http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110256398-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D317-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D317-62 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D317-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-62 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-54 |
| filingDate | 2019-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2022-01-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2022-01-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-110256398-B |
| titleOfInvention | A kind of synthetic method of methylene ether urushiol hydroxamic acid derivative with HDAC inhibitory activity |
| abstract | The invention relates to a method for synthesizing a methylene ether urushiol hydroxamic acid derivative with HDAC inhibitory activity. Using unsaturated urushiol as raw material, the oxidative polymerization of urushiol is blocked by etherification reaction, and the hydroxamic acid group is introduced into the tail of urushiol side chain through reactions such as Diels-Alder, hydrolysis and hydroxylation. Three kinds of methylene ether urushiol hydroxamic acid derivatives were synthesized by introducing different pharmacological groups such as nitro and hydroxyl groups into the ring or alkyl chain. It forms stable hydrogen bond interactions with its residues, and can form stable chelation with Zn 2+ at the bottom of the active pocket. It has very good HDAC inhibitory activity. The half inhibitory concentration of the three compounds on HDAC 2 and HDAC 8 (IC 50 ) value is comparable to the IC 50 value of the FDA-approved HDAC inhibitor SAHA, which can be used in clinical anti-tumor drugs with extremely high added value, and can become a new technology for clinical development of new urushiol-based HDAC inhibitors. |
| priorityDate | 2019-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 114.