Full metadata record
| DC Field | Value | Language |
|---|---|---|
| dc.contributor | Department of Applied Biology and Chemical Technology | en_US |
| dc.contributor.advisor | Chow, Larry (ABCT) | - |
| dc.creator | Zhu, Xuezhen | - |
| dc.identifier.uri | https://theses.lib.polyu.edu.hk/handle/200/10226 | - |
| dc.language | English | en_US |
| dc.publisher | Hong Kong Polytechnic University | - |
| dc.rights | All rights reserved | en_US |
| dc.title | Chemical modulation of multidrug resistant proteins by triazole bridged flavonoid dimers | en_US |
| dcterms.abstract | The central theme of this thesis is the exploration of new modulators of ABC transport proteins by the design and synthesis of a series of triazole-bridged flavonoid dimers. Chapter 1 briefly introduces the background of multidrug resistance, ABC transport proteins, click chemistry as well as the objective of this thesis. Chapter 2 describes a rapid generation of a flavonoid dimer library using "click chemistry". Following this, a high-throughput screening led to the discovery of some highly potent and safe MRP1 modulators is presented. Chapter 3 elucidates the design and synthesis of a series of triazole bridged flavonoid heterodimers and homodimers. Besides, the compounds are evaluated for their potency in reversing BCRP-mediated multidrug resistance. Structure activity relationship of flavonoid dimers towards modulating BCRP is discussed. Finally, a homodimer, Ac22Az8, as a non-cytotoxic, potent and selective BCRP modulator is presented. Chapter 4 describes the design and synthesis a series of triazole bridged flavonoid heterodimers. Following this, the compounds evaluated for their potency in reversing multidrug resistance in P-gp, BCRP and MRP1. Chapter 5 describes the summary future work of this thesis. | en_US |
| dcterms.extent | 388 pages : color illustrations | en_US |
| dcterms.isPartOf | PolyU Electronic Theses | en_US |
| dcterms.issued | 2019 | en_US |
| dcterms.educationalLevel | Ph.D. | en_US |
| dcterms.educationalLevel | All Doctorate | en_US |
| dcterms.LCSH | Hong Kong Polytechnic University -- Dissertations | en_US |
| dcterms.LCSH | ATP-binding cassette transporters | en_US |
| dcterms.LCSH | Drug resistance | en_US |
| dcterms.accessRights | open access | en_US |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| 991022289512503411.pdf | For All Users | 12.29 MB | Adobe PDF | View/Open |
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