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Title: New methods for the synthesis of biologically active phenanthridine-based libraries
Author: Donaldson, Lauren Rona
ISNI:       0000 0004 2731 2792
Awarding Body: University of Edinburgh
Current Institution: University of Edinburgh
Date of Award: 2009
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Small molecule libraries have become essential for the development of drug discovery campaigns and chemical genetics. The studies towards the synthesis of a small molecule library, based upon the cis-ring fused phenanthridine core I, will be described. The first section of this thesis examines the development and application of a novel intramolecular Heck cyclisation to the synthesis of core phenanthridine structure II, via precursor III (Chapter 2).The second section (Chapter 3) describes the extension of this methodology towards the development of a library of phenanthridines IV. This includes methodology designed to incorporate the key principles of diversity-oriented synthesis, namely appendage, stereochemical and skeletal diversity. The final part of this thesis (Chapter 4) describes the merging of these various methodologies to generate a small library of novel phenanthridine analogues. Preliminary biological evaluation of the phenanthridine library using whole organism zebrafish phenotyping, will also be discussed.
Supervisor: Hulme, Alison N. ; Lam, Hon Wai Sponsor: Not available
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available
Keywords: small molecule library ; phenanthridine ; intramolecular Heck cyclisation