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Naphtho dihydrofuryl o-quinone compound and its preparation method and use

A technology of naphthodihydrofuran ortho and quinone compounds, which can be applied in the fields of organic chemistry, drug combination, antitumor drugs, etc., can solve problems such as causing cancer

Inactive Publication Date: 2006-12-27
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If PTPα is abnormally activated or overexpressed, it can lead to cancer

Method used

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  • Naphtho dihydrofuryl o-quinone compound and its preparation method and use
  • Naphtho dihydrofuryl o-quinone compound and its preparation method and use
  • Naphtho dihydrofuryl o-quinone compound and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0030] (1) We will take the compound 2,3-dihydro-6-hydroxy-3-methylnaphtho[1,2-b]-furan-4,5-dione (structural formula 8) as an example to introduce the synthetic route 1, but does not limit this patent in any way. The reaction route is shown as follows:

[0031]

[0032] a. Synthesis of compound 2-4: Compound 1 (Jung M.E., Hagenah J.A., J.Org.Chem. 1987, 52, 1889) (1.03 g, 3.86 mmol), 50 ml of diethyl ether, and hydrosulfite (5.00 g) were added to the flask , 28.7mmol) was dissolved in 50ml of water, added to a flask, stirred for 30 minutes, the mixture was put into a separatory funnel, separated into layers, separated from the water layer, washed with water, washed with saturated brine, and dried over anhydrous sodium sulfate. Filter and concentrate to obtain compound 2. Compound 2 was quickly dissolved in 20ml of acetone, anhydrous potassium carbonate powder (2.92g, 38.6mmol) was added, stirred for a while, allyl bromide (0.934g, 7.72mmol) was added dropwise, and the mi...

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Abstract

The invention provides an inhibitor aiming at PTP, the construction formula of which is presented in diagram. It is demonstrated that the inhibitor can inhibit activity of different PTP, and it can be used to treat disease caused by PTP, especially tumor. The invention also provides the method for preparing said inhibitor, inhibiting action for PTP at molecular level and anti-tumor action at cell level.

Description

technical field [0001] The present invention relates to a class of naphthodihydrofuran o-quinone compounds with antitumor activity, including the preparation method of these compounds, the inhibitory effect on several protein tyrosine phosphatases (PTP) at the molecular level and the inhibitory effect at the cellular level. Antitumor effect. Background technique [0002] Cancer is a great threat to human health. The World Health Organization released the World Cancer Report on April 3, 2003, saying that the next few years will be a year of high incidence of cancer worldwide. If countries do not take urgent measures, the incidence of cancer will increase by 50%. , 15 million new cases will be added each year by 2020. The World Health Organization first published the "World Cancer Report" in 1995, calling on countries to monitor, prevent and treat cancer. However, due to environmental pollution, unhealthy lifestyles, lack of exercise, and a serious aging population, cancer ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/92A61K31/343A61P35/00
Inventor 吕伟李佳张涛黄维刚李静雅
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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