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Diphenylaminopyridine type anti-tumor compound as well as preparation method and application thereof

A compound and anti-tumor technology, applied in the field of medicine, can solve the problems of limited application scope, toxic and side effects, etc.

Inactive Publication Date: 2018-05-18
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The discovery of the above drugs satisfies the EGFR to a certain extent T790M Drug-resistant patients need medication, but the above-mentioned drugs are all pyrimidine derivatives, have similar efficacy and pharmacological mechanism, and have certain toxic and side effects, so the scope of application is limited

Method used

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  • Diphenylaminopyridine type anti-tumor compound as well as preparation method and application thereof
  • Diphenylaminopyridine type anti-tumor compound as well as preparation method and application thereof
  • Diphenylaminopyridine type anti-tumor compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of embodiment 1 target molecule

[0044] Use Yantai Huanghai GF254 or Qingdao GF254 silica gel plate for thin-layer chromatography. 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 products is 0.4 mm-0.5mm.

[0045] 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.

[0046] Unless otherwise specified in the examples, the solution refers to an aqueous solution.

[0047] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.

[0048] The technical scheme that the present invention adopts is as follows:

[0049]

[0050] Synthetic route of compound (I). Reagents and conditions: (a) m-nitroaniline, DIP...

Embodiment 2

[0078] Example 2 Evaluation of Target Molecule Biological Activity

[0079] 1. In vitro test method for receptor tyrosine kinase inhibitory activity

[0080] Prepare Kinase Assay Buffer

[0081] ① Melt the Kinase Detection Buffer at room temperature and observe whether there is precipitation.

[0082] ②If 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.

[0083] Prepare Kinase Assay Reagents

[0084] ①Equilibrate Kinase Detection Buffer and Kinase Detection Substrate at room temperature before use.

[0085] 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.

[0086] 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 a diphenylaminopyridine type anti-tumor compound as well as a preparation method and application thereof. Specifically, the anti-tumor compound has a structure shown as a formula (I). The invention further relates to the application of the compound shown as the formula (I) or pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the compound to treatment of tumor diseases through inhibiting a wild type EGFR (Epidermal Growth Factor Receptor) and a mutant EGFRT790M epidermal factor receptor protein tyrosine kinase, and especially relates tothe application to the treatment of small cell lung cancer, non-small-cell lung cancer and EGFRT790M type mutant non-small-cell lung cancer; (The formula (I) is shown in the description.).

Description

technical field [0001] The invention relates to an antitumor compound and its preparation method and use. Specifically, the antitumor compound is a dianilinylpyridine compound, which belongs to the technical field of medicine. Background technique [0002] Targeted therapy for malignant tumors has greatly prolonged the survival period of cancer patients and significantly improved the quality of life of patients. The core of "molecular targeted therapy" is to target precise molecular "targets" and then apply small molecule drugs that can specifically bind to these targets. Protein tyrosine kinases (protein tyrosinekinase, PTKs) are important signal messengers of cell life activities, which can catalyze the transfer of the γ-phosphate group at the end of ATP to the substrate, and can catalyze the phosphorylation of tyrosine residues in various substrate proteins It plays an important role in cell proliferation, survival, apoptosis, metabolism, transcription and differentiatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/74C07D405/12A61K31/4433A61K31/5377A61K31/496A61P35/00
CPCC07D213/74C07D405/12
Inventor 马晓东爱民白悦王长远孟强唐泽耀孙慧君舒晓宏刘克辛
Owner DALIAN MEDICAL UNIVERSITY
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