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Preparation and uses of a class of novel signal transducer and activator of transcription type3 (STAT3) inhibitors

A signal transduction and inhibitor technology, applied in organic active ingredients, medical preparations containing active ingredients, organic chemistry, etc., can solve the problems of difficult modification of natural compounds, easy to cause drug resistance, and no increase in biological activity of compounds

Inactive Publication Date: 2018-09-07
HENAN RADIOMEDICAL SCI & TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other STAT3 inhibitors reported in international related research include: STAT 21 (the biological activity of the second-generation optimized compound is not improved), STATTIC (there is no structural model of compound-protein interaction, and there is no way to start the structure optimization) and the Chinese University of Hong Kong. Cucurbitacin I that inhibits nasopharyngeal carcinoma (natural compound modification is difficult)
In short, the targets of targeted anticancer drugs currently used in clinical treatment tend to be upstream of the cell signal transduction pathway, which is likely to cause drug resistance, and the drug under development based on the STAT3 target can effectively overcome this weakness

Method used

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  • Preparation and uses of a class of novel signal transducer and activator of transcription type3 (STAT3) inhibitors
  • Preparation and uses of a class of novel signal transducer and activator of transcription type3 (STAT3) inhibitors
  • Preparation and uses of a class of novel signal transducer and activator of transcription type3 (STAT3) inhibitors

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Example 1: N-(3-((1H-1,2,4-triazole-5-)thio)-4-hydroxynaphthalene-1-yl)-4-bromobenzenesulfonamide (compound S060117) Synthesis

[0047]

[0048] Compound S060117

[0049] 1) Synthesis of N-(4-(4H)naphthyloneimine)-4-bromo-benzenesulfonamide:

[0050]

[0051] 4-Amino-1-naphthol hydrochloride (1.95g, 10mmol) solid was dissolved in 15ml of pyridine, 4-bromobenzenesulfonyl chloride (3.82g, 15mmol) was added, and the reaction was stirred for 5 hours; TLC detected that the reaction was complete, evaporated Pyridine was removed, the residual solid was washed with water and recrystallized from ethyl acetate to give a yellow solid as N-(4-hydroxy-1-naphthyl)-4-bromobenzenesulfonamide.

[0052]Disperse N-(4-hydroxy-1-naphthyl)-4-bromobenzenesulfonamide (3.76g, 10mmol) in 50ml of dichloromethane, add Ag 2 O (2.78g, 12mmol), stirred and reacted for 30 minutes, TLC detected that the reaction was complete, filtered, the filter cake was washed with dichloromethane, the filtr...

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Abstract

The invention belongs to the field of medical biology, and specifically provides a designing and preparing method of a class of effective signal transduction inhibition compounds for signal transducerand activator of transcription type3 (STAT3), and applications of the effective signal transduction inhibition compounds mainly in clinical treatment of breast cancer. According to the present invention, a variety of breast cancer cell lines have the abnormal intracellular STAT3 signaling system regulation mechanisms, and the compounds of the present invention can significantly inhibit the signaltransduction of STAT3 so as to provide the potential important significance in the clinical treatment and research of breast cancer.

Description

technical field [0001] The invention relates to the preparation of a signal transduction system inhibitor compound and its clinical application in treating cancer. Background technique [0002] Cancer has become one of the factors affecting the health of Chinese nationals and causing significant economic losses. Traditional cancer treatment methods - surgery, radiotherapy, chemotherapy and biological therapy have certain limitations in the control of cancer patients. In 2001, the advent of Gleevec, the first-generation targeted drug, brought new opportunities and hopes to the clinical treatment of cancer patients, and has the advantages of significant clinical efficacy and less toxic side effects. The only targeted drug independently developed in China for the treatment of non-small cell lung cancer - the biological target of icotinib attack is the epidermal growth factor receptor (EGFR), which is the same as the target of gefitinib for the treatment of non-small cell lung ...

Claims

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Application Information

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IPC IPC(8): A61K31/4196A61K31/4439A61K31/422C07D249/12C07D401/12C07D413/12A61P35/00A61P35/02
Inventor 徐学军卞龙骧王磊林昇徐红运赵媛
Owner HENAN RADIOMEDICAL SCI & TECH CO LTD
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