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Application of aromatic ester compounds in preparing anti-tumor drugs

A technology of ester compounds and anti-tumor drugs, applied in the field of anti-tumor drugs, can solve the problems of biological activity evaluation and other problems

Active Publication Date: 2017-05-31
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Its biological activity has not been evaluated

Method used

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  • Application of aromatic ester compounds in preparing anti-tumor drugs
  • Application of aromatic ester compounds in preparing anti-tumor drugs
  • Application of aromatic ester compounds in preparing anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] [Example 1] In vitro anti-tumor activity evaluation of compounds

[0024] Tested tumor cells: human liver cancer cells HepG2, human lung cancer cells A549, human breast cancer cells MCF-7, human breast cancer cells resistant to doxorubicin (MCF-7 / ADR), human gastric cancer cells SGC-7901, human cervical cancer cells Cell Hela, human glioma cell C6.

[0025] Cell culture: GIBCO DMEM medium, 10% fetal bovine serum and 0.01% L-glutamine were prepared as culture medium. Cultured cell lines were placed at 37°C, 5% CO 2 The cells were routinely cultured and subcultured under saturated humidity, and the cells in the logarithmic growth phase were used in the experiments.

[0026] In vitro anti-tumor activity evaluation (MTT method):

[0027] The above tumor cells were plated in 96-well plates respectively, and kept at 37°C, 5% CO 2 After the monolayer was grown in the incubator, the cell culture medium was discarded, and the cell maintenance medium containing different conc...

Embodiment 2

[0036] [Example 2] The tumor cell pathological effect caused by compound WY90

[0037] We further documented the tumor cytopathic effect induced by WY90 by microscopy. The specific implementation method is as follows:

[0038] HepG2, MCF-7, MCF-7 / ADR, SGC-7901, Hela, and C6 tumor cells in the logarithmic growth phase were respectively plated on 24-well plates, cultured in a 5% CO2 incubator at 37°C, and then discarded. Cell-free culture medium was added to the cell maintenance medium containing 20 μg / mL WY90 (Hela cells plus 10 μg / mL) to continue the culture. At 48 hours, the cells were visually observed under a microscope and photographed.

[0039] The tumor cell pathological effect caused by compound WY90 is as follows: image 3 shown. Under the microscope, the untreated tumor cells grew well, with firm adherence, plump shape, and clear borders. 20μg / mL WY90 treatment for 48 hours led to the apoptosis of all tumor cells, and the cells became round in different forms and fe...

Embodiment 3

[0040] [Example 3] Evaluation of tumor cell apoptosis activity caused by compound WY90

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Abstract

The invention relates to the field of anti-tumor drugs and provides an application of aromatic ester compounds in preparing anti-tumor drugs. The aromatic ester compounds are compounds shown by WY90, WY96 and MY99. According to anti-tumor activity study experiments, the compounds all show activity in resisting tumor cell proliferation in different degrees, wherein the WY90 shows the strongest inhibiting effect and can efficiently inhibit the tumor cell growth at low concentration to promote tumor cell apoptosis, and the inhibiting effect is stronger than that of a positive control compound. The preparation process of the compounds is simple and easy to implement, and the raw materials are cheap and easily available; and anti-tumor effect targets can be found through structure-activity relationship study, so that a valuable guide effect is provided for further drug development. The aromatic ester compounds provided by the invention provide a foundation for new drug screening.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, and in particular relates to the application of ester compounds with novel structures in the preparation of antitumor drugs. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. The mortality rate of human beings caused by malignant tumors ranks second among all diseases, becoming the second "killer" after cardiovascular diseases. At the beginning of 2013, the National Cancer Registry Center issued a version of the "2012 China Cancer Registration Annual Report", indicating that there are about 3.12 million new cancer cases in China every year, and more than 2 million cancer deaths, which means that 6 people are diagnosed with cancer every minute. cancer. At present, the incidence of cancer in the whole country is severe, and the incidence and mortality are on the rise. Cancer has become one of the major problems that ser...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4402A61P35/00
CPCA61K31/4402
Inventor 魏艳红奚彩丽尧晨光胡康洪李栋张谦
Owner HUBEI UNIV OF TECH
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