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dc.contributor.advisorDavis, Rohan
dc.contributor.authorKumar, Rohitesh
dc.date.accessioned2018-01-23T02:32:08Z
dc.date.available2018-01-23T02:32:08Z
dc.date.issued2017
dc.identifier.doi10.25904/1912/2604
dc.identifier.urihttp://hdl.handle.net/10072/366694
dc.description.abstractNatural products (NPs) continue to have significant impact in the area of drug discovery and development. More than 50% of the approved drugs between 1981 and 2014 were either unaltered NPs, NP derivatives or synthetic drugs inspired by NP pharmacophores. NPs have also served as lead molecules in drug development programs; noteworthy example include the semi-synthetic antifungal drugs caspofungin, anidulafungin, and micafungin that were based on NP lead compounds isolated from the fermentation products of various fungus. Other notable examples include the sponge metabolite halichondrin B that was developed into the anticancer drug eribulin, and camptothecin, a plant NP that was developed into the oncology drugs, topotecan and irinotecan. Many research groups are now utilizing isolated NPs as scaffolds for the generation of semi-synthetic analogue libraries rather than pursuing the total synthesis of a bioactive NP followed by classic medicinal chemistry. This approaches main advantage is the reduction in timelines and resource allocation, which is typically associated with de novo multi-step syntheses of a bioactive NP. Furthermore, once the NP scaffold has been isolated from the source biota rapid analogue generation and subsequent SAR data can be acquired. Thus the evaluation of a scaffold chemotype for potential lead optimization studies is quickly assessed.
dc.languageEnglish
dc.publisherGriffith University
dc.publisher.placeBrisbane
dc.rights.copyrightThe author owns the copyright in this thesis, unless stated otherwise.
dc.subject.keywordsDrug discovery
dc.subject.keywordsNatural products
dc.subject.keywordsCaspofungin
dc.subject.keywordsAnidulafungin
dc.subject.keywordsMicafungin
dc.subject.keywordsSponge metabolite halichondrin B
dc.subject.keywordsScaffold chemotype
dc.titleDesign and Synthesis of Natural Product-Based Screening Libraries
dc.typeGriffith thesis
dc.date.embargoEnd2018-02-27
gro.facultyScience, Environment, Engineering and Technology
gro.rights.copyrightThe author owns the copyright in this thesis, unless stated otherwise.
gro.hasfulltextFull Text
dc.contributor.otheradvisorCoster, Mark
gro.identifier.gurtIDgu1500341453658
gro.source.ADTshelfnoADT0
gro.source.GURTshelfnoGURT
gro.thesis.degreelevelThesis (PhD Doctorate)
gro.thesis.degreeprogramDoctor of Philosophy (PhD)
gro.departmentSchool of Natural Sciences
gro.griffith.authorKumar, Rohitesh


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