Theses - Chemistry
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Rationally designed aplyronine analogues for use in antibody-drug conjugates
(2019-07-31)The aplyronines are a family of antimitotic marine macrolides which show highly potent antiproliferative effects at picomolar concentrations in human cancer cell lines. Through a novel dual protein-targeting mechanism of ... -
Synthesis of Structurally Diverse N-Substituted Quaternary Carbon Containing Small Molecules and Their Application as Novel Starting Points for Drug Discovery
(2019-07-09)New bioactive small molecules are urgently required to seed both medicinal chemistry and chemical biology research. Within the two last decades, however, organic synthesis has been identified as a limiting factor in this ... -
Computer-Aided Design of Ligands at Multiple Protein Targets for Multifactorial Diseases
(2019-04-27)Today, drug discovery predominately focuses on the design of ligands with high selectivity towards a specific biological target. A significant limitation in the case of multi-factorial diseases (e.g. neurodegenerative ... -
The synthesis and biological evaluation of a library of autoinducer-antibiotic conjugates
Microbial resistance to antibiotics is a serious global health threat, and the discovery of new, safe and effective antibiotics is required urgently. A new class of antibiotics, namely sideophore-antibiotic conjugates, has ...
