http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-104169267-B
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D311-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-352 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-35 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D249-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-32 |
filingDate | 2013-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2017-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2017-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-104169267-B |
titleOfInvention | Flavonoid containing alkynes, the flavonoid containing azide and the flavonoid containing triazole are used for the multidrug resistance of cancer as regulator |
abstract | Triazole bridging flavonoid dimer compound library effectively builds via a series of cycloaddition reactions containing azide (Az 1 15) and the flavonoid of alkynes (Ac 1 17).Contain the flavonoid of alkynes and the flavonoid containing the azide ability of regulation multidrug resistance (MDR) in the cell strain (HEK293/R2 and MCF7 MX100) of the cell strain (LCC6MDR) of overexpression P gp, the cell strain (2008/MRP1) of overexpression MRP1 and overexpression BCRP for these triazole bridging flavonoid dimers and its presoma it is screened.It generally shows the MDR Reversal activity of Drug-resistant extremely promising and that BCRP mediates.Additionally, it shows the selectivity of varying level to various transport proteins.Generally speaking, it can be divided into mono-selectivity, double selectivity and multi-selection regulator for P gp, MRP1 and BCRP transport protein.The EC50 value of the topotecan-resistance (0.9 135nM) of Paclitaxel drug resistance (141 340nM), the DOX (78 590nM) of 2008/MRP1 cell and vincristine (82 550nM) drug resistance and HEK293/R2 and MCF7 MX100 cell reversing LCC6MDR cell is in nanomolar range.Importantly, chemical compound lot shows the EC50 at or below 10nM in the cell strain of overexpression BCRP, show compared with P gp and MRP1 transport protein, these bivalence triazoles more optionally suppress BCRP transport protein.Most of dimer is noticeable safe MDR chemical sensitizer, as indicated by its high therapeutic index value. |
priorityDate | 2012-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 380.