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Pharmaceutical composition composed of hydroxamic acid compounds and vitamin A compounds and application thereof

The technology of a compound and hydroxime, which is applied to a pharmaceutical composition composed of a hydroxamic acid compound and a vitamin A acid compound and its application field, can solve the problems of patient pain, toxicity, adverse side effects of normal cells and the like, and achieves the Injury reduction, cost saving, and effect of reducing drug dosage

Active Publication Date: 2014-10-29
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although SAHA can inhibit the proliferation of cancer cells, any drug that inhibits the proliferation of cancer cells has varying degrees of toxicity, and has adverse side effects on normal cells in the body, bringing pain to patients

Method used

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  • Pharmaceutical composition composed of hydroxamic acid compounds and vitamin A compounds and application thereof
  • Pharmaceutical composition composed of hydroxamic acid compounds and vitamin A compounds and application thereof
  • Pharmaceutical composition composed of hydroxamic acid compounds and vitamin A compounds and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of N-(3-chlorophenyl)-N'-hydroxysuberamide (abbreviated as B102).

[0026] Step (1): Weigh 2.04g (16mmol) of 3-chloroaniline, 3.07g (16.32mmol) of monomethyl suberate, and 0.25g (4mmol) of boric acid into a 100mL three-necked round-bottomed flask, add 30mL of toluene, and protect it under nitrogen , magnetically stirred, the oil bath was heated until the toluene refluxed, and the water generated during the reaction was separated with a water separator. Before the reaction, the water separator was filled with toluene, and the reaction time was 18h. The agent is ether:petroleum ether=2:1. After the reaction is completed, pour the reaction solution into 500mL of petroleum ether under stirring, and after stirring for 0.5h, vacuum filter the solid with a sand core funnel, and wash the solid with water to remove the catalyst boric acid, then drain it and wash it with petroleum ether solid and drain the solid. Finally, 3.40g of solid was obtained, and the yield w...

Embodiment 2

[0029] Preparation of N-(3,4-dimethylphenyl)-N'-hydroxysuberamide (abbreviated as B113).

[0030] Step (1): Weigh 1.21g (10mmol) of 3,4-dimethylaniline, 1.88g (10mmol) of monomethyl suberate, and 0.31g (5mmol) of boric acid in a 100mL three-necked round-bottomed flask, and add 30mL of toluene , nitrogen protection, magnetic stirring, heating the oil bath to toluene reflux, using a water separator to separate the water generated in the reaction process, filling the water separator with toluene before the reaction, the reaction time is 10h, and tracking with a thin layer chromatography plate during the reaction For the reaction, the developer is ethyl acetate:petroleum ether=1:1. After the reaction is completed, pour the reaction solution into 300mL of petroleum ether under stirring. After stirring for 0.5h, vacuum filter the solid with a sand core funnel, and wash the solid with water to remove the catalyst boric acid, and then wash it with petroleum ether after draining. soli...

Embodiment 3

[0033] Preparation of N-(3-trifluoromethoxyphenyl)-N'-hydroxysuberamide (referred to as B124).

[0034] Step (1): Weigh 0.89g (5mmol) of 3-trifluoromethoxyaniline, 0.96g (5.1mmol) of monomethyl suberate, and 0.16g (2.5mmol) of boric acid in a 100mL three-necked round-bottomed flask, and add 30mL toluene, nitrogen protection, magnetic stirring, oil bath heating to toluene reflux, use a water separator to separate the water generated during the reaction, fill the water separator with toluene before the reaction, the reaction time is 13h, and use thin layer chromatography during the reaction Plate tracking reaction, the developer is ether: petroleum ether = 1:1. After the reaction is completed, pour the reaction solution into 200mL of petroleum ether under stirring, and after stirring for 0.5h, vacuum filter the solid with a sand core funnel, and wash the solid with water to remove the catalyst boric acid, then drain it and wash it with petroleum ether solid and drain the solid....

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Abstract

The invention relates to the field of medicinal chemistry and particularly relates to a pharmaceutical composition composed of hydroxamic acid compounds and vitamin A compounds and an application thereof. The pharmaceutical composition provided by the invention has the capacity of inhibiting the proliferation of cancer cells, so as to achieve the purpose of curing cancers. The pharmaceutical composition provided by the invention has an obvious assisted synergistic effect, the capacity of inhibiting the proliferation of cancer cells of the pharmaceutical composition is stronger than that of single use of the hydroxamic acid compounds, and the pharmaceutical composition particularly has excellent anti-proliferation activity on human cancer cells.

Description

technical field [0001] The invention relates to a combination medicine composed of hydroxamic acid compounds and vitamin A acid compounds. The invention relates to the preparation of combination medicine for inhibiting cancer cell proliferation and / or treating cancer. Background technique [0002] Cancer, also known as malignant tumor. Cancer is caused by uncontrolled cell growth caused by a part of cells in humans or mammals, to varying degrees, not complying with normal cell proliferation and differentiation control mechanisms. Cancer cells can not only grow and multiply rapidly in internal organs and tissues, but also transfer to other parts of the body through the internal circulatory system or lymphatic system. Cancer cells can proliferate indefinitely without controlled intervention, which will consume a large amount of nutrients in the patient's body and release a large amount of toxins, which in turn will cause severe organ failure in the patient. There are many an...

Claims

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Application Information

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IPC IPC(8): A61K31/203A61K35/00A61K31/167
Inventor 袁其朋邓炳华师婧华谢瑞武新颖
Owner BEIJING UNIV OF CHEM TECH
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