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

Fascaplysin derivative as well as preparation method and application

A compound and drying technology, applied in the fields of drug combination, organic chemistry, antitumor drugs, etc., can solve the problems of fascaplysin's high cytotoxicity, limited clinical application, large toxic and side effects, etc., and achieves low price, good water solubility and short preparation route. Effect

Inactive Publication Date: 2018-04-10
南通杏睿生物科技有限公司
View PDF2 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This chimerism makes fascaplysin have high cytotoxicity and side effects, which seriously limit its clinical application

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
  • Fascaplysin derivative as well as preparation method and application
  • Fascaplysin derivative as well as preparation method and application
  • Fascaplysin derivative as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0017] 1. Preparation of compounds

[0018] (1) Preparation of the compound of formula (I)

[0019]

[0020] 1. Weigh 2mmol of tryptamine and dissolve it in 20ml of water, stir at room temperature, add 3mmol of concentrated sulfuric acid drop by drop, the solution is clarified, take 20mmol of 40% acetaldehyde solution, dissolve it in 5ml of water and slowly add it into the reaction solution, stir at room temperature for 30min, 100 Reflux at ℃ for 7 hours, cool the reaction solution to room temperature, adjust the pH to 10 with aqueous sodium hydroxide solution, extract with dichloromethane, combine the organic phases, rinse with brine, dry with anhydrous sodium sulfate, filter and distill under reduced pressure, and purify through a chromatographic column (Dichloromethane:petroleum ether:methanol=5:2:1; 1% triethylamine) The target intermediate compound 1-methyl-1,2,3,4-tetrahydro-β-carboline was obtained.

[0021] 2. Weigh the corresponding acid (1.8mmol) and dissolve it ...

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 discloses a fascaplysin derivative as well as a preparation method and application thereof to a drug. A general formula of the fascaplysin derivative disclosed by the invention is shownas a formula (I) and the formula (I) is shown in the description. The compound disclosed by the invention can be applied to preparation of drugs for preventing or treating diseases related to a cyclin-dependent kinase CDK4 inhibitor and anti-tumor drugs. The fascaplysin derivative keeps a pharmacodynamics effect of the CDK4 inhibitor; the compound has a high yield, is relatively stable in the air,has relatively good water solubility and is simple to operate; and the compound has the advantages of easiness for obtaining raw materials, low price, short preparation route, simple preparation method and low production cost.

Description

technical field [0001] The present invention relates to a compound and its preparation and application of the compound. Specifically, the present invention relates to a derivative of Fascaplysin, its preparation and its application in medicine. Background technique [0002] Fascaplysin is a red pigment that was first isolated from the Fiji marine sponge Fascaplysinopsis sp by Rolletal. b] Diindole members. Fascaplysin exhibits a wide range of biological activities, including antibacterial, antifungal, antiviral, HIV-1-RT, p56 tyrosine kinase, antimalarial, also effective against many cancer cell lines, and CDK4 inhibition. Fascaplysin inhibits the growth of several microorganisms, including Staphylococcus aureus, Escherichia coli, Candida albicans, and Saccharomyces cerevisiae. Fascaplysin shows inhibition of the proliferation of mouse leukemia cell line L-1210 with an ED50 value of 0.2 μM / mL and is selective in a murine tumor cytotoxicity assay. Fascaplysin exhibits anti...

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
IPC IPC(8): C07D471/04A61P35/00
CPCC07D471/04
Inventor 贺殿王震赵全义贾忠
Owner 南通杏睿生物科技有限公司
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