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A novel 3-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

A compound, estrogen technology, used in organic chemistry, amide active ingredients, drug combinations, etc.

Inactive Publication Date: 2018-05-22
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 novel 3-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application
  • A novel 3-methoxybenzyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 uses reporter gene test formula I compound to the transcription regulation activity of ERR-alpha

[0016]

[0017] This example illustrates that the compound of formula I involved in the present invention can effectively inhibit the expression of the reporter gene regulated by ERR-alpha in human embryonic kidney cells HEK-293, indicating that the compound of formula I involved in the present invention can effectively regulate ERR-alpha alpha function. Reporter gene testing techniques are familiar to those skilled in the art.

[0018] We used the GAL4 fusion receptor activation method to test the transcriptional regulation activity of the compound of formula I on ERRs. The GAL4 fusion receptor activation method is based on the one-hybrid principle of mammalian cells, that is, the receptor LBD and the yeast transcription factor DBD are constructed into a fusion protein expression plasmid, and the receptor LBD acts as the activation domain (Activation doma...

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Abstract

The invention discloses a novel 3-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 novel 3-methoxybenzyl-benzamide compound and a pharmaceutically acceptable salt thereof as an estrogen-related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRα) regulator Agents and their drug combinations and their use in the preparation of drugs for the prevention and / or treatment of 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) amin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C311/08A61K31/18A61P35/00
CPCA61K31/18C07C311/08
Inventor 杜永丽韩炜炜凌浩李群益
Owner QILU UNIV OF TECH
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