Synthesis and Testing of Vinyl Heteroaromatics with Application in an ADC Bioconjugation Platform

Andrew, Jack (2022) Synthesis and Testing of Vinyl Heteroaromatics with Application in an ADC Bioconjugation Platform. Doctoral thesis, University of East Anglia.

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Abstract

With an ever-increasing number of cancer diagnoses, the search for more effective cancer treatment continues. One such promising treatment is the combination of antibodies and chemotherapeutic agents, known as antibody-drug conjugates, which aim to combine highly cytotoxic payloads with antibody specificity creating a “magic bullet” in the fight against cancer.

Key to the function of antibody drug conjugates are the conjugation chemistries which connect cytotoxic payload to the antibody through a stable linkage. One such class of bioconjugation chemistries are vinylpyridine analogues, which selectively react with thiol residues to form stable thioether adducts.

The aim of the project was two-fold; increasing the reactivity and thus rate of conjugation, and modifying the pKa of the pyridine ring. Alternate heteroaromatic cores were also explored as possibilities. These aims were addressed through the application of known and novel synthetic chemistry to a variety of compounds, described within this thesis.

Item Type:	Thesis (Doctoral)
Faculty \ School:	Faculty of Science > School of Chemistry
Depositing User:	Chris White
Date Deposited:	31 May 2023 14:04
Last Modified:	31 May 2023 14:04
URI:	https://ueaeprints.uea.ac.uk/id/eprint/92214
DOI:

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