New application for imidazo(1,2-A)pyridine compound capable of serving as androgen receptor antagonist

A technology of pyridoimidazole and androgen receptor, applied in the field of medicine, can solve problems such as no reports

Inactive Publication Date: 2017-09-19
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there has never been any report on the research on pyridoimidazole compounds as antitumor drugs, especially anti-prostate cancer

Method used

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  • New application for imidazo(1,2-A)pyridine compound capable of serving as androgen receptor antagonist
  • New application for imidazo(1,2-A)pyridine compound capable of serving as androgen receptor antagonist
  • New application for imidazo(1,2-A)pyridine compound capable of serving as androgen receptor antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Preparation and Characterization of Pyridoimidazole Compounds I and II.

[0026] 5-(1-Methylcyclopropyl)-7-trifluoromethyl-4,5,6,7-tetrahydropyrazol[1,5-α]pyrimidine-2-carboxylic acid, 3-chloro-5 -Phenyl-7-trifluoromethyl-4,5,6,7-tetrahydropyrazol[1,5-α]pyrimidine-2-carboxylic acid was purchased from Bailingwei Technology Co., Ltd.

Embodiment 2

[0027] Example 2 Preparation and Characterization of Pyridoimidazole Compound III.

[0028] Example III of pyridoimidazole compounds, 4(5-(3,4-dimethoxyphenyl)-7-(trifluoromethyl)-4,5,6,7 tetrahydropyrazol[1,5- α]-2-pyrimidine) benzoic acid, its structure is as follows, and concrete synthetic method is according to reference 1:

Embodiment 3

[0029] Example 3 Determination of antitumor activity of pyridoimidazole compounds.

[0030] The cell lines used in the experiment of the present invention are the prostate tumor cell lines of people in the world, that is:

[0031] Prostate tumor LNCaP cells were purchased from Shanghai Meixuan Bioreagent Company.

[0032] Antitumor activity experiments of pyridoimidazole compounds.

[0033] The antitumor activity experiments of pyridoimidazole compounds Ⅰ, Ⅱ and Ⅲ were carried out by cell culture method. Determination of IC by MTT method 50 .

[0034] Prostate cancer LNCaP cells were selected as target cells. Cells were diluted to 10 with 1640 medium 4 cells / mL of cell suspension, 200 μL of LNCaP cell suspension per well was added to a 96-well plate, placed in a 5% CO2 incubator at 37°C for 48 hours, and 100 μL of the original medium was aspirated. Dilute the compound to be tested at a certain concentration and add it to the cells at 10 μL / . Mixture. At the same time, ...

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Abstract

The invention relates to the technical field of medicines, and provides application of an imidazo(1,2-A)pyridine compound capable of serving as an androgen receptor antagonist in preparing anti-tumor medicines. Through a cell experiment, the imidazo(1,2-A)pyridine compound disclosed by the invention has a function of inhibiting the growth of tumor cells in vitro, can be used for preparing medicines capable of preventing or / and treating benign prostatic hyperplasia, prostatic cancer, woman hirsutism, severe androgen-dependent alopecia or acne symptoms or diseases related to androgen receptors, and has a potential prospect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to pyridoimidazole compounds which can be used as androgen receptor antagonists. Background technique [0002] Prostate cancer is a serious male disease with a very high morbidity and mortality rate in Europe and the United States. It ranks in the forefront of male malignant tumors, second only to lung cancer. Although the incidence of prostate cancer in my country is lower than that in Europe and the United States, it is on the rise with the acceleration of the aging process and the improvement of the diagnosis level of this type of disease. Clinical studies have shown that the age of onset of such diseases tends to be younger, especially among people who sit and work for a long time. So far, the research on the mechanism of prostate cancer and the development of anti-prostate cancer drugs have attracted widespread attention all over the world. [0003] As an important class of ...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P13/08A61P35/00
CPCA61K31/519
Inventor 李加忠王欣王少华王育伟
Owner LANZHOU UNIVERSITY
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