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Piperlongumine derivatives and medicinal composition and application to preparation of medicament for inhibiting tumor growth thereof

A technology of longinamide and derivatives, applied in drug combination, anti-tumor drugs, organic chemistry, etc., can solve problems such as inability to treat normal cells and cancer cells differently, normal cell death, side effects, etc.

Inactive Publication Date: 2011-08-10
LAIYI TECH DEV XINCHANG COUNTY
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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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  • Piperlongumine derivatives and medicinal composition and application to preparation of medicament for inhibiting tumor growth thereof
  • Piperlongumine derivatives and medicinal composition and application to preparation of medicament for inhibiting tumor growth thereof
  • Piperlongumine derivatives and medicinal composition and application to preparation of medicament for inhibiting tumor growth thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Compound 1 of the present invention (structural formula sees attached figure 1 ), when R 1 =-OCH 3 , R 2 =CH 3 Compound a is extracted from natural plants.

Embodiment 2

[0033] Compound formula 2 is synthesized according to the following steps:

[0034]

[0035] Step 1: 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 argon protection, 50 mL of anhydrous DMF solvent was added. After all the reactants were dissolved, 272mg (1.1 equivalent) of sodium hydride was added at 0°C. After the reaction was stirred at 0°C for 2 hours, it was gradually warmed to room temperature; stirring was then continued overnight. After the reaction was completed, most of the DMF was removed under high vacuum, and the reaction concentrate was 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 analysis...

Embodiment 3

[0039] Compound formula 3 is synthesized according to the following steps:

[0040]

[0041] Step 1: 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, 50 mL of anhydrous DMF solvent was added. After all the reactants were dissolved, 272mg (1.1 equivalent) of sodium hydride was added at 0°C. After the reaction was stirred at 0°C for 2 hours, it was gradually warmed to room temperature; stirring was then continued overnight. After the reaction was completed, most of the DMF was removed under high vacuum, and the reaction concentrate was 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 through a silica gel separation column. Final product: 2.77 g; Yield: 85%. Mass spectrum (HRMS, ESI): 318.1259 (M+1). Elemental analysis...

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Abstract

The invention provides application of piperlongumine derivatives to the preparation of a medicament for treating a cancer and a medicinal composition which uses the piperlongumine derivatives as active ingredients and can be used for treating the cancer. The invention provides various piperlongumine derivatives which are extracted from natural plants and are synthetized artificially. Experiments prove that the compounds can be used for selectively killing cancer cells without influencing the physiological functions of normal cells, and animal in-vivo experiments prove that the compounds can be used for obviously inhibiting tumor growth without influencing the normal physiological functions of animals so as to show that the compounds can be used for preparing the novel anti-cancer medicament capable of selectively killing the cancer cells.

Description

technical field [0001] The present invention relates to the field of pharmaceutically useful compounds for the treatment of cancer. Specifically, the present invention relates to the use of the perylene amide derivatives in the preparation of medicines for treating cancer and the pharmaceutical composition which can be used for the treatment of cancers with the perylene amide derivatives as active ingredients. Background technique [0002] According to the introduction of the World Health Organization: in the 1980s, the incidence of cancer in the world was about 7 million people every year, and the number of cancer deaths was about 5 million people every year. By the 1990s, about 10 million people were diagnosed with cancer every year in the world, and about 7 million people died every year. The harm of cancer in the world is becoming more and more serious. In the mid-1970s in my country, the National Cancer Prevention and Research Office of the Ministry of Health organize...

Claims

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Application Information

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IPC IPC(8): C07D211/86C07D401/12A61K31/4412A61K31/4545A61P35/00
Inventor 曹瑞伟何益民
Owner LAIYI TECH DEV XINCHANG COUNTY
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