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Thiopyrimidine heterocycle anti-tumor compounds 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 range, toxic and side effects, etc.

Active Publication Date: 2018-10-16
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-mentioned drugs meets the medication needs of EGFR-T790M drug-resistant patients to a certain extent, but the above-mentioned drugs are all pyrimidine derivatives, have similar drug effects and pharmacological mechanisms, and have certain toxic and side effects, so the scope of application is limited

Method used

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  • Thiopyrimidine heterocycle anti-tumor compounds as well as preparation method and application thereof
  • Thiopyrimidine heterocycle anti-tumor compounds as well as preparation method and application thereof
  • Thiopyrimidine heterocycle anti-tumor compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of Target Molecules

[0039] 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.

[0040] 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.

[0041] Unless otherwise specified in the examples, the solution refers to an aqueous solution.

[0042] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.

[0043] The technical scheme that the present invention adopts is as follows:

[0044]

[0045] Synthetic routes of compounds (I-1), (I-2), (I-3). Reagents and conditions:...

Embodiment 2

[0058] Example 2 Evaluation of biological activity of target molecule

[0059] 1. In vitro test method for receptor tyrosine kinase inhibitory activity

[0060] Prepare Kinase Assay Buffer

[0061] ① Melt the kinase assay buffer at room temperature and observe whether there is precipitation.

[0062] ②If precipitation occurs, incubate Kinase Assay Buffer at 37°C for 15 minutes with frequent shaking to dissolve the precipitate. Alternatively, carefully aspirate the supernatant to remove the pellet.

[0063] Prepare Kinase Assay Reagents

[0064] ①Equilibrate Kinase Assay Buffer and Kinase Assay Substrate at room temperature before use.

[0065] 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.

[0066] ③Gently oscillate, vortex or invert to mix to form a homogeneous solution, and the substrate should be dissolved within 1 minute.

[...

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Abstract

The invention relates to thiopyrimidine heterocycle anti-tumor compounds as well as a preparation method and an application thereof. The anti-tumor compounds specifically have the structure shown in aformula (I). The invention also relates to the compounds shown in the formula (I), pharmaceutically acceptable salts of the compounds or pharmaceutical composition containing the compounds. The pharmaceutical composition can treat tumor diseases by inhibiting wild type EGFR (epidermal growth factor receptor) and mutant type EGFR-T790M PTK (protein tyrosine kinase) and is particularly applied to treatment of small cell lung cancer, non-small cell lung cancer and EGFR-T790M mutant type non-small cell lung cancer.

Description

technical field [0001] The invention relates to an antitumor compound and its preparation method and application. Specifically, the antitumor compound is a thiopyrimidine heterocyclic 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 tyrosine kinases, 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 tyrosine residues of various substrate proteins Phosphorylation, thereby transmitting signals, plays an important role in cell proliferation, survival, apoptosis, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/48C07D239/47A61K31/5377A61P35/00
CPCA61P35/00C07D239/47C07D239/48
Inventor 舒晓宏迟富云杨松马晓东李传刚李宏吴茉莉甄宇红刁云鹏宋丹阳李慧金俊美
Owner DALIAN MEDICAL UNIVERSITY
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