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Alkoxyl terminal group oligo-PEG modified aminopyrimidine derivative and antitumor application

An alkyl compound technology, applied in the field of pyrazolo[3,4-d]pyrimidine derivatives, can solve the problems of low bioavailability, high toxicity and side effects, and low specificity, so as to promote apoptosis, Promising effect of inhibiting cell proliferation and clinical medicinal use

Active Publication Date: 2017-08-29
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are a variety of drugs for the treatment of cancer on the market, they all have various defects, such as low bioavailability, low specificity, and large toxic and side effects.
These defects are often caused by the structural characteristics of the compound itself and its target, and it is difficult to overcome it in further research and development.

Method used

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  • Alkoxyl terminal group oligo-PEG modified aminopyrimidine derivative and antitumor application
  • Alkoxyl terminal group oligo-PEG modified aminopyrimidine derivative and antitumor application
  • Alkoxyl terminal group oligo-PEG modified aminopyrimidine derivative and antitumor application

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Experimental program
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Effect test

Embodiment 1

[0042] The preparation of embodiment 1 compound of the present invention

[0043]

[0044] Compound 1 (269mg, 1mmol) was dissolved in 1,4-dioxane / water (4:1) 150ml solution, and transferred to a 250ml round bottom flask, and then added (1.38g, 10mol) to the reaction solution Potassium carbonate, after stirring at room temperature for three minutes, add the catalyst bis-diphenylphosphinoferrocene palladium chloride (73.1 mg, 0.1 mol), heat the reaction mixture to 100 ° C, detect the reaction by TLC, after the reaction is completed , first, after the reaction solution is cooled, add 50ml of distilled water, then transfer to a separatory funnel, add 100ml of dichloromethane to extract 3 times, combine the organic phases, add anhydrous sodium sulfate, spin dry the organic solvent, and separate through a silica gel column Intermediate compound 2 (200 mg, 70%) was obtained, (dichloromethane:(dichloromethane:methanol)=100:2.5).

[0045] 1 H NMR (600MHz, DMSO-6d) δ9.83(s, 1H, HOA...

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Abstract

The invention discloses a pyrazolo[3,4-d]pyrimidine derivative that is represented as the formula (I), which has significant growth inhibiting effect, apoptosis promoting effect and cell proliferation alleviating effect on tumor cells, can be used for preventing and / or treating tumor related diseases, and has wide application prospect.

Description

technical field [0001] The invention belongs to the field of compound drugs, in particular to pyrazolo[3,4-d]pyrimidine derivatives and applications thereof. Background technique [0002] Malignant tumors grow fast and show invasive growth, prone to hemorrhage, necrosis, ulcers, etc., and often have distant metastasis, resulting in body weight loss, weakness, anemia, loss of appetite, fever, and severe damage to organ functions, eventually causing The death of the patient poses a huge threat to the health and life of the crowd. [0003] Surgical treatment Radical resection is still the most basic and commonly used treatment for lung cancer, kidney cancer, liver cancer and other cancers. However, resection is usually traumatic, and it will cause damage to body tissues and loss of blood after surgery, so it is not suitable The elderly, those with poor physical fitness and those with heart, lung, liver and other important organ diseases are selected. Therefore, it is necessary...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P35/00
CPCC07D487/04
Inventor 何杨周兴龙柴莹莹李长富黄日东陈海陈勃江李为民
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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