Alkyne metathesis: A new tool for the self-assembly of complex molecular architectures

Lead Research Organisation: University of Edinburgh
Department Name: Sch of Chemistry

Abstract

Project Aims:

To exploit this highly convergent modular synthetic strategy through the synthesis of heteroaryl analogues of
the disorazoles, termed "hetero-disorazoles", positioning alkyne metathesis as an important tool in this field
(catalyst design optimised in collaboration with Prof. A. Furstner, Max Plank Institute, Mulheim, Germany).

Be inspired in our choice of hetero-disorazole targets by rigorous in silico studies to show which analogues
have the highest predicted dimer/monomer and head-to-tail/head-to-head alkyne metathesis coupling ratios
(molecular modelling conducted in collaboration with Prof. J. Goodman, University of Cambridge).

Access a new class of disorazoles which are not covered by the patent literature and which might be more
stable, more synthetically tractable and have enhanced therapeutic potential (phenotypic and RPPA assays
conducted in collaboration with Prof. N. Carragher at the Edinburgh Cancer Research Centre).
Combining in silico design with experimental validation, this project will demonstrate that Mo-catalysed alkyne
metathesis can be used as an effective tool for the rapid self-assembly of complex macrocyclic architectures of
pharmaceutical interest.

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/N509644/1 01/10/2016 30/09/2021
1940702 Studentship EP/N509644/1 01/09/2017 31/10/2021 Ektoras Yiannakas
 
Description AG Leventis Scholarship
Amount £2,750 (GBP)
Organisation AG Leventis Foundation 
Sector Charity/Non Profit
Country Cyprus
Start 09/2018 
End 09/2019
 
Description Leverhulme Trust Study Abroad Studentship
Amount £21,000 (GBP)
Funding ID SAS-2019-012 
Organisation The Leverhulme Trust 
Sector Charity/Non Profit
Country United Kingdom
Start 09/2019 
End 09/2020