that 6 people are diagnosed with cancer every 1 minute. cancer. At present, the trend of cancer incidence in the country is severe, and the incidence and mortality rates are on the rise. Cancer has become one of the major problems that seriously threaten the safety of human l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/50A61K31/4418A61P35/00
CPCC07D213/50
Inventor 魏艳红奚彩丽张谦李栋胡康洪尧晨光
Owner HUBEI UNIV OF TECH
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