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Application of 3, 4-dimethoxyphenyl-benzo [d] oxazole as tumor drug-resistant reversal agent

A drug resistance reversal and tumor technology, which is applied in the direction of antineoplastic drugs, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as the complex formation mechanism of MDR, improve tumor cell drug resistance, reduce drug toxicity, The effect of reducing dosage

Active Publication Date: 2020-07-31
无锡享源信息科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The formation mechanism of MDR is complex, in which the overexpression of ABC drug transport pump is the main reason for mediating MDR

Method used

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  • Application of 3, 4-dimethoxyphenyl-benzo [d] oxazole as tumor drug-resistant reversal agent
  • Application of 3, 4-dimethoxyphenyl-benzo [d] oxazole as tumor drug-resistant reversal agent
  • Application of 3, 4-dimethoxyphenyl-benzo [d] oxazole as tumor drug-resistant reversal agent

Examples

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Embodiment 1

[0038] In this example, the compound 4,6-di-tert-butyl-2-(3,4-dimethoxyphenyl)benzo[d]oxazole-7-ol (CAS: 175881- 00-2) as an example to illustrate its application as a transport pump inhibitor.

[0039] Cell culture: H460 / MX20 (non-small cell lung cancer drug-resistant cell line with high ABCG2 expression) was cultured in DMEM medium containing 10% fetal bovine serum and 1% penicillin-streptomycin, and the cells were maintained at 37°C containing 5 %CO 2 in a humid incubator.

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Abstract

The invention specifically relates to application of 3, 4-dimethoxyphenyl-benzo [d] oxazole as a tumor drug-resistant reversal agent. During the later period of tumor treatment, a main failure reasonof a chemotherapy regimen is from tumor cell drug resistance, and an existing related research indicates that a drug-resistant formation reason of a tumor cell is related to a medicine transport protein. The invention researches to indicate that 4, 6-di-tertiary butyl-2-(3, 4-dimethoxyphenyl) benzo [d] oxazole-7-ol can inhibit the transportation of associated proteins in tumor cells, the drug resistance of the tumor cells can be reversed, and the sensitivity of the tumor cell for a tumor-resistant drug can be improved. The invention can be used for the adjuvant therapy of the chemotherapy regimen and can be cooperated with other tumor-resistant drugs to jointly act, and the invention has a good clinical drug utilization meaning.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to 3,4-dimethoxyphenyl-benzo[d]oxazole compounds——4,6-di-tert-butyl-2-(3,4-dimethoxy The application of phenyl) benzo [d] oxazole-7-ol as tumor resistance reversal agent, and the 4,6-di-tert-butyl-2-(3,4-dimethoxyphenyl ) Application of the pharmaceutical composition of benzo[d]oxazole-7-ol 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] The high mortality rate of malignant tumors is often associated with drug resistance in the late stage of cancer, especially multidrug resistance (MDR). MDR refers to the cross-resistance of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/423A61K31/136A61P35/00A61P35/02C07D263/57
CPCA61K31/136A61K31/423A61P35/00A61P35/02C07D263/57A61K2300/00
Inventor 卢佳澳盛卸晃类红旭赵子婧
Owner 无锡享源信息科技有限公司