http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-106977584-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06034 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-062 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 |
| filingDate | 2017-04-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2019-12-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2019-12-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-106977584-B |
| titleOfInvention | Compound for targeted ubiquitination degradation of PLK1 and BRD4 proteins and application thereof |
| abstract | The invention relates to a compound for targeted ubiquitination degradation of PLK1 and BRD4 proteins and application thereof, belonging to the field of compound synthesis. The invention selects the structural analogue of the compound A as a binding part of PROTACs with E3 ligase, and selects a connecting chain to connect the structural analogue with the activity of a Polo-like kinase 1(PLK1) and bromodomain protein 4(BRD4) protease inhibitor to construct the PROTACs. Meanwhile, the constructed compound aims at double targets of PLK1 and BRD4, and the drug resistance of the anti-tumor activity of the compound can be reduced compared with a single-target drug. The in vitro PLK1 and BRD4 protease inhibition activity, in vitro anti-tumor activity test and in vitro PLK1 and BRD4 protein degradation activity show that the compounds (PROTACs) for targeted ubiquitination degradation of PLK1 and BRD4 proteins can degrade PLK1 and BRD4 targeted proteins, have good anti-tumor activity and show excellent PLK1 and BRD4 inhibition effects. The preparation method is simple to operate and mild in conditions, and the obtained compounds have the activities of inhibiting and degrading PLK1 and BRD4 proteases and have obvious anti-tumor effect. |
| priorityDate | 2017-04-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 106.