http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AU-2021104778-A4

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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

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