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

A technology of dinitrophenyl and drug resistance reversal, which is applied in the field of medical technology, can solve problems such as reducing the antitumor effect of drugs, and achieve good guiding significance.

Active Publication Date: 2021-02-26
无锡享源信息科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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

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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 medicines, and relates to an application of 3, 5-dinitrophenyl-pyrazolo [3, 4-d] [1,3] oxazine as a tumor drug resistance reversal agent. Researches show that 1-phenyl-6-(3, 5-dinitrophenyl)-pyrazolo[3, 4-d] [1, 3] oxazine-4(1H)-ketone can significantly improve the sensitivity of tumor cells to antitumor drugs and reverse the drug resistance of the tumor cells, and the treatment dosage is safe and non-toxic, so that the compound has potential to become a novel tumor drug resistance reversal agent. Based on the research results, the compound can be used for adjuvant therapy of a chemotherapy regimen and can be matched with other anti-tumor drugs for common medication, and has good clinical medication 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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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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