http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AU-2021104778-A4
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d7594a27aec86a239c0448ab4210c266 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J53-002 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-02 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J53-00 |
filingDate | 2021-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2022-04-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e6c6a07a9db115d9a0eec73aca7a7fb3 |
publicationDate | 2022-04-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AU-2021104778-A4 |
titleOfInvention | Chemical transformation of betulin, a pentacyclic triterpene and studies on the inhibitory activity of the betulin analogues against leishmania donovani dna topoisomerases. |
abstract | It was observed by our group that betulinic acid is a potent inhibitor of mammalian type I DNA ntopoisomerase. The identification of topoisomerase I as the cellular target for betulinic acid is ndue to hydrogen bonding capability or acidity at position C 1 7 , moreover replacement of the nCOOH group at C 17 with a CH2OH group as in betulin diminishes the inhibitory effect. These nobservations provide a rational approach to synthesise of selective half ester analogues of nbetulin and dihydrobetulin. A series of analogous modified at C3 , C 17 position of betulin and ndihydrobetulin were prepared and subsequently assayed for inhibition of topoisomerase I ncatalytic activity. Among them, 3-0-28-0-disuccinyl betulin,3-0-28-0-diglutaryl dihydrobetulin n3-0-28-0-disuccinyl dihydrobetulin showed inhibitory activity against DNA topoisomerase IB nfrom Leishmania donovani. |
priorityDate | 2021-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 32.