Application of Rhodanine derivates as antineoplastic medicine
A technology of anti-tumor drugs and derivatives, applied in the field of anti-tumor drugs, can solve the problem of no further research and other problems
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0030] Embodiment one: see figure 1 As shown, the derivatives with rhodanine as the parent ring are prepared:
[0031] Aldehyde (1.0mmol), rhodanine (1.0mmol), sodium acetate (2.0-4.0mmol) and 50mL acetic acid were added to the reaction flask, and stirred at reflux for 5-10h. After the reaction solution was cooled to room temperature, it was poured into 100 mL of water and stirred for 1.0 h. Suction filtration, washing with water, and drying to obtain crude product A.
[0032] Add A (1.0mmol), diisopropylethylamine (2.0-5.0mmol) and 50mL absolute ethanol into the reaction flask, and add iodomethane (2.0-5.0mmol) dropwise under stirring. After reacting at room temperature for 2 h, the reaction solution was poured into 100 mL of water and stirred vigorously for 1 h. Suction filtration, washing with water, and drying to obtain crude product B.
[0033] Add B (1.0mmol), diisopropylethylamine (1.0-3.0mmol), L-phenylalanine (1.0-3.0mmol) and 25mL ethanol into the reaction flas...
Embodiment 2
[0064] Analysis of rhodanine derivatives (compound SZ0104) as an anti-tumor compound to inhibit tumor effect:
[0065] 1. First, determine the binding constant K of the compound and the target protein by fluorescence polarization method i , Fluorescence polarization can characterize the tightness of small molecules and binding proteins, and is widely used in drug screening in vitro. The recombinant Bcl-2 protein (1.0 μM) is mixed with the substrate Flu-Bak polypeptide at room temperature to form a protein-polypeptide The complex, and then add various concentrations of small molecule drugs (rhodanine derivatives), the small molecule compound will displace the substrate polypeptide after binding to the protein, and cause the change of the fluorescence polarization signal of the solution. This variable is determined by the TecanGENiosPro multifunctional enzyme Standard instrument 96-well plate detection.
[0066] Such as image 3 As shown, the K of compound SZ0104 on Bcl-2 i I...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More 
PatSnap Eureka turns technology decisions into work you can execute. Powered by our Innovation Knowledge Graph, it runs expert workflows across engineering, life sciences, materials and intellectual property. Get your review-ready output in minutes.
