http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110256398-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6d7f722cc064b823c523a268b7179a8f |
| 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/C07D317-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-62 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2019-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dcb327cd4c4c979d868a96e0ecb676ec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e9f6fa4e01205a7f040475ed215b8d64 |
| publicationDate | 2019-09-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-110256398-A |
| 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 methylene ether urushiol hydroxamic acid derivatives with HDAC inhibitory activity. Using unsaturated urushiol as raw material, block the oxidative polymerization of urushiol through etherification reaction, introduce hydroxamic acid group at the tail of urushiol side chain through Diels-Alder, hydrolysis and hydroxylation reactions, and introduce hydroxamic acid groups in its benzene Different pharmacophore groups such as nitro group and hydroxyl group were introduced into the ring or alkyl chain, and three kinds of methylene ether urushiol hydroxamic acid derivatives were synthesized. All three compounds can be well combined with the active pocket of HDAC, and can It forms stable hydrogen bond interaction with its residues, and can form a stable chelation with Zn 2+ at the bottom of the active pocket, and has good HDAC inhibitory activity. The half maximal inhibitory concentration (IC 50 ) value is equivalent to the IC 50 value of FDA-approved HDAC inhibitor SAHA, can be applied to clinical antitumor drugs, has extremely high added value, and can become a new technology for clinical development of new urushiol-based HDAC inhibitors. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111440138-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-116675677-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-116675677-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-116375698-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-116375698-B |
| 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: 140.