Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Cytarabine derivatives and purposes thereof in resisting cancers and tumors

A technology of cytarabine and its derivatives, applied in the medical field, can solve problems such as toxicity, cytarabine cannot be used to treat liver cancer, slow

Active Publication Date: 2013-03-13
高峰 +1
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cytarabine derivatives and purposes thereof in resisting cancers and tumors
  • Cytarabine derivatives and purposes thereof in resisting cancers and tumors
  • Cytarabine derivatives and purposes thereof in resisting cancers and tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0093] 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.

[0094] Synthetic route 1:

[0095]

[0096] 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

[0097] 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 ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
purityaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/09A61K31/7068A61P35/00A61P35/02
Inventor 高峰徐峻
Owner 高峰
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com