Amine compound and application thereof to antitumor drug

A technology of amine compounds and anti-tumor drugs, applied in the field of amine compounds and their application in anti-tumor drugs, can solve the problems of mortality, patient and family burden, and high difficulty of treatment

Inactive Publication Date: 2018-04-13
窦玉玲
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Cancer is a malignant disease with a very high mortality rate. It is difficult to trea

Method used

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  • Amine compound and application thereof to antitumor drug
  • Amine compound and application thereof to antitumor drug
  • Amine compound and application thereof to antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] (1) Synthesis of 4-carbonylfuro[3,2-d]pyrimidine:

[0024]

[0025] Into a three-necked flask, add formamide (15 mL) and 2-carboxy-3-aminofuran (6.10 g, 48 mmol). The reaction mixture was then heated at 170 °C for 4-6 hours. The completion of the reaction was monitored by TLC; ice was added to the reaction mixture, resulting in a precipitate, which was filtered to obtain a solid, washed with water, redissolved in ethyl acetate, and dissolved in MgSO 4 After drying and concentration, 5.03 g of pure white solid furo-4-carbonyl[3,2-b]pyrimidine was obtained with a yield of 77%. 1 H-NMR (400 MHz, CDCl3) δ:7.09(d, 1H), 7.54(d, 1H), 7.89(s, 1H). 13 C-NMR (125 MHz, CDCl3) δ: 109.31, 120.49, 134.70, 143.12, 143.53, 151.34. LC-MS (ESI, pos, ion) m / z: 137[M+H].

[0026] (2) Synthesis of N-(4-chloro-3-(trifluoromethyl)phenyl)furo[3,2-d]pyrimidin-4-amine

[0027]

[0028] 5-Amino-2-chlorobenzotrifluoride (5.87g, 30mmol) was dissolved in methanol (50ml). Then 4-carbonylfu...

Embodiment 2

[0057] Example 2: Study on Bel-7402 Liver Cancer Transplanted Tumor Mouse Model

[0058] 1. Establishment of human liver cancer xenograft model in nude mice

[0059] SPF grade Balb / c nude mice, male, 4 weeks old, were transplanted into nude mice with human Bel-7402 liver cancer cells to form tumors, and then the nude mice were passaged for more than 2 generations. The tube needle was inoculated subcutaneously in the axilla of nude mice to establish a nude mouse xenograft cancer model of human liver cancer.

[0060] 2. Dosing regimen

[0061] Use a vernier caliper to measure the length and width of each animal tumor, according to the formula: V=1 / 2*ab 2 Calculate the tumor volume until the tumor volume grows to about 100mm 3 At the beginning of administration, all animals were randomly divided into model group, positive drug capecitabine group (400 mg / kg), high (100 mg / kg) and low (25 mg / kg) dose groups of the compound of the present invention according to tumor volume, with...

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PUM

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Abstract

The invention discloses an amine compound, the structure of which is , and discloses the synthesis route, synthesis steps and application of the amine compound in antitumor drugs. In vitro pharmacological experiments have found that the amine compound has inhibitory activity on various human cancer cells, and in vivo pharmacological experiments have a significant effect on reducing tumor weight in nude mouse xenograft cancer models of human liver cancer.

Description

technical field [0001] The invention belongs to the field of chemical drug synthesis and pharmacological activity, and relates to an amine compound and its application in antitumor drugs. Background technique [0002] Malignant tumor is one of the diseases that endanger human health, and it ranks at the forefront of the death rate of various diseases. Cancer is a malignant disease with a very high mortality rate. It is difficult to treat and has a high mortality rate, which brings a heavy burden to patients and families. According to relevant research reports, in the 1970s, cancer in my country increased from 10.13% to 22.32%, and the death rate increased by 82.11%. Cancer is the number one cause of death in cities and the second in rural areas. Currently, the top ten cancers in my country are: lung cancer, gastric cancer, colorectal cancer, liver cancer, esophageal cancer, female breast cancer, pancreatic cancer, lymphoma cancer, bladder cancer and thyroid cancer. Lung c...

Claims

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Application Information

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IPC IPC(8): C07D491/048A61P35/00A61P35/02
CPCC07D491/048
Inventor 窦玉玲
Owner 窦玉玲
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