Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/82038
DC Field | Value | Language |
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dc.contributor | Department of Applied Biology and Chemical Technology | - |
dc.creator | Chow, LMC | en_US |
dc.creator | Chan, TH | en_US |
dc.creator | Chan, KF | en_US |
dc.creator | Wong, ILK | en_US |
dc.creator | Law, MC | en_US |
dc.date.accessioned | 2020-05-05T05:58:24Z | - |
dc.date.available | 2020-05-05T05:58:24Z | - |
dc.identifier.uri | http://hdl.handle.net/10397/82038 | - |
dc.language.iso | en | en_US |
dc.rights | Assignee: The Hong Kong Polytechnic University | en_US |
dc.rights | Assignee: The Royal Institution for the Advancement of Learning/McGill University | en_US |
dc.title | Alkyne-, azide- and triazole-containing flavonoids as modulators for multidrug resistance in cancers | en_US |
dc.type | Patent | en_US |
dc.description.otherinformation | US10208025; US10208025 B2; US10208025B2; US10,208,025; US10,208,025 B2; 10208025; Appl. No. 15/296,471 | en_US |
dcterms.abstract | A triazole bridged flavonoid dimer compound library was efficiently constructed via the cycloaddition reaction of a series of flavonoid-containing azides (Az 1-15) and alkynes (Ac 1-17). These triazole bridged flavonoid dimers and their precursor alkyne- and azide-containing flavonoids were screened for their ability to modulate multidrug resistance (MDR) in P-gp-overexpressed cell line (LCC6MDR), MRP1-overexpressed cell line (2008/MRP1) and BCRP-overexpressed cell line (HEK293/R2 and MCF7-MX100). Generally, they displayed very promising MDR reversal activity against P-gp-, MRP1- and BCRP-mediated drug resistance. Moreover, they showed different levels of selectivity for various transporters. Overall, they can be divided into mono-selective, dual-selective and multi-selective modulators for the P-gp, MRP1 and BCRP transporters. The EC.sub.50 values for reversing paclitaxel resistance (141-340 nM) of LCC6MDR cells, DOX (78-590 nM) and vincristine (82-550 nM) resistance of 2008/MRP1 cells and topotecan resistance (0.9-135 nM) of HEK293/R2 and MCF7-MX100 cells were at nanomolar range. Importantly, a number of compounds displayed EC.sub.50 at or below 10 nM in BCRP-overexpressed cell lines, indicating that these bivalent triazoles more selectively inhibit BCRP transporter than the P-gp and MRP1 transporters. Most of the dimers are notably safe MDR chemosensitizers as indicated by their high therapeutic index values. | - |
dcterms.bibliographicCitation | US Patent 10,208,025 B2. Washington, DC: US Patent and Trademark Office, 2019. | en_US |
dcterms.issued | 2019-02-19 | - |
dc.description.country | US | - |
dc.description.validate | 202006 bcrc | - |
dc.description.oa | Version of Record | en_US |
Appears in Collections: | Patent |
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File | Description | Size | Format | |
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us10208025b2.pdf | 5.73 MB | Adobe PDF | View/Open |
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