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Bi-amido heterocyclic derivative with antitumour activity and its preparation method and use

A technology of anti-tumor activity and derivatives, applied in the fields of anti-tumor drugs, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as difficulties in bone marrow donors, inaccurate effects on patient survival chances, and high costs

Inactive Publication Date: 2009-06-03
INST OF HEMATOLOGY & BLOOD HOSPITAL CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although bone marrow transplantation has a good curative effect at present and may cure the disease, it is limited by many factors such as the difficulty of bone marrow donors, rejection, age, and high cost; the application of interferon α can make the patient's "Philadelphia chromosome" negative, But the effect of improving patients' chances of survival is uncertain

Method used

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  • Bi-amido heterocyclic derivative with antitumour activity and its preparation method and use
  • Bi-amido heterocyclic derivative with antitumour activity and its preparation method and use
  • Bi-amido heterocyclic derivative with antitumour activity and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] p-Benzamidoacetophenone (IV)

[0069] 4-Aminoacetophenone (16.4g, 120mmol) and benzoyl chloride (14g, 100mmol) were dissolved in 1000ml of dichloromethane, triethylamine (18g, 180mmol) was added, stirred at room temperature for 4 hours, and the reaction solution was washed with 1N hydrochloric acid , dried over anhydrous sodium sulfate, and distilled off the solvent to obtain 20 g of the product, with a yield of 83.68%. m.p.126-128°C.

Embodiment 2

[0071] p-Butyrylaminoacetophenone (IV)

[0072] The method is the same as in Example 1 except that benzoyl chloride is replaced by butyryl chloride, and the yield is 71% in 17 g.

Embodiment 3

[0074] p-Ethoxybenzamidoacetophenone

[0075] The method is the same as in Example 1 except that benzoyl chloride is replaced with p-ethoxybenzoyl chloride, and the yield is 73% in 35 g.

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PUM

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Abstract

A biamidoheterocyclic derivative with antineoplastic activity and its preparing process are disclosed. It can be used to treat cancers, such as chronic granulocyte leukemia, acute lymphocyte leukemia and melanotic cancer etc.

Description

technical field [0001] The present invention relates to antitumor drugs and their synthesis, more specifically to a bisamidoheterocyclic derivative with antitumor activity and its preparation method, and a pharmaceutical composition containing such derivatives in a therapeutically effective amount And the application of the composition in treating various malignant tumors such as chronic myelogenous leukemia (CML), adult acute lymphocytic leukemia (ALL), neuroblastoma, human myeloid erythroleukemia and melanoma. Background technique [0002] Cancer is a large class of diseases that seriously threaten human health. Finding effective treatments to conquer cancer has always been a research area that people pay close attention to. Traditional anticancer drugs are mainly cytotoxic drugs, which rely on the differences in the kinetics of growth, repair, and death between tumor cells and normal cells to kill tumor cells, so these drugs will inevitably affect normal cells. The thera...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/75C07D215/38C07D231/40C07D239/42C07D239/94C07D261/14C07D277/44C07D277/18C07D487/04A61K31/44A61K31/415A61K31/426A61K31/505A61P35/00
Inventor 杨纯正彭晖齐静黄牛王建祥谢平王彩云周圆
Owner INST OF HEMATOLOGY & BLOOD HOSPITAL CHINESE ACAD OF MEDICAL SCI
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