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Application of benzothiazoles and benzopyrroles in the preparation of antitumor drugs

An anti-tumor drug, benzothiazole technology, applied in the field of medicine, can solve problems such as benzothiazole and benzopyrrole compounds and their pharmaceutical compositions that have not been seen

Active Publication Date: 2020-08-14
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 relevant report about benzothiazoles and benzopyrroles and their pharmaceutical compositions in the preparation of Wee1 kinase inhibitors and antitumor drugs in the prior art

Method used

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  • Application of benzothiazoles and benzopyrroles in the preparation of antitumor drugs
  • Application of benzothiazoles and benzopyrroles in the preparation of antitumor drugs
  • Application of benzothiazoles and benzopyrroles in the preparation of antitumor drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The compound of the present invention was partially purchased from IBScreen, and the corresponding numbers of compounds I and II in the library are: STOCK1S-28804; STOCK6S-58881.

[0028] The structural formulas of compounds I and II are as follows:

[0029]

Embodiment 2

[0031] The half growth inhibitory concentration IC of the compound of the present invention on five different tumor cell lines 50 Determination of:

[0032] 1. Experimental principle and steps

[0033] MTS is an analog 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 culture medium. When testing, only a small amount of CellTiter Aqueous One Solution reagent is directly added to the medium of the culture plate well, incubated for 1-4h, and then read the absorbance value at 490nm with a microplate reader. The optical density OD (490nm) of the compound is directly proportional to the number of living cells. Cisplatin and paclitaxel were used as positive controls. Compound IC 50 The value is determined by calculation of the concentration effect growth curve.

[0034] Let stand for 90 minutes at room temperature to completely melt CellTiter Aq...

Embodiment 3

[0049] Compound I or II is added with 4% sulfuric acid ethanol solution, pH=4, filtered and dried to prepare sulfate compound.

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Abstract

The invention provides a benzothiazole and benzopyrrole compound, a pharmaceutical composition which takes the benzothiazole and benzopyrrole compound as an active ingredient,and application thereof in preparing a Weel kinase inhibitor and an anti-cancer drug. Weel is proved to combine with a DNA damage drug for strengthening anti-tumor activity of the benzothiazole and benzopyrrole compound. Theinvention also provides application of the benzothiazole and benzopyrrole compound in preparing the Weel kinase inhibitor. The compound is proved to have obvious anti-tumor cell proliferation activityaccording to in vitro anti-tumor cell activity screening experiment.

Description

Technical field [0001] The present invention relates to the technical field of medicine, in particular to benzothiazoles and benzopyrrole compounds, pharmaceutical compositions using them as active ingredients, and their application in the preparation of Wee1 kinase inhibitors, and their preparation in anti-tumor drugs In the application. Background technique [0002] Wee1 protein kinase was first found in fission yeast cells, belonging to the serine and threonine protein kinase family, highly conserved and widely present in eukaryotes. It is a cell cycle regulatory protein, which 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 complex of CDK1 and cyclin B (cyclinB) to achieve cell cycle regulation, and is important for DNA damage checkpoints Regulation effect. Wee1 protein kinase regulates mitosis through the action of three cell checkpoint...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/428A61K31/4439A61P35/00A61P35/02
CPCA61K31/428A61K31/4439A61P35/00A61P35/02A61K2300/00
Inventor 左之利李雅萍张树群刘兴勇李艳张利
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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