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Application of 3-[4-(sulfonyl)benzene] urea compound in preparation of medicine for tumour

A compound and urea technology, applied in the field of 3-[4-phenyl]urea compounds, can solve the problem of limitation and achieve the effect of proliferation inhibition

Inactive Publication Date: 2013-03-20
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, although several ROCK inhibitors have entered Phase I or Phase II clinical research (such as BA-210), there is only one ROCK inhibitor that has been successfully marketed, namely Fasudil, and it is limited to Japan. market

Method used

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  • Application of 3-[4-(sulfonyl)benzene] urea compound in preparation of medicine for tumour
  • Application of 3-[4-(sulfonyl)benzene] urea compound in preparation of medicine for tumour
  • Application of 3-[4-(sulfonyl)benzene] urea compound in preparation of medicine for tumour

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Analysis of 1-(3-chloro-4-fluorophenyl)-3-[4-(N-methylsulfonamido)phenyl]urea Enzyme inhibition activity assay of ROCK1. Enzyme inhibitory activity assay of ROCK1

[0028] Experimental principle: Invitrogen’s Z′-LYT technology was used to measure the ROCK1 inhibitory activity of the compound. This technology is based on the principle of fluorescence resonance energy transfer (FRET) and is based on the difference in sensitivity of phosphorylated and non-phosphorylated peptides to proteolytic cleavage. .

[0029] experimental method:

[0030] (1) Preparation of reagents. Kinase buffer: dilute 2ml of 5X kinase buffer to 10ml with water; compound: dilute the compound to be tested with water to a concentration gradient; ROCK kinase / substrate mixed solution: prepare 2250 μL of ROCK / substrate mixed solution; The concentration of enzyme is 10ng / ml, the concentration of substrate is 4μM, and the solvent is kinase buffer; phosphorylated peptide solution: add 2μL o...

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Abstract

The invention discloses application of a 3-[4-(sulfonyl)benzene] urea compound or a pharmaceutically acceptable salt thereof to the preparation of anti-lung cancer and anti-mammary cancer medicaments. The chemical structural formula of the 3-[4-(sulfonyl)benzene] urea compound is shown in the specifications, wherein X is O or S; R1 is an aromatic group containing a benzene ring or a mono-substituted benzaldehyde group; R4 is halogen; and R2 and R3 can be selected from hydrogen, alkyl with 1-4 carbon atoms, phenyl having 6-8 carbon atoms and containing 1-2 substitution groups or a chemical substance shown in the specifications. The 3-[4-(sulfonyl)benzene] urea compound or the pharmaceutically acceptable salt thereof has the functions of a ROCK inhibitor, has a remarkable inhibiting function on the proliferation of lung cancer cells and mammary cancer cells, and can be used for preparing anti-lung cancer and anti-mammary cancer medicaments.

Description

technical field [0001] The invention relates to a 3-[4-(sulfonyl)phenyl]urea compound and its application in the preparation of antitumor drugs. Background technique [0002] Cancer, namely malignant tumor, is currently the number one killer of human health. Statistics released by the Ministry of Health in 2010 show that malignant tumors have become the leading cause of death in China. Therefore, the treatment of cancer is urgent. Cancer is a multi-step process, generally involving the mutation of multiple genes; when the genes that regulate cell growth are mutated or damaged, the programmed cell death is inhibited, making the cells out of control, continuous growth and division, and tumors At the same time, the infiltration and metastasis of these cancer cells can accelerate the formation of tumor new capillaries. Among the most prevalent genetic variants that cause these defects is abnormal activation of the Ras family of GTPases. Mutations in Ras protein are found to ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/63A61P35/00
Inventor 侯廷军余慧东沈明云潘培辰李有勇周顺晔
Owner SUZHOU UNIV