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Application of NF-kB inhibitor in preparing anti-lung cancer medicine

A technology of anti-lung cancer drugs and inhibitors, which is applied in the field of medicine and can solve problems such as large toxicity

Inactive Publication Date: 2019-03-12
WENZHOU MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, EF24 has greater toxicity, which may be one of the factors limiting the clinical development of EF24

Method used

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  • Application of NF-kB inhibitor in preparing anti-lung cancer medicine
  • Application of NF-kB inhibitor in preparing anti-lung cancer medicine
  • Application of NF-kB inhibitor in preparing anti-lung cancer medicine

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Embodiment Construction

[0038] see Figure 1 to Figure 7 , the application of a NF-κB inhibitor disclosed in the present invention in the preparation of anti-lung cancer drugs provides a pharmaceutical composition for treating lung cancer, which contains a therapeutically effective amount of the NF-κB inhibitor as an active ingredient Any one or more of the agents or their pharmaceutically acceptable salts and pharmaceutical excipients.

[0039] Active compounds with high efficiency and low toxicity were screened out from various NF-κB inhibitors. The molecular mechanism by which the active compound exerts its anti-lung cancer effect was studied. Active compounds can inhibit NF-κB pathway to induce apoptosis and pyroptosis to exert anti-lung cancer effect.

[0040] Specifically, the present invention designs and synthesizes three kinds of NF-κB inhibitors (compound 6d, compound 7d, compound 13d), and the structures of other reference compounds are as follows:

[0041]

[0042] Among them, the m...

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Abstract

The invention discloses application of an NF-kB inhibitor in preparing an anti-lung cancer medicine. The NF-kB inhibitor is prepared from a medicine compound used for treating lung cancer, wherein themedicine compound contains therapeutically effective amounts of active component and medical auxiliaries, the active component at least contains one of three NF-kB inhibitors of a compound 6d, a compound 7d and a compound 13d, and by inhibiting an NF-kB pathway, cell apoptosis and pyroptosis are induced to treat lung cancer. By modifying an N group on an EF24 framework, multiple efficient NF-kB inhibitors are found, wherein the toxicity of the active compound 13d is obviously lower than that of EF24. By studying an anti-lung cancer mechanism of the active compound 13d, the fact that the active compound 13d can have an excellent anti-lung cancer effect by inhibiting the NF-kB signal pathway to induce cell apoptosis and pyroptosis is found, so that the NF-kB inhibitor 13d is expected to become the efficient low-toxicity anti-lung cancer targeted therapy medicine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of an NF-κB inhibitor in the preparation of anti-lung cancer drugs. Background technique [0002] Because targeted drugs can partially overcome the defects of chemotherapy drugs and have the advantages of high efficiency and low toxicity, they have become a hot spot in anti-tumor research. The NF-κB signaling pathway has been reported to be continuously activated in lung cancer cells, and the abnormally activated NF-κB pathway is involved in the occurrence and development of lung cancer. NF-κB is expected to be an effective target for the treatment of lung cancer. [0003] EF24 is currently a "star drug" for anti-tumor research. EF24 has also been reported to inhibit the activation of NF-κB, induce apoptosis and play an anti-tumor role. However, EF24 has high toxicity, which may be one of the factors limiting the clinical development of EF24. [0004] Therefo...

Claims

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Application Information

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IPC IPC(8): A61K31/4412A61P35/00
CPCA61K31/4412A61P35/00
Inventor 李物兰陈丽坪吴建章冯雨傲郑智伟
Owner WENZHOU MEDICAL UNIV
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