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Application of 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine as a tumor drug resistance reversal agent

A technology of dinitrophenyl and pyrazolo, which is applied in the field of medical technology, can solve the problem of reducing the anti-tumor effect of drugs, and achieve good guiding significance and safe use

Active Publication Date: 2021-12-03
无锡享源信息科技有限公司
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

ABCG2 transporter can pump anti-tumor drugs such as mitoxantrone, gefitinib, doxorubicin and imatinib from intracellular to extracellular, thereby reducing the anti-tumor effect of drugs

Method used

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  • Application of 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine as a tumor drug resistance reversal agent
  • Application of 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine as a tumor drug resistance reversal agent
  • Application of 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine as a tumor drug resistance reversal agent

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Effect test

Embodiment 1

[0040] The drug resistance reversal experiment of the compound of embodiment 1 to tumor cells

[0041] 1. Drug-resistant cell culture: S1-MI-80 cells are a MX-induced ABCG2 overexpression-resistant subline derived from the human colon cancer cell line S123. S1-MI-80 was cultured in DMEM medium. All cell lines were maintained at 37°C in 5% CO 2 in a humid incubator.

[0042] 2. Cytotoxicity testing: MTT colorimetric cell proliferation assay was used to determine drug sensitivity in in vitro cell models. Prepare a single-cell suspension and seed it on a 96-well plate at 160 μL per well in CO 2 After culturing in the incubator for 24 hours, add a series of concentrations (0, 1, 2, 4, 8, 18, 32 μmol / L) of 1-phenyl-6-(3,5-dinitrophenyl)-pyrazolo [3,4-d][1,3]oxazin-4(1H)-one. Add 20 μL of 0.5% MTT to each well and incubate for an additional 4 hours. The supernatant was then removed, and 150 μL of DMSO was added to each well to dissolve MTT crystals. The absorbance was detecte...

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Abstract

The invention belongs to the technical field of medicine and relates to the application of 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine as a tumor drug resistance reversal agent. Research of the present invention shows that 1-phenyl-6-(3,5-dinitrophenyl)-pyrazolo[3,4-d][1,3]oxazin-4(1H)-ketone can significantly improve The sensitivity of tumor cells to anti-tumor drugs can reverse the drug resistance of tumor cells, and the treatment dose is safe and non-toxic, which has the potential to become a new type of tumor drug resistance reversal agent. Based on the results of this study, the above-mentioned compounds can be used as adjuvant therapy of chemotherapy regimens and co-administered with other anti-tumor drugs, which has good clinical significance.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to 3,5-dinitrophenyl-pyrazolo[3,4-d][1,3]oxazine compounds——1-phenyl-6-(3, The application of 5-dinitrophenyl)-pyrazolo[3,4-d][1,3]oxazin-4(1H)-one as tumor resistance reversal agent, and including 1-phenyl-6 Application of a pharmaceutical composition of -(3,5-dinitrophenyl)-pyrazolo[3,4-d][1,3]oxazin-4(1H)-one in the preparation of antitumor agents. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Tumor multidrug resistance (multidrug resistance, MDR) has always been a worldwide problem that plagues cancer treatment. MDR refers to the long-term exposure of tumor cel...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5365A61P35/00A61P35/02A61K31/136A61K31/704
CPCA61K31/136A61K31/5365A61K31/704A61P35/00A61P35/02A61K2300/00
Inventor 类红旭盛卸晃赵子婧郝梦珠卢佳澳
Owner 无锡享源信息科技有限公司
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