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Application of amine derivative in preparation of anti-tumor medicine composition

A technology of amine derivatives and anti-tumor drugs, which is applied in the field of anti-tumor drugs to achieve good inhibitory activity, mild catalytic conditions, and reduce economic burden

Active Publication Date: 2021-11-19
GUANGXI UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no relevant research report on the anti-tumor biological activity or clinical application of N-(tert-butyl)-3-methyl-1,2,4-oxadiazol-5-amine derivatives

Method used

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  • Application of amine derivative in preparation of anti-tumor medicine composition
  • Application of amine derivative in preparation of anti-tumor medicine composition
  • Application of amine derivative in preparation of anti-tumor medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0035] Application of N-(tert-butyl)-3-methyl-1,2,4-oxadiazol-5-amine derivatives in the preparation of antitumor pharmaceutical compositions:

[0036] The chemical structural formula of the N-(tert-butyl)-3-methyl-1,2,4-oxadiazol-5-amine derivatives is as follows:

[0037]

[0038] Among them, R are:

[0039]

[0040]

[0041] The N-(tert-butyl)-3-methyl-1,2,4-oxadiazol-5-amine derivatives,

[0042] From N′-hydroxybenzimidamide and tert-butyl isocyanide via Pd(OAc) 2 (5mol%) catalytic synthesis, specifically comprises the following steps:

[0043] N′-hydroxybenzimidamide1a(0.2mmol),tert-butylisocyanide(0.3mmol),Pd(PPh 3 ) 4 (5mol%), K 2 CO 3 (3equiv.) reacted in toluene (1mL) at room temperature and pressure for 4 hours, the electron-deficient group (4-CF of hydroxybenzimidamide1a skeleton 3 , 4-F, 4-Cl 4-Br) and electron-rich groups (4-OMe, 4-Me, 3-Me, 2-Me, 3,4-dimethyl, 3,2-dimethyl) were reacted.

experiment example

[0045] In vitro anti-tumor cell activity test of N-(tert-butyl)-3-methyl-1,2,4-oxadiazol-5-amine derivatives:

[0046] 1. Cells and drugs:

[0047] Human liver cancer cell HepG-2, human lung cancer cell A549, human cervical cancer cell Hela, human breast cancer cell MDA-MB-231, human gastric cancer cell MKN45, and human malignant lymphoma cell NK-92 were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences;

[0048] Positive drug: 5-fluorouracil (5-Fu), purchased from Sigma Aldrich Company (St. Louis, MO, USA), with a purity >99.5% (HPLC).

[0049] 2. Experimental method

[0050] Take 5.0×10 tumor cells in the logarithmic growth phase 4 cells / mL inoculated into 96-well plate, 200 μL per well, 37°C and 5% CO 2 Cultivate under the condition for 24h;

[0051] Dissolve the test sample with dimethyl sulfoxide (DMSO), and then use fresh medium to prepare a sample culture solution with a final concentration of 2.5-20 μM, add it to a 96-well plate, and store it...

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PUM

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Abstract

The invention discloses application of an amine derivative in preparation of an anti-tumor medicine composition, and particularly relates to application of an N-(tert-butyl)-3-methyl-1, 2, 4-oxadiazole-5-amine derivative in preparation of an anti-tumor medicine composition. The N-(tert-butyl)-3-methyl-1, 2, 4-oxadiazole-5-amine derivative provided by the invention has a remarkable inhibition effect on liver cancer, lung cancer, cervical cancer, breast cancer, stomach cancer and lymph cancer, shows excellent anti-tumor characteristics, can be used as an anti-tumor lead drug molecule, and has a good development and application prospect in the aspect of developing anti-tumor drugs.

Description

【Technical field】 [0001] The invention relates to the technical field of antitumor drugs, and relates to the application of an amine derivative in the preparation of an antitumor drug composition, in particular to N-(tert-butyl)-3-methyl-1,2,4-oxadi Application of azole-5-amine derivatives in the preparation of antitumor pharmaceutical compositions. 【Background technique】 [0002] Tumor is a malignant abnormal hyperplasia caused by abnormal cell mutation or genetic variation, and the body loses its normal regulation of growth and reproduction. At present, with the increasing morbidity and mortality worldwide, the prevention and treatment of cancer has become a world public health focus of attention. The research and development of new anti-tumor drugs to save more patients suffering from cancer is the commanding heights of health that countries are competing for. [0003] At present, there have been many studies on antineoplastic drugs. For example, Chinese patent applicat...

Claims

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Application Information

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IPC IPC(8): A61K31/4245A61P35/00
CPCA61K31/4245A61P35/00
Inventor 玉万国汪煦梁妮
Owner GUANGXI UNIVERSITY OF TECHNOLOGY
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