Application of compound in preparing anti-tumor medicament

A leukemia and drug technology, applied in the field of compounds, can solve the problems of no research on ROCK protein, no anti-tumor activity, no discovery of biomedicine or related uses, etc.

Inactive Publication Date: 2013-09-18
深圳瀜新生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It is only one of the products of Chembridge's compound library, and no biomedicine or related applications have been found, and no studies have shown that the compound has the ability to inhibit ROCK protein, nor has it shown any anti-tumor activity

Method used

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  • Application of compound in preparing anti-tumor medicament
  • Application of compound in preparing anti-tumor medicament
  • Application of compound in preparing anti-tumor medicament

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0017] The present invention finds that 4-quinolinyl (5-vinyl-1-azabicyclo[2.2.2]octane-2-yl)methanone may inhibit ROCK1 protein through its own virtual screening software based on molecular docking active.

[0018] Through follow-up experiments, it was proved that it does have good ROCK1 protein inhibitory activity.

[0019] The present invention will be further described below in conjunction with experiments and experimental data.

[0020] Enzyme inhibitory activity assay of ROCK1

[0021] Experimental principle: Invitrogen’s Z′-LYTE was used to measure ROCK1 inhibitory activity TM technology, which is based on the principle of fluorescence resonance energy transfer (FRET), based on the difference in susceptibility of phosphorylated and non-phosphorylated peptides to proteolytic cleavage.

[0022] experimental method:

[0023] (1) Preparation of reagents. Kinase buffer: dilute 2ml of 5X kinase buffer to 10ml with water; compound: dilute the compound to be tested with w...

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PUM

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Abstract

The invention discloses application of compound in preparing an anti-tumor medicament. Computer screening and in vivo and in vitro activity tests on a compound indicate that the compound 4-quinolyl (5-vinyl-1-azabicyclo[2.2.2]octane-2-yl) ketone has a strong inhibition effect to ROCK (rho-associated protein kinase) I, has a remarkable inhibition effect to proliferation to breast cancer and leukemia cells, has small cell toxicity and good developing prospect, and is expected to be developed into a novel ROCK protein inhibitor, in particular a ROCK I protein inhibitor. The compound can be expected to be developed into a novel anti-tumor medicament, in particular a novel medicament for treating leukemia and breast cancer.

Description

technical field [0001] The present invention relates to a new application of a compound, in particular to the use of 4-quinolinyl (5-vinyl-1-azabicyclo[2.2.2]octane-2-yl)methanone in the preparation of anticancer drugs, especially It is an application in the preparation of anti-breast cancer and leukemia 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 capi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/49A61P35/00A61P35/02
Inventor 侯廷军余慧东沈明云潘培辰
Owner 深圳瀜新生物科技有限公司
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