Antineoplastic active canthardin derivative and method for preparing same

A technology of anti-tumor activity and derivatives, applied in the field of medicine, can solve the problems of limiting the wide application of cannabinoid derivatives and being unsafe, and achieve the effects of good market prospects, safe raw materials and novel structures

Inactive Publication Date: 2008-04-16
GUANGDONG PHARMA UNIV +1
View PDF1 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent No. 200510034018.4 "Acanthin Derivatives and Its Preparation Method" provides a preparation method of cantharidin derivatives, but highly toxic potassium cyanide must be used, which is very unsafe
These factors largely limit the wide application of chiroin derivatives in medicine.

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
  • Antineoplastic active canthardin derivative and method for preparing same
  • Antineoplastic active canthardin derivative and method for preparing same
  • Antineoplastic active canthardin derivative and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] One, according to the synthetic route shown in Figure 6

[0047] (1) Add 1.13g of norcantharidin and 0.55g of glycine that are well ground and mixed into a 25ml round bottom flask, stop the reaction after 20 minutes in an oil bath at 180°C, cool and solidify, and recrystallize with 15ml of 1:4 ethanol aqueous solution to obtain white Needle crystals, yield 80%, mp 202-204°C. The spectral data of the product are:

[0048] IR (KBr, cm -1 ): v3466 (-COOH), 2978 (saturated C-H), 1733 (C=O), 1689 (five-membered lactam), 1418 (C-N), 1222 (C-O-C)

[0049] (2) Add 2g of the reaction product of step (1) and the rotor in the three-necked flask. The reaction device is as shown in Figure 4. A drying tube is installed at the top of the condenser tube, and a separatory funnel is installed at the other top. Add 8ml of thionyl chloride and 2 drops of N,N-dimethylformamide to the separatory funnel, add slowly in a cold water bath, and after the reaction is stable, raise the temperatu...

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 present invention discloses a novel cantharidin derivative with selective suppressive activity on tumor cells but low toxicity on human body. The present invention also discloses the preparation method of the cantharidin derivative, in which norcantharidin, glycin, and amantadine are adopted as the raw materials to synthesize the cantharidin through steps, and the preparation method is safe, simple and easily accomplishable. The cantharidin derivative with suppressive activity on tumor cells has smart structure and strong suppressive activity on tumor cells, fills in the gap in the field, makes the solid foundation for the preparation of cantharidin derivative which has selective suppressive activity on tumor cells and minor toxicity on human body, and has both potential significance on the industrialized exploit and great contribution to the research on human anti-tumor drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new canraoin derivative with antitumor activity and a preparation method thereof. Background technique [0002] Cantharidin (CA) is a natural defensive toxin widely present in more than 1500 species of cantharidin. Banao is an insect belonging to the Coralaceae family. It is cold in nature and pungent in taste. It is a highly toxic Chinese herbal medicine. In addition to its anti-cancer activity, it also has various activities such as anti-virus, aphrodisiac, and white blood cell increase. my country is the first country in the world to recognize the medicinal value of Banao. Its form, habit and usage are recorded in detail in "Compendium of Materia Medica". Canraoin, which is extracted from canopy or synthesized in the laboratory, is a kind of hemitenene toxin, which is highly toxic. Oral administration can cause gastrointestinal inflammation, mucosal necrosis, severe damag...

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): C07D491/18A61K31/407A61P35/00
Inventor 谭载友张浩曾胜梁可张志华黄彦王晓明
Owner GUANGDONG PHARMA UNIV
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