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Novel pyrimidine anti-tumor compound and preparation method and application thereof

A technology of compound and use, applied in the field of medicine

Inactive Publication Date: 2017-10-10
DALIAN MEDICAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tae226 has shown effective anti-proliferation and anti-tumor effects on a series of malignant tumors in vivo and in vitro experiments, and there is no report about its clinical trials (Schultze A., et al. Invest New Drugs, 2010, 28 (6) :825-33.)

Method used

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  • Novel pyrimidine anti-tumor compound and preparation method and application thereof
  • Novel pyrimidine anti-tumor compound and preparation method and application thereof
  • Novel pyrimidine anti-tumor compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The preparation of embodiment 1 target molecule

[0071] The thin-layer chromatography silica gel plate uses Yantai Huanghai HSGF254 or Qingdao GF254 silica gel plate, the specification of the silicon amine plate used in thin-layer chromatography (TLC) is 0.15mm-0.2mm, and the specification of thin-layer chromatography separation and purification product is 0.4 mm-0.5mm.

[0072] The raw materials used in the present invention are mainly purchased from Sinopharm Chemical Reagent Co., Ltd., Beijing Coup Technology Co., Ltd., Aladdin Chemical Reagent Co., Ltd., Darui Chemicals and other companies.

[0073] Unless otherwise specified in the examples, the solution refers to an aqueous solution.

[0074] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.

[0075] The technical scheme that the present invention adopts is as follows:

[0076]

[0077] Synthetic route, reagents and conditions of compound I-i: (d) ...

Embodiment 2

[0176] Example 2 Evaluation of Target Molecule Biological Activity

[0177] 1. In vitro test method for receptor tyrosine kinase inhibitory activity

[0178] (1) Preparation of Kinase Detection Buffer

[0179] ① Melt the Kinase Detection Buffer at room temperature and observe whether there is precipitation.

[0180] ②If precipitation occurs, incubate at 37°C (Kinase Detection Buffer) for 15 minutes and shake frequently to dissolve the precipitation. Alternatively, carefully aspirate the supernatant to remove the pellet.

[0181] (2) Preparation of Kinase Detection Reagent

[0182] ①Equilibrate Kinase Detection Buffer and Kinase Detection Substrate at room temperature before use.

[0183] ② Pour all the Kinase Detection Buffer into the brown bottle containing the Kinase Detection Substrate to dissolve the lyophilized powder substrate, thus making the Kinase Detection Reagent.

[0184] ③Gently oscillate, vortex or invert to mix to form a homogeneous solution, and the substr...

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Abstract

The invention relates to a novel pyrimidine anti-tumor compound and a preparation method and application thereof. The novel pyrimidine anti-tumor compound is a compound shown in a formula (I), wherein each substituted group in the formula (I) is defined in the description. The invention also relates to the compound shown in the formula (I) or a pharmaceutically acceptable salt thereof, or application of a medicine composition containing the compound in inhibiting focal adhesion kinase, further treating tumor diseases, and especially treating pancreatic cancers, lung cancers and breast cancers. The formula (I) is shown in the description.

Description

technical field [0001] The invention relates to a novel pyrimidine antitumor compound and its preparation method and application, belonging to the technical field of medicine. Background technique [0002] Protein tyrosine kinases (PTKs) regulate a series of physiological and biochemical processes such as cell growth, differentiation, and apoptosis by controlling cell signal transduction pathways. Receptor-type tyrosine kinases are a relatively large class of kinases that span cell membranes, possess a ligand-binding extracellular domain, a transmembrane domain, and act as kinases—in phosphorylating specific tyrosine residues and by This affects the intracellular domain of cell proliferation. Aberrant expression of these kinases has been found in common human cancers (eg, lung cancer, breast cancer, gastric cancer, ovarian cancer, lymphoma). Protein tyrosine kinase has become one of the important targets in the research and development of anticancer drugs. [0003] Focal ...

Claims

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Application Information

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IPC IPC(8): C07D295/15A61K31/5377A61P35/00
Inventor 马晓东王璐红袁宏吴斌赵婧媛李艳霞王长远刘克辛
Owner DALIAN MEDICAL UNIVERSITY
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