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Anti-tumor compound, and preparation method and purpose thereof

A compound and anti-tumor technology, applied in the field of medicine, can solve problems such as poor resistance to drugs

Inactive Publication Date: 2017-09-26
FIRST AFFILIATED HOSPITAL OF DALIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs inevitably have the problem of poor drug resistance

Method used

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  • Anti-tumor compound, and preparation method and purpose thereof
  • Anti-tumor compound, and preparation method and purpose thereof
  • Anti-tumor compound, and preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation of embodiment 1 target molecule

[0030]Use Yantai Huanghai GF254 or Qingdao GF254 silica gel plates for thin-layer chromatography. The specifications of the silicon amine plates used in thin-layer chromatography (TLC) are 0.15mm-0.2mm, and the specifications used for thin-layer chromatography separation and purification products are 0.4 mm-0.5mm.

[0031] 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.

[0032] Unless otherwise specified in the examples, the solution refers to an aqueous solution.

[0033] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.

[0034] The technical scheme that the present invention adopts is as follows:

[0035]

[0036] Synthetic route of compound (I). Reagents and conditions: (a) p-nitroa...

Embodiment 2

[0055] Example 2 Evaluation of Target Molecule Biological Activity

[0056] 1. In vitro test method for receptor tyrosine kinase inhibitory activity

[0057] Prepare Kinase Assay Buffer

[0058] ① Melt the Kinase Detection Buffer at room temperature and observe whether there is precipitation.

[0059] ② If precipitation occurs, incubate Kinase Detection Buffer at 37°C for 15 minutes and shake frequently to dissolve the precipitation. Alternatively, carefully aspirate the supernatant to remove the pellet.

[0060] Prepare Kinase Assay Reagents

[0061] ①Equilibrate Kinase Detection Buffer and Kinase Detection Substrate at room temperature before use.

[0062] 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.

[0063] ③Gently oscillate, vortex or invert to mix to form a homogeneous solution, and the substrate should be dissolved within...

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Abstract

The invention relates to an anti-tumor compound, and a preparation method and a purpose thereof. The anti-tumor compound is concretely of a structure shown by a formula I. The invention also relates to a purpose of the compound shown by the formula I or a pharmaceutically acceptable salt of the compound or a medicine composition containing the compound for treating tumor diseases, particularly for treating non-small cell lung cancer and small cell lung cancer through inhibiting EGFR, mutant EGFRT790M skin factor receptor protein tyrosine kinase and FAK focal adhesion kinase. The formula I is shown in the specification.

Description

technical field [0001] The invention relates to an anti-tumor compound and its preparation method and application. Specifically, the anti-tumor compound is a pyrimidine compound and belongs 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/48A61K31/5377A61P35/00
CPCC07D239/48
Inventor 李艳霞刘卓冯敏张文涵刘文娟张赢张杰张中和
Owner FIRST AFFILIATED HOSPITAL OF DALIAN MEDICAL UNIV
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