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Application of moving point motor protein small molecular inhibitor to inhibition of tumor cell proliferation

A tumor cell proliferation and motor protein technology, which is applied in the application field of small molecule inhibitor of motor protein in inhibiting tumor cell proliferation, and can solve the inactivation of spindle checkpoint, errors in chromosome movement and separation process, and chromosome aberrations. Stable phenotypes, etc.

Active Publication Date: 2013-10-23
姚雪彪 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Loss of CENP-E inactivates the spindle checkpoint, leading to errors in chromosome movement and segregation resulting in chromosomal instability phenotypes

Method used

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  • Application of moving point motor protein small molecular inhibitor to inhibition of tumor cell proliferation
  • Application of moving point motor protein small molecular inhibitor to inhibition of tumor cell proliferation
  • Application of moving point motor protein small molecular inhibitor to inhibition of tumor cell proliferation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Embodiment 1, the synthesis of target compound formula VII:

[0068]

[0069] (Formula XV) (Formula VII)

[0070] Add 1mmol 5a, the compound shown in 1.1mmol intermediate formula XV (its synthetic reference document Monatshefte fuer Chemie, 127 (5), 549-555,1996) in the three-necked flask, in 10ml THF, add 2mmol K under stirring 2 CO 3 , heated to reflux, monitored by TLC until the reaction was complete, cooled, filtered with suction, recovered the solvent under reduced pressure, dissolved the obtained residue in chloroform, washed with water, washed with saturated brine, and dried over anhydrous sodium sulfate. The solvent was recovered by suction filtration, and the residue was recrystallized from isopropanol / dichloromethane to obtain the pure product of the target compound of formula VII.

[0071] figure 1 It is the nuclear magnetic detection spectrogram of the pure product formula VII compound (named as Syntelin), A is the carbon spectrum, and B is the nitroge...

Embodiment 2

[0085] Embodiment 2, the synthesis of target compound formula III:

[0086]

[0087] (Formula XIV) (Formula III)

[0088] Add 1mmol 5b, the compound shown in 1.1mmol intermediate formula XIV (its synthetic reference Bioorganic & Medicinal Chemistry Letters 16 (17), 4444-4449, 2006) in the three-necked flask, in 10ml THF, add 2mmol K under stirring 2 CO 3 , heated to reflux, monitored by TLC until the reaction was complete, cooled, filtered with suction, recovered the solvent under reduced pressure, dissolved the obtained residue in chloroform, washed with water, washed with saturated brine, and dried over anhydrous sodium sulfate. The solvent was recovered by suction filtration, and the residue was recrystallized from isopropanol / dichloromethane to obtain the pure product of the target compound represented by formula III.

[0089] Wherein, compound 5b is prepared according to the following steps:

[0090] 1) Synthesis of intermediate 1b:

[0091]

[0092] For the syn...

Embodiment 3

[0102] Embodiment 3, the synthesis of target compound formula VIII:

[0103]

[0104] (Formula XV) (Formula VIII)

[0105] Add 1mmol 5a, the compound shown in 1.1mmol intermediate formula XV (its synthetic reference document Monatshefte fuer Chemie, 127 (5), 549-555,1996) in the three-necked flask, in 10ml THF, add 2mmol K under stirring 2 CO 3 , heated to reflux, monitored by TLC until the reaction was complete, cooled, filtered with suction, recovered the solvent under reduced pressure, dissolved the obtained residue in chloroform, washed with water, washed with saturated brine, and dried over anhydrous sodium sulfate. The solvent was recovered by suction filtration, and the residue was recrystallized from isopropanol / dichloromethane to obtain the pure product of the target compound formula VIII.

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Abstract

Disclosed are a small molecule inhibitor Syntelin against kinetochore motor protein CENP-E and use thereof. Provided is a small molecule organic compound that binds to the motor domain of CENP-E motor protein. The binding of the compound to CENP-E inhibits the movement of CENP-E motor protein along microtubules without influencing its interaction with microtubules. The compound can enter the cells to inhibit the function of CENP-E when added to a cell culture medium, leading to partial error in chromosome arrangement and maintaining the spindle checkpoint activity for a long period of time.

Description

technical field [0001] The invention relates to the application of small molecular inhibitors of motor protein in inhibiting tumor cell proliferation. Background technique [0002] The precise self-replication of cells is an important part of life activities, and the high conservation of replication plays an important role in the reproduction of organisms and species. During the process of cell replication, the parental genetic information contained in the chromosomes is equally and accurately distributed to the two daughter cells after undergoing many complex movements. Cell cycle events are carried out in a highly orderly manner, and the biochemical regulatory pathways that ensure the orderly progress of the cell cycle are called "checkpoints". [0003] Kinetochores are multicomponent protein complex structures located at centromeres. It not only directly maintains the connection between the spindle filament and the chromosome, but also regulates the temporal and spatial...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P35/00
CPCC07D495/04A61K31/675A61K31/519C07F9/6561A61P35/00A61P43/00
Inventor 姚雪彪杨志宏万卫红姚彧丁霞张健存
Owner 姚雪彪
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