http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-112209875-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-42 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2020-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2021-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-112209875-B |
| titleOfInvention | A kind of 6-amino-4-(4-phenoxyphenethylamino)quinazoline derivative and its preparation method and application |
| abstract | The invention belongs to the technical field of medicine, and in particular relates to a 6-amino-4-(4-phenoxyphenethylamino)quinazoline (QNZ) derivative and a preparation method and application thereof. In the present invention, a structural unit of inverted cyanoacrylamide is introduced into the 6-position of the quinazoline parent ring, and a series of reversible covalent addition reactions with intracellular sulfhydryl protein are constructed to break the redox balance in cancer cells, thereby killing QNZ-like active compounds of dead cancer cells. This reversible reaction is expected to improve the contact time of the active compound with the target in vivo, thereby enhancing the efficacy and selectivity. In the present invention, the IC50 value in human colon cancer cell SW620 is only 74 nM (48 hours of action), while the IC50 value in normal cell line is close to 30 μM, which has better proliferation inhibitory activity and selectivity. The present invention finds that QNZ-C blocks the cell cycle in the G2/M phase by promoting the generation of intracellular ROS through subsequent mechanism research, thereby inducing apoptosis. |
| priorityDate | 2020-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 89.