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Applications of tea double-chlorine carboxamide and tea double-bromine carboxamide or like in preparation of products for prevention and treatment of diseases such as cancer

A technology of tea bisbromide and tea bischloramide, which is applied in the medical field, can solve problems such as restriction prevention and side effects, and achieve the effects of good curative effect, small side effects, and reduced side effects

Inactive Publication Date: 2013-05-22
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Due to the toxic and side effects of clinical chemotherapy and radiotherapy, the effective prevention and treatment of it is limited

Method used

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  • Applications of tea double-chlorine carboxamide and tea double-bromine carboxamide or like in preparation of products for prevention and treatment of diseases such as cancer
  • Applications of tea double-chlorine carboxamide and tea double-bromine carboxamide or like in preparation of products for prevention and treatment of diseases such as cancer
  • Applications of tea double-chlorine carboxamide and tea double-bromine carboxamide or like in preparation of products for prevention and treatment of diseases such as cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Two compounds for the treatment of tumors in this example, the name of which is (R)-ethyl ester-2-(6,8-dichloro-2-oxo-2H-benzopyran-3-carboxamide) -5-(Ethylamino)-5-oxopentanoic acid ester, referred to as tea dichloroaromatic amide (DTClC), has a chemical structural formula shown in formula (I); its 2 names are (R)-ethyl ester-2- (6,8-dibromo-2-oxo-2H-benzopyran-3-carboxamido)-5-(ethylamino)-5-oxopentanoate, referred to as tea bisbromamide (DTBrC ), having a chemical structural formula shown in formula (IV);

[0042] As the compound shown in formula (I) and formula (IV), the physical properties are all pale yellow powdery solids, and the melting point decomposes above 136° and 121° Celsius respectively;

[0043] The compound shown in formula (I) and formula (IV) is a pharmaceutically acceptable carrier; the pharmaceutically acceptable carrier includes any substance suitable for injection, preferably water for injection, or emulsifying agent, lipid body, nano preparati...

Embodiment 2

[0058] The difference between this embodiment and embodiment 1 is:

[0059] Step 1: Preparation of 6,8-dichlorocoumarin-3-carboxylic acid and 6,8-dibromocoumarin-3-carboxylic acid

[0060] (1) Add 205g of 3,5-dichlorosalicylaldehyde or 3,5-dibromosalicylaldehyde, 205mL of diethyl malonate, 610mL of absolute ethanol, 11mL of hexahydropyridine and 1-1.3ml of glacial acetic acid; (2) Under anhydrous conditions, in a water bath at 80°C, stir and reflux for 2.5 hours, then cool; (3) Add about 610mL of cold water (0°C), filter with suction after crystallization, and cool with 110mL of ice water (0°C) Wash twice with 50% ethanol to get 6,8-dichlorocoumarin-3-acidate or 6,8-dibromocoumarin-3-acidate; (4) add 6 , 8-dichlorocoumarin-3-condensate or 6,8-dibromocoumarin-3-condensate 128g and 103g sodium hydroxide, then add 510ml of absolute ethanol and 510mL of water, 80 ℃ water bath Under certain conditions, heat to reflux for about 2.5 hours; (5) After the reaction is completed, immed...

Embodiment 3

[0066] The difference between this embodiment and embodiment 2 is that

[0067] Step 1: Preparation of 6,8-dichlorocoumarin-3-carboxylic acid or 6,8-dibromocoumarin-3-carboxylic acid

[0068] (1) Add 210g of 3,5-dichlorosalicylaldehyde or 3,5-dibromosalicylaldehyde, 210mL of diethyl malonate, 615mL of absolute ethanol, 12mL of hexahydropyridine and 1-1.3ml of glacial acetic acid; (2) Under anhydrous conditions, stir and reflux for 3 hours in a water bath at 80°C, and cool; (3) Add about 615mL of cold water (0°C), filter with suction after crystallization, and cool with 115mL of ice water (0°C) Wash twice with 50% ethanol to obtain 6,8-dichlorocoumarin-3-acidate or 6,8-dibromocoumarin-3-acidate; (4) add 6, 132g of 8-dichlorocoumarin-3-condensate or 6,8-dibromocoumarin-3-condensate and 106g of sodium hydroxide, then add 515ml of absolute ethanol and 515mL of water, in a water bath at 80°C (5) Immediately after the reaction is completed, put it in an ice bath at 0°C, add concen...

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Abstract

The invention relates to the technical field of medical treatment. The tea double-chlorine carboxamide and tea double-bromine carboxamide are newly synthesized compounds which can inhibit growths and invasions of cancer cells such as lung cancer, breast cancer, liver cancer, stomach cancer, colon cancer, prostate cancer, pancreatic cancer, cervical cancer, lymphoma, leukemia, and melanoma, and can obviously inhibit the tumor growth and metastasis in the body, and the inhibition effect of the compound is better than that of an anticancer medicament; the mechanism of action involves a receptor which is closely related to down-regulation and inhibition of the growth, invasion and metastasis of a tumor, signal transduction and regulation protein and kinase levels and a binding of a nuclear factor and DNA (Deoxyribonucleic Acid), and up-regulation of factors such as tumor suppressor proteins and cell cycle inhibitor proteins simultaneously; double tea chlorine carboxamide and double tea chlorine carboxamide can directly inhibit activities of histone deacetylase and histone methyltransferase EZH2(Enhancer Of Zeste Homolog 2) and the binding of the inflammatory factor NF-kB and DNA, and the activities of tea double-chlorine carboxamide and tea double-bromine carboxamide are better than that of the clinical anti-cancer medicament. The invention provides new applications of tea double-chlorine carboxamide and tea double-bromine carboxamide and intermediate compounds in preventing and treating the diseases such as cancers, inflammation, cardiovascular and immune deficiencies.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to tea dichloro-aromatic amide (DTClC) and tea bisbromo-aromatic amide (DTBrC) and intermediate compounds 6,8-dichloro-3-carboxylic acid coumarin (DCLC) and 6 , the application of 8-dibromo-3-carboxylic acid coumarin (DBrC) in the preparation of disease inhibitors for the prevention and treatment of tumors, inflammation, cardiovascular and cerebrovascular diseases, and immunodeficiency. Background technique [0002] The abnormal growth, invasion and metastasis of malignant tumors such as human lung cancer, breast cancer, liver cancer, gastric cancer, colon cancer, prostate cancer, pancreatic cancer, cervical cancer and chronic leukemia, lymphoma and melanoma lead to the death of tens of thousands of patients every year It has become a major disease that seriously endangers human health. Due to the toxic and side effects of clinical chemotherapy and radiotherapy, the effective prev...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61K31/223A61P35/00A61P35/02A61P29/00A61P9/00A61P37/04
Inventor 张国营张颖
Owner YANTAI UNIV
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