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CTCF transcription factor inhibitor and application thereof

A technology of transcription factor and inhibitor, applied in the field of CTCF transcription factor inhibitor, to achieve good cancer cell toxicity activity and inhibit cancer cell metastasis effect

Active Publication Date: 2020-12-29
THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Among them, Sorafenib (Sorafenib) is a multi-targeted kinase inhibitor drug for liver cancer. By blocking the Ras / Raf / MEK / ERK signal transduction pathway, it simultaneously inhibits VEGFR (vascular endothelial growth factor receptor) and PDGFR (platelet Derived growth factor receptor) and other receptor tyrosine kinase activity, high selectivity, but there are still side effects such as fatigue, gastrointestinal reactions, rash, hair loss, etc.

Method used

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  • CTCF transcription factor inhibitor and application thereof
  • CTCF transcription factor inhibitor and application thereof
  • CTCF transcription factor inhibitor and application thereof

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Experimental program
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Embodiment approach

[0046] As a preferred embodiment, the active ingredient of the CTCF transcription factor inhibitor includes: compound I.

[0047] As another preferred embodiment, the active ingredient of the CTCF transcription factor inhibitor includes: compound I, and at least one of compound II, compound III, compound IV, compound V and compound VI. Combining different types of compounds with liver cancer cell toxicity can reduce the dosage of the drug, improve the efficacy of the drug, and avoid the toxic and side effects of a single drug on normal cells. In some embodiments, the active ingredients of the CTCF transcription factor inhibitor include: at least one of compound Ia to compound If, and at least one of compound II, compound III, compound IV, compound V and compound VI.

[0048] As yet another preferred embodiment, the active ingredient of the CTCF transcription factor inhibitor includes: compound I and compound VI, and at least one of compound II, compound III, compound IV and co...

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Abstract

The invention belongs to the technical field of biological medicine, and particularly relates to a CTCF transcription factor inhibitor and an application thereof. Active components of the CTCF transcription factor inhibitor provided by the invention comprise at least one of a compound I, a compound II, a compound III, a compound IV, a compound V and a compound VI, wherein R1 and R2 are respectively and independently selected from H, alkyl or alkoxy; R3 is selected from H, halogen or alkyl; and R4 is selected from H, hydroxyl or alkoxy. The CTCF transcription factor inhibitor regulates and controls the transcription expression of the CTCF transcription factor by inhibiting the combination of the CTCF transcription factor and DNA, has good cancer cell toxic activity, can effectively inhibitcancer cell metastasis, and has the potential of being applied to preparation of anti-cancer drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a CTCF transcription factor inhibitor and application thereof. Background technique [0002] Liver cancer, the full name of hepatocellular carcinoma (HCC), ranks fifth in the global cancer mortality rate, and in China, HCC is the third cancer with the highest mortality rate after gastric cancer and esophageal cancer. Due to the occult onset, high metastasis rate, and lack of specific early tumor markers of HCC, many patients are already in the middle and late stages of cancer when they see a doctor, and the mortality rate is as high as 50%. [0003] Traditional anti-liver cancer drugs lack targeting, and while killing cancer cells, they also cause varying degrees of damage to normal tissue cells. With the development of tumor molecular biology and translational medicine, antineoplastic drugs have developed from traditional cytotoxic drugs to non-cytotoxic drugs. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D261/14C07D513/04C07D417/12C07D277/46C07D333/38A61P35/00A61P35/04
CPCC07D487/04C07D261/14C07D513/04C07D417/12C07D277/46C07D333/38A61P35/00A61P35/04
Inventor 柯子斌马聪张雅晶陈颖祥张玉琴
Owner THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST