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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

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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP60204
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP62184
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID557061
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP60205
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419478483
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419551199
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP60206
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP62201
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ05055
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCO35379
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID536203
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ6R520
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP62202
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP62203
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID442428
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419492855
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID154496482
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID4324384
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458392875
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID5281884
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID445635
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCA8I1Q0
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID6450806
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID547786
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP05933
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID410471421
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP05934
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID928
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP27161
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP05935
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP27165
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP27166
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419482810
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419523360
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID145858
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID152743212
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ6LCY3
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ9HFY6
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID5243
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ9GRJ1
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419519714
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID102577873
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCO94739
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID9429
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID24565
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID414278310
http://rdf.ncbi.nlm.nih.gov/pubchem/taxonomy/TAXID37656
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP02593
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ9UWF0
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID415851732
http://rdf.ncbi.nlm.nih.gov/pubchem/taxonomy/TAXID93250
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP02594
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP02595
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP02598
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ7Y052
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419520349
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCO96102
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP02599
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCO60041
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID421057440
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419535139
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID22272175
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCA4UHC0
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID281585
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419535157
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID281588
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID10286
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID104815
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ40302
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419529019
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ8CG09
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID10358258
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7553
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID543984
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID24646
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID426067522

Total number of triples: 380.