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Application and medicines of benzamide compound

A technology of benzamides and compounds, applied in the direction of drug combinations, medical preparations containing active ingredients, anti-tumor drugs, etc., to achieve obvious inhibitory effects

Inactive Publication Date: 2017-12-08
JIANGSU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The chromene-3-carboxamides and 2-phenyliminobenzopyrans obtained by the virtual screening method based on the structure of AKR1B10 / tolrestat are the most active AKR1B10 inhibitors (the minimum IC50 value is 6nM), but Also highly inhibitory activity against AKR1B1

Method used

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  • Application and medicines of benzamide compound
  • Application and medicines of benzamide compound
  • Application and medicines of benzamide compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: The enzyme inhibitory activity test of compound 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl)benzamide on AKR1B10 .

[0021] Experimental principle: Design based on the characteristic that the coenzyme NADPH is transformed into NADP+ with the reduction reaction of aldehyde and ketone substrates catalyzed by AKR1B10. Since NADPH has a characteristic maximum ultraviolet absorption peak at 340nm, and the product NADP+ absorbs very weakly at this wavelength, the degree of reduction of the coenzyme NADPH can be detected by detecting the decrease in the ultraviolet absorption value at 340nm, so as to obtain the speed of the enzyme-catalyzed reaction. In the initial stage of the reaction, the change curve of ultraviolet absorption at 340nm should be a straight line (zero-order reaction) theoretically, and the slope is proportional to the reaction speed.

[0022] When the compound was added, the reaction rate decreased, proving that the compound ...

Embodiment 2

[0034]Example 2: The enzyme inhibitory activity test of compound 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl)benzamide on AKR1B1 .

[0035] Experimental principle: Design based on the characteristic that the coenzyme NADPH is transformed into NADP+ with the reduction reaction of aldehyde and ketone substrates catalyzed by AKR1B1. Since NADPH has a characteristic maximum ultraviolet absorption peak at 340nm, and the product NADP+ absorbs very weakly at this wavelength, the degree of reduction of the coenzyme NADPH can be detected by detecting the decrease in the ultraviolet absorption value at 340nm, so as to obtain the speed of the enzyme-catalyzed reaction. In the initial stage of the reaction, the change curve of ultraviolet absorption at 340nm should be a straight line (zero-order reaction) theoretically, and the slope is proportional to the reaction speed.

[0036] When the compound was added, the reaction rate decreased, proving that the compound had...

Embodiment 3

[0047] Example 3: MTT method detects the effect of compound 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl)benzamide on liver cancer tumors in vitro Effects on Cellular HCC Survival.

[0048] Experimental principle: MTT, trade name thiazole blue, full name

[0049] 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. MTT colorimetry is a method for detecting cell viability. The detection principle is that succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystalline formazan (Formazan) and deposit in the cells, while dead cells do not have this function. Dimethyl sulfoxide (DMSO) can dissolve formazan in cells, and its light absorption value is measured at a wavelength of 570nm with a microplate reader, which can indirectly reflect the number of surviving cells. Within a certain range, the amount of MTT crystal formation is directly proportional to the number of cell survival.

[0...

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Abstract

The invention discloses a novel application of a benzamide compound. Specifically, 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl) benzamide provided by the invention has a function as an AKR1B10 inhibitor; and meanwhile, the 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl) benzamide has a relatively weak inhibitory activity on AKR1B10; therefore, the 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2-methylphenyl) benzamide can be used for preparing selective anti-cancer medicines related to the AKR1B10.

Description

technical field [0001] The invention belongs to the field of medical technology, and relates to the medical application of a small molecule compound, in particular to 4-(3,5-dimethoxybenzoyl)-N-(4-hydroxy-5-isopropyl-2- Use of methylphenyl)benzamide or a pharmaceutically acceptable salt thereof in the preparation of medicines for treating AKR1B10-related cancer diseases, especially AKR1B10 inhibitors. Background technique [0002] AKR1B10 is a member of the aldo-keto reductase superfamily (Aldo-keto Reductase, AKR). AKR is a nicotinamide purine dinucleotide NAD(P)(H)-dependent oxidoreductase that mainly catalyzes the reduction of the carbonyl of an aldehyde or ketone to a Primary or secondary alcohols are primary metabolic enzymes in the body. Studies have found that AKR1B10 is abnormally expressed in a variety of tumor tissues and cells: in 84% of squamous cell lung cancers (squamous cell pulmonary carcinomas), 70% of pancreatic cancers (pancreaticadenocarcinomas) and 54% ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/167A61P35/00
CPCA61K31/167
Inventor 许磊刘蒙蒙孙立磊孔韧
Owner JIANGSU UNIV OF TECH
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