Glutathione derivative and anti-tumor medical application thereof

A glutathione and anti-tumor drug technology, applied in anti-tumor drugs, tripeptide components, drug combinations, etc., can solve the problem of low activity of GlxII

Inactive Publication Date: 2010-03-03
SHANGHAI YUANNONG MEDICAL SCI
View PDF0 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the activity of GlxII in their tumor cells was low

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
  • Glutathione derivative and anti-tumor medical application thereof
  • Glutathione derivative and anti-tumor medical application thereof
  • Glutathione derivative and anti-tumor medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0018] Synthetic Irreversible Inhibitors of GlxI

[0019] The synthetic pathways of S-(bromoacetamidoalanylmethyl)glutathione (BPSG) and S-(bromoacetamidobutanylmethyl)glutathione (BBSG) are as follows:

[0020]

[0021] Dibromoacetyl(1,3)propylenediamine

[0022] Put 50 milliliters of chloroform and 1,3-propanediamine (13mmol) in the flask of 100 milliliters, then put into ice bath and wait for cooling, slowly drop bromoacetyl chloride (1.03g, 26mmol) under stirring condition , Continue to stir for half an hour after dripping. The solvent was evaporated to dryness with a rotary evaporator under reduced pressure to obtain a light brown crude product. Yield: 90%. 1 H NMR 300MHz (CDCl 3 , TMS) δ3.80 (4H, s, -C(O)CH 2 Br), 3.25 (4H, t, J=6.25Hz, -NHCH 2 CH 2 -), 1.85 (2H, p, J=6.25Hz, -NHCH 2 CH 2 -).ESI MS: (M(Br 79 )+H + ) 314.93. Dibromoacetyl (1,4) butanediamine

[0023] The synthetic pathway of this compound is roughly the same as that of dibromoacetyl (1,3) p...

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

No PUM Login to view more

Abstract

The invention belongs to the technical field of medicaments, and discloses anti-tumor medicaments of S-(bromo-acetamido-alanyl-methyl) glutathione and S-(bromo-acetamido-butaminoacyl-methyl) glutathione. The compound reacts with aldoketomutase I in a covalent bond mode so that the aldoketomutase I losses the activity irreversibly. The compound has good development and application prospects in theaspects of medicaments for treating the malignant tumors of prostate cancer, lung cancer, intestinal cancer, testicular cancer, leukemia, mammary cancer, skin cancer and the like.

Description

technical field [0001] Many drugs currently used clinically or under development rely on direct or indirect inhibition of DNA and / or protein to achieve the purpose of attacking tumor cells. Therefore, rapidly dividing normal cells, such as the intestinal epithelium and bone marrow, are also adversely affected to produce strong side effects. This technology invention describes a unique small molecule anti-tumor compound, which does not depend on cell division and differentiation, but acts on the glyoxalase system to cause programmed death of tumor cells, which can greatly reduce toxic and side effects. [0002] The human body's sugar metabolism inevitably produces a toxic compound called methylglyoxal, which can cause programmed cell death. During the long-term evolution process, the human body has developed a system called glyoxalase, which is composed of glyoxalase I (glyoxalase I, GlxI for short) and glyoxalase II (glyoxalase II, GlxII for short). Detoxification effect of ...

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 Applications(China)
IPC IPC(8): A61K38/06A61P35/00
Inventor 郑哲彬
Owner SHANGHAI YUANNONG MEDICAL SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap