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Antitumor drug and preparation method thereof

A pharmaceutical and prodrug technology, applied in the field of medicine, can solve problems such as unsatisfactory curative effect, difficulty in obtaining therapeutic effect, and damage to patient immunity

Inactive Publication Date: 2019-01-04
GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no effective drug that can cure most cancer patients. Although chemotherapy drugs have a certain effect on cancer, they have large toxic and side effects. The curative effect of Chinese patent medicines on cancer is generally low and the curative effect is not ideal
At present, most of the anticancer drugs in clinical application are cytotoxic drugs. While inhibiting the proliferation of tumor cells, the proliferation of normal cells in the body is also inhibited, such as hematopoietic stem cells, which will lead to damage to the hematopoietic function of the bone marrow, and low levels of red blood cells or white blood cells. It inhibits the proliferation of tumors, but it also destroys the immunity of patients, and it is difficult to achieve good therapeutic effects in the end, which also limits the clinical application of chemotherapy drugs.

Method used

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  • Antitumor drug and preparation method thereof
  • Antitumor drug and preparation method thereof
  • Antitumor drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: the synthesis of compound 1

[0055]

[0056] Step 1: 2H-benzo[d][1,2,3]triazol-4-amine (10mmol) and 2-(bromomethyl)benzo[d]thiazole (10mmol), potassium carbonate (20mmol) The aqueous solution and 100ml of ethanol were added into a round-bottomed flask, stirred and heated to reflux under nitrogen protection, and reacted overnight. After the reaction solution was cooled and filtered, 200ml of ethyl acetate was added, then washed with water, and the organic layer was dried over anhydrous sodium sulfate. After the solvent was evaporated under reduced pressure, it was separated by silica gel column chromatography (petroleum ether:ethyl acetate=20:1) to obtain Intermediate 2-(benzo[d]thiazol-2-ylmethyl)-2H-benzo[d][1,2,3]triazol-4-amine 2.08g, yield 74.2%. ESI-MS: 282.34[M+H] +

[0057] Step 2: Add 2-(benzo[d]thiazol-2-ylmethyl)-2H-benzo[d][1,2,3]triazol-4-amine (5mmol), 4-isocyanato- 1-Methylpiperidine (5 mmol) was dissolved in 100 ml of dichloromethane...

Embodiment 2

[0062] Embodiment 2: the synthesis of compound 2

[0063]

[0064] Step 1: Mix 2H-benzo[d][1,2,3]triazol-4-amine (10mmol) and 2-(bromomethyl)-5,6-dimethoxybenzo[d]thiazole (10mmol), an aqueous solution of potassium carbonate (20mmol), and 100ml of ethanol were added into a round-bottomed flask, stirred and heated to reflux under nitrogen protection, and reacted overnight. After the reaction solution was cooled and filtered, 200ml of ethyl acetate was added, then washed with water, and the organic layer was dried over anhydrous sodium sulfate. After the solvent was evaporated under reduced pressure, it was separated by silica gel column chromatography (petroleum ether:ethyl acetate=30:1) to obtain Intermediate 2-(5,6-dimethoxy-benzo[d]thiazol-2-ylmethyl)-2H-benzo[d][1,2,3]triazol-4-amine 2.34g , yield 69.3%. ESI-MS: 341.39[M+H] +

[0065] Step 2: 2-(5,6-dimethoxy-benzo[d]thiazol-2-ylmethyl)-2H-benzo[d][1,2,3]triazol-4-amine (5 mmol), 1-(4-isocyanatopiperidin-1-yl)ethano...

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Abstract

The invention relates to an antitumor drug which benzotriazole compounds. The antitumor drug has the advantages that the compounds have a good proliferation inhibition effect on human hepatocellular carcinoma cell lines Hep G2 and Hep 3B, and human gastric cancer cell lines SGC-7901 and HS-746T, and the proliferation inhibition is not inferior to sorafenib; part of compounds even have far more inhibitory activity than the sorafenib; the antitumor drug can be used for treating various cancers, especially liver cancer and stomach cancer.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to a medicine for antitumor, and the invention also relates to a preparation method of the medicine. Background technique [0002] Tumor is a frequently-occurring and common disease that seriously threatens human health. The morbidity and mortality have been on the rise, and it has become the first fatal disease. Cancer is a malignant tumor. There are about 1.6 million new cases of cancer in my country every year, and about 1.3 million people die of cancer every year. The number of deaths from cancer in the country is increasing year by year. my country is a high-incidence area for liver cancer, gastric cancer, lung cancer and other cancers. / about 10,000. [0003] At present, there is no effective drug that can cure most cancer patients. Although chemotherapy drugs have a certain effect on cancer, they have large toxic and side effects. Chinese patent medicines gene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/14A61K31/454A61P35/00
CPCA61P35/00C07D417/14
Inventor 薛娟杨欣李亚辉
Owner GUIYANG COLLEGE OF TRADITIONAL CHINESE MEDICINE
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