Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy

A technology of tetrahydropyridine and its composition, which is applied in the field of medicine, and can solve problems such as unseen and no reports on the application of pharmaceutical compositions

Active Publication Date: 2020-07-17
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no report on the pharmaceutical composition of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compounds as active ingredients in the prior art, nor Application report of the compound and its pharmaceutical composition in the preparation of Wee1 kinase inhibitors and antitumor drugs

Method used

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  • Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy
  • Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy
  • Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy

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Embodiment 1

[0024] The compound of the present invention was purchased from specs company in the Netherlands (website: http: / / www.specs.com / ), and its database number is: AO-476 / 42169315.

Embodiment 2

[0026] Compound 1 of the present invention is to the mensuration of the half growth inhibitory concentration IC50 of five different tumor cell lines:

[0027] 1. Experimental principle and steps

[0028] MTS is an analogue of MTT. The succinate dehydrogenase in the mitochondria of living cells can metabolize and reduce MTS to generate soluble formazan (Formazan) compounds, which can be directly dissolved in the medium. When detecting, only a small amount of CellTiter Add Aqueous One Solution reagent directly to the culture medium in the wells of the culture plate, incubate for 1-4 hours, and then read the absorbance value at 490nm with a microplate reader. The optical density OD (490nm) value of the compound is directly proportional to the number of living cells. Cisplatin and paclitaxel were used as positive controls. The IC50 values ​​of compounds were determined by calculating concentration-effect growth curves.

[0029] Let stand at room temperature for 90 minutes to ...

Embodiment 3

[0039] Compound 1 was added with 4% sulfuric acid ethanol solution, pH = 4, filtered and dried to prepare sulfate compound 1.

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Abstract

The invention provides a pharmaceutical composition using tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound as an active ingredient, and application thereof in the preparation of Wee1 small-molecular inhibitor. Wee1 kinase serves as a candidate drug target for tumor treatment; it is possible to enhance the antitumor activity of the Wee1 kinase by the joint use of its inhibitors with certain chemotherapy drugs. Up to now, and there is only one Wee1 small-molecular inhibitor is under clinical test phase; in-vitro antitumor activity screening shows that the compound of the invention shows good inhibitory activity for five different tumor strains. The compound is applicable to the development of novel Wee1 small-molecular inhibitors, a new choice is provided for the field of tumor treatment, and the compound has good applicable value.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular to a tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound, and a pharmaceutical combination containing the compound as an active ingredient. compound, and the application of the compound and pharmaceutical composition in the preparation of anticancer drugs for inhibiting the overexpression of Wee1 kinase. The compound has an inhibitory effect on tumor cell lines and can be used as a lead compound for developing new antitumor drugs. Background technique [0002] Wee1 protein kinase was first discovered in fission yeast cells, belongs to the serine and threonine protein kinase family, is highly conserved and widely exists in eukaryotes. It is a cell cycle regulatory protein that is mainly activated in the S phase or G2 / M phase of the cell cycle. It can regulate the phosphorylation state of cyclin-dependent kinase 1 (CDK1), thereby regulating the activity of the com...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519C07D495/12A61P35/00A61P35/02
CPCA61K31/519C07D495/12
Inventor 左之利李雅萍张树群杨静张利刘兴勇
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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