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http://hdl.handle.net/10397/85421
DC Field | Value | Language |
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dc.contributor | Department of Applied Biology and Chemical Technology | - |
dc.creator | Zhu, Xuezhen | - |
dc.identifier.uri | https://theses.lib.polyu.edu.hk/handle/200/10226 | - |
dc.language.iso | English | - |
dc.title | Chemical modulation of multidrug resistant proteins by triazole bridged flavonoid dimers | - |
dc.type | Thesis | - |
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. | - |
dcterms.accessRights | open access | - |
dcterms.educationLevel | Ph.D. | - |
dcterms.extent | 388 pages : color illustrations | - |
dcterms.issued | 2019 | - |
dcterms.LCSH | Hong Kong Polytechnic University -- Dissertations | - |
dcterms.LCSH | ATP-binding cassette transporters | - |
dcterms.LCSH | Drug resistance | - |
Appears in Collections: | Thesis |
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