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Title: Functionalised peptidomimetic metallohelices
Author: Song, Hualong
Awarding Body: University of Warwick
Current Institution: University of Warwick
Date of Award: 2018
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Chapter 1 introduces small host-defence peptides in cancer therapy. The main mechanisms proposed in their interactions with membranes and intracellular targets are discussed. The biologically relevant peptide mimetics are also reviewed. Chapter 2 describes the synthesis and characterisation of alkyne derivatives of metallohelices. These alkyne metallohelices demonstrated promising anticancer activity in vitro. Investigations of click reactions on alkyne flexicates were partially successful. Chapter 3 describes the click reaction of alkyne triplexes. A range of aromatic clicked triplexes were synthesized and characterised. These novel complexes showed potential anticancer activity and high selectivity, and antimetastatic properties. Preliminary mechanism study revealed these metallohelices inhibit Na+/K+ ATPase activity. Chapter 4 describes two different methodologies to synthesize and characterise glycoconjugate metallohelices. A variety of glyco-metallohelices were then investigated for activity and selectivity in cancer cell lines and normal cell lines. The glyco-metallohelices displayed similar inhibition to the growth of human tumour xenografts, but lower side effect than cisplatin. Chapter 5 focuses on the synthesis and characterisation of triplex metallohelices containing triazole ligands and their potential biological application. Chapter 6 details the experimental procedures used to carry out the work in this thesis.
Supervisor: Not available Sponsor: China Scholarship Council
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available
Keywords: QD Chemistry