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Use of piperlongumine derivatives in preparation of medicines for treating cancers and medicinal compositions thereof

A technology of perylene amide and its derivatives, which can be used in drug combinations, antineoplastic drugs, and pharmaceutical formulations, and can solve problems such as inability to treat normal cells and cancer cells differently, side effects, and normal cell death

Inactive Publication Date: 2011-07-20
李绍路
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the research and development of new anticancer drugs, those drugs that can selectively kill cancer cells but are harmless to normal cells are hot spots among hotspots. This is because traditional cancer treatment drugs cannot combine normal cells with cancer cells. Differential treatment, if conventional drug delivery methods are used, it will cause a large number of normal cells in the drug delivery area to die, causing serious side effects
And if anticancer drugs that can selectively kill cancer cells are developed, the above disadvantages will no longer exist, and patients will be freed from the painful chemotherapy process

Method used

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  • Use of piperlongumine derivatives in preparation of medicines for treating cancers and medicinal compositions thereof
  • Use of piperlongumine derivatives in preparation of medicines for treating cancers and medicinal compositions thereof
  • Use of piperlongumine derivatives in preparation of medicines for treating cancers and medicinal compositions thereof

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Experimental program
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Effect test

Embodiment 1

[0037] Compound 1 of the present invention (see attached for the structural formula figure 1 ), when R 1 = -OCH 3 , R 2 =CH 3 The compound a is extracted from natural plants.

Embodiment 2

[0039] Compound formula 2 is synthesized as follows:

[0040]

[0041] The first step: in a 100 mL round bottom flask, add 1 g (1 equivalent) of reactant (1) and 4.10 g (1 equivalent) of reactant (2). Under the protection of argon, add 50 mL of anhydrous DMF solvent. After all the reactants were dissolved, 272 mg (1.1 equivalent) of sodium hydride was added at 0°C. After the reaction was stirred at 0°C for 2 hours, the temperature was gradually raised to room temperature; then the stirring was continued overnight. After the reaction is completed, most of the DMF is removed under high vacuum, and then the reaction concentrate is extracted with dichloromethane. The organic phases were combined, washed with saturated sodium bicarbonate and saturated brine, and concentrated with a rotary evaporator. Finally, the reaction product (3) is purified through a silica gel separation column. Final product: 2.65 g; Yield: 90%. Mass spectrum (HRMS, ESI): 288.1161 (M+1). Elemental analysi...

Embodiment 3

[0045] Compound formula 3 is synthesized as follows:

[0046]

[0047] The first step: In a 100 mL round-bottom flask, add 1 g (1 equivalent) of reactant (1) and 4.72 g (1 equivalent) of reactant (5). Under argon protection, add 50 mL of anhydrous DMF solvent. After all the reactants were dissolved, 272 mg (1.1 equivalent) of sodium hydride was added at 0°C. After the reaction was stirred at 0°C for 2 hours, the temperature was gradually raised to room temperature; then the stirring was continued overnight. After the reaction is completed, most of the DMF is removed under high vacuum, and then the reaction concentrate is extracted with dichloromethane. The organic phases were combined, washed with saturated sodium bicarbonate and saturated brine, and concentrated with a rotary evaporator. Finally, the reaction product (6) is purified by a silica gel separation column. Final product: 2.77 g; Yield: 85%. Mass spectrum (HRMS, ESI): 318.1259 (M+1). Elemental analysis: C, 64.35;...

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Abstract

The invention discloses the use of piperlongumine derivatives in the preparation of medicines for treating cancers and anticancer medicinal compositions taking the piperlongumine derivatives as active ingredients. The invention provides several piperlongumine derivatives, which are extracted from natural plants and synthesized artificially. Experiments prove that these compounds can selectively kill cancer cells without influencing the physiological functions of normal cells. Animal in-vivo experiments prove that these compounds can obviously suppress the growth of tumors without influencing the normal physiological functions of animals. Thus, these compounds can be used for preparing new anticancer medicines capable of killing cancer cells selectively.

Description

Technical field [0001] The present invention relates to the field of medicinal compounds for the treatment of cancer. Specifically, the present invention relates to the use of a piper amide derivative in the preparation of a medicine for the treatment of cancer and a pharmaceutical composition that uses the piper amide derivative as an active ingredient and can be used for the treatment of cancer. Background technique [0002] According to the World Health Organization: In the 1980s, there were about 7 million cancers worldwide each year, and about 5 million cancer deaths each year. By the 1990s, there were about 10 million cancers worldwide and 7 million deaths each year. Cancer is becoming more and more serious around the world. In the mid-1970s of our country, the National Cancer Research Office of the Ministry of Health organized a national retrospective survey of cancer deaths. At that time, there were about 900,000 cancer incidences and 700,000 cancer deaths each year. B...

Claims

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Application Information

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IPC IPC(8): A61K31/4412A61K31/4545A61P35/00
Inventor 李绍路
Owner 李绍路
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