http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111925371-B
Outgoing Links
Predicate | Object |
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classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D473-18 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D473-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
filingDate | 2020-03-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2022-07-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2022-07-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-111925371-B |
titleOfInvention | Nitrobenzene-substituted O6-3-aminomethylbenzylguanine and its preparation method and application |
abstract | The invention discloses a nitrobenzene-substituted O 6-3 -aminomethylbenzylguanine and a preparation method and application thereof. The compound of the present invention, its structural formula is shown in formula I: In formula I, R 1 and R 2 are both CH 3 or H. The preparation method includes the following steps: reacting the imino group and the amino group in the compound represented by the formula II with an amino protecting reagent respectively to obtain the compound represented by the formula III, and performing a hydrolysis reaction under alkali catalysis to obtain the compound represented by the formula IV It contains an alkylamino group, and then activates the alkylamino group to generate a compound represented by formula VI containing an amide bond, which is obtained by the reaction of removing the amino protecting group. The preparation method of the invention is simple, can be used as an inhibitor of hypoxia targeting tumor cell DNA repair enzyme MGMT, has a hypoxia activating group, and as a prodrug, it can specifically activate and release active MGMT in the hypoxia solid tumor area inhibitors, thus specifically overcoming MGMT-mediated drug resistance in tumor cells while reducing toxic side effects on normal tissues. |
priorityDate | 2020-03-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 73.