Cytarabine prodrug derivatives and purposes thereof in resisting cancers and tumors

A technology of cytarabine and its derivatives, which is applied in the medical field and can solve problems such as metabolic failure, cytarabine cannot be used to treat liver cancer, and slow activation process

Active Publication Date: 2010-07-28
高峰 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Cytarabine generally cannot be used to treat liver cancer because its N4 amino group (see figure 1 ) is metabolized and causes toxicity; on the other hand, it is the O5 hydroxyl group on its glycoside structure (see figure 1 ) must be activated by phosphorylation, and this activation process is too slow in the liver

Method used

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  • Cytarabine prodrug derivatives and purposes thereof in resisting cancers and tumors
  • Cytarabine prodrug derivatives and purposes thereof in resisting cancers and tumors
  • Cytarabine prodrug derivatives and purposes thereof in resisting cancers and tumors

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Embodiment Construction

[0094] The synthesis routes of some representative cytarabine derivatives of the present invention are listed below, and other cytarabine derivatives in the patent of the present invention are synthesized by the same or similar methods.

[0095] Synthetic route 1:

[0096]

[0097] Synthesis of the first intermediate product B1 (route 1): Dissolve salicylic acid (13.8g, 100mmol) in 40 milliliters of butanediol, then add dropwise 5 drops of concentrated sulfuric acid, reflux reaction for 4 hours, decompression after the end of the reaction Evaporated to dryness, the first intermediate product B1 of gained is directly used in next step reaction

[0098] Synthesis of the second intermediate C1 (Route 1): The first intermediate B1 (2.1 g, 100 mmol) was dissolved in 10 mL of THF, then succinic anhydride (1.0 g, 100 mmol) and DMAP (1.2 g, 100 mmol) were added , stirred at room temperature for 24 hours, filtered the reaction solution, and evaporated the filtrate to dryness under ...

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Abstract

The invention relates to novel anti-tumor cytarabine prodrug derivatives through chemically modifying the N4 and O5 positions of cytarabine to prevent N4 amino being metabolized to lose efficacies and result in toxicity and let O5 hydroxy be easily phosphorylated for activation and introducing multifunctional groups of aspirins to the prodrug modules of the cytarabine to increase the drug functions for improving the anti-solid tumor activities. The invention also provides multiple synthesis routes of the cytarabine prodrug derivatives, a cytarabine prodrug derivative preparation and a preparation method thereof in detail and proves the purposes of the cytarabine prodrug derivatives at the aspect of resisting cancers and tumors through a great amount of experimental data. The cytarabine prodrug derivatives have a multi-targeting function and the advantages of increasing bioavailability, reducing multiple drug resistance and increasing solubility and ester dissolution.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to cytarabine derivatives and their synthesis route, the present invention also relates to preparations of cytarabine derivatives and their preparation methods and the anti-cancer and anti-cancer effects of cytarabine derivatives and their preparations. Use in tumors. Background technique [0002] Cancer is currently the most important disease that endangers human life and health. The existing methods for treating cancer mainly include: surgical resection, radiotherapy, chemotherapy or a combination of these methods. Chemotherapy is widely used and has been used in the treatment of many different types of cancer. However, most of the anticancer drugs used in chemotherapy are limited to delaying the progression of cancer so as to prolong the patient's life, and it is difficult to achieve the purpose of curing. Although the pathogenesis of various cancers is different, they...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/09A61K31/7068A61P35/00A61P35/02
Inventor 高峰徐峻
Owner 高峰
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