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Novel N-isopropyl-benzamide compound for adjusting activity of estrogen-related receptor and medical application of novel N-isopropyl-benzamide compound

A compound, estrogen technology, used in amide active ingredients, drug combinations, anti-tumor drugs, etc.

Inactive Publication Date: 2017-04-05
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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  • Novel N-isopropyl-benzamide compound for adjusting activity of estrogen-related receptor and medical application of novel N-isopropyl-benzamide compound
  • Novel N-isopropyl-benzamide compound for adjusting activity of estrogen-related receptor and medical application of novel N-isopropyl-benzamide compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 uses reporter gene test formula I compound to the transcription regulation activity of ERR-alpha

[0017]

[0018] 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.

[0019] 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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PUM

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Abstract

The invention discloses a novel N-isopropyl-benzamide compound (with a formula I) for adjusting activity of an estrogen-related receptor, medical acceptable salt of the novel N-isopropyl-benzamide compound and an application of the novel N-isopropyl-benzamide compound. The compound and the medical acceptable salt of the compound can be used for preparing drugs capable of adjusting the activity of the estrogen-related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERR alpha) and preventing and curing the breast cancer, the prostatic cancer, the stomach cancer, the colon cancer, the ovarian cancer, the cervical cancer and other malignant tumors.

Description

technical field [0001] The present invention relates to a novel N-isopropyl-benzamide compound and a pharmaceutically acceptable salt thereof as a modulator for regulating estrogen-related receptor alpha (ERR-alpha or ERRα) The medicine combination thereof and the application thereof in preparing medicines 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 68%, an...

Claims

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Application Information

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IPC IPC(8): A61K31/18A61P35/00
Inventor 杜永丽宋莲华凌浩李群益
Owner QILU UNIV OF TECH
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