Trityl compound and its preparation method and application
A compound and drug technology, applied in medicine, small molecule inhibitor trityl compound and its preparation field, can solve the problems affecting tumor formation and inactivation, and achieve the effect of inhibiting tumor occurrence and development
Active Publication Date: 2018-04-03
PEKING UNIV
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Problems solved by technology
The inventor's previous research found that PTEN can dephosphorylate the spindle kinesin Eg5 and make it inactive, thereby affecting the formation of tumors
Method used
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Embodiment 1
Embodiment 2
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The present invention relates to trityl compounds and their preparation methods and applications, in particular to small molecule inhibitors of spindle kinesin Eg5 trityl compounds and their preparation methods, and the preparation of the compounds for the prevention or treatment of anti-tumor application in medicines. The compound is a compound of formula I or a compound of formula II. The compounds of the present invention increase the interaction between the compound and amino acid residues by specifically targeting the allosteric pocket of the spindle kinesin Eg5, thereby enhancing the activity of inhibiting Eg5. The compound of the present invention has effective inhibitory effect on cell proliferation and cell cycle-specific induction effect on apoptosis of cancer cells.
Description
Trityl compound and its preparation method and application technical field The present invention relates to trityl compounds and their preparation methods and applications, in particular to small molecule inhibitors of spindle kinesin Eg5 trityl compounds and their preparation methods, and the preparation of the compounds for the prevention or treatment of anti-tumor The application in the medicine of the present invention belongs to the field of biotechnology. Background technique At present, cancer has become the greatest threat to human health, and there is an urgent need to develop new anti-tumor drugs. PTEN is a recognized tumor suppressor factor, which is involved in the conduction of PTEN / PI3K / Akt pathway, so that cells stop dividing and enter programmed death, thereby preventing uncontrolled cell growth and limiting tumor formation. Spindle kinesin Eg5 also plays an important role in cell mitosis. It has been reported that overexpression of Eg5 can cause genome in...
Claims
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IPC IPC(8): C07H19/167C07H1/00C07C43/23C07C41/16A61P35/00
Inventor 尹玉新王玉飞周德敏杨振军
Owner PEKING UNIV
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