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A kind of p-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

A compound, estrogen technology, applied in the direction of amide active ingredients, drug combination, antineoplastic drugs, etc.

Inactive Publication Date: 2020-02-18
QILU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These studies suggest that modulators targeting ERRα have the potential to serve as clinically effective antitumor agents

Method used

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  • A kind of p-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application
  • A kind of p-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application
  • A kind of p-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0024] Example 2 The detection technology of time-resolved fluorescence resonance energy transfer (Time-Resolved Fluoresen-ce Resonance Energy Transfer assay, TR-FRET assay) was used to test the competitive binding activity of the compound of formula I of the present invention to ERRα at the molecular level

[0025] This example illustrates that the compounds involved in the present invention can effectively inhibit the combination of ERRα and PGC1α, indicating that the compounds involved in the present invention competitively bind to ERRα (molecular level). TR-FRET is a technique familiar to those skilled in the art. FRET (Fluorescence Resonance Energy Transfer), that is, fluorescence resonance energy transfer, is based on the energy transfer of two fluorophores (donor and acceptor), when the two fluorophores are close to each other. Interactions between biomacromolecules can be measured with fluorescent labels and energy transfer between the two. When the two groups are clo...

Embodiment 3

[0029] Example 3 Using CCK-8 Cell Proliferation Assay to Determine the Proliferation Inhibitory Effects of Compounds on Various Tumor Cell Lines

[0030] This example illustrates that the compounds involved in the present invention can effectively inhibit the proliferation of various tumor cell lines, indicating that the compounds involved in the present invention exhibit effective anti-tumor activity in vitro. The CCK-8 cell proliferation assay is a technique familiar to those skilled in the art.

[0031] (1) Tumor cell culture and seeding in 96-well cell culture plate: Take out the tumor cells in the logarithmic growth phase in good condition, observe the cell morphology, if the cells have been 80% confluent, start passage. Wash and discard the old culture medium in the petri dish, wash with sterile 1mL PBS for 3-5 times, add 1mL of warmed trypsin, shake the dish horizontally to make the trypsin evenly distributed and fully digested. Put the cells in the incubator for 1-2 m...

Embodiment 4

[0036] Example 4 Using Transwell tumor cell migration assay to determine the effect of compounds on the migration function of breast cancer cell MDA-MB-231

[0037] This example illustrates that the compounds involved in the present invention can effectively inhibit the migration of breast cancer cells MDA-MB-231, indicating that the compounds involved in the present invention exhibit effective anti-migration activity of breast cancer cells in vitro. Transwell tumor cell migration assay is a technique familiar to those skilled in the art.

[0038] (1) Preparation of Transwell chamber: Matrigel 1:8 (50mg / L) dilution was used to coat the upper chamber surface of the bottom membrane of the Transwell chamber to coat the basement membrane, and air-dried at 4°C. After air-drying, hydrate the basement membrane, suck out the residual liquid in the culture plate, add 50uL serum-free DMEM culture solution containing 10g / L BSA to each well, and incubate in a 37°C incubator for 30min.

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PUM

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Abstract

The invention discloses a novel p-methoxybenzyl-benzamide compound with formula I for regulating the activity of estrogen-related receptors, a pharmaceutically acceptable salt and applications thereof. The compound and its pharmaceutically acceptable salt can be used for the preparation of estrogen-related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRα) activity for the prevention and treatment of breast cancer, prostate cancer, gastric cancer, colon cancer Cancer, ovarian cancer, cervical cancer and other malignant tumors.

Description

technical field [0001] The present invention relates to a p-methoxybenzyl-benzamide compound and a pharmaceutically acceptable salt thereof as a modulator for regulating estrogen-related receptor alpha (ERR-alpha, ERR-alpha or ERRα) and The drug combination thereof and its application in the preparation of drugs for preventing and / or treating tumors such as breast cancer, prostate cancer, gastric cancer, colon cancer, ovarian cancer, cervical cancer or endometrial cancer. Background technique [0002] ERRα was cloned and identified by Giguere et al. in 1988. As an orphan nuclear receptor (Orphan nuclear receptor), the endogenous ligand of ERRα has not been discovered. ERRα is widely expressed in the body and can be detected from myocardium, digestive tract, brain, skeletal muscle, brown fat, breast cancer, ovarian cancer and other malignant tumors. ERRα has high homology with estrogen receptor α (ERα): DNA binding domain (DNA binding domain, DBD) amino acid similarity is 6...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/18A61P35/00A61P35/04
CPCA61K31/18
Inventor 杜永丽李群益凌浩张留弟
Owner QILU UNIV OF TECH
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