PhD defence E.M.M. Abdelraheem
|When:||Mo 18-06-2018 14:30 - 16:00|
Exploitation of macrocyclic chemical space by multicomponent reaction (MCR) and their applications in medicinal chemistry
The research described in the thesis of Eman Mahmoud Mohamed Abdelraheem is focused on the development of new synthetic technology to access artificial macrocycles with potential biological activity. Artificial macrocycles are an emerging and largely underexploited part of chemical space where potentially drugs for difficult genomic targets can be discovered. Current pharmaceutical libraries are largely unsuitable to target the large and interesting class of genomic targets and artificial macrocycles promise to fill the gap between small molecules and the large molecular weight biologics. While artificial macrocycles can have advantages over their natural twins such as better control over synthesis, ADMET properties and target binding, fast and convergent synthesis pathways are underdeveloped. Multi-component reaction (MCR) is a promising synthetic methodology for the rapid and easy access to scaffold with a great diversity and for synthesis of a diverse range of macrocycles. MCRs are able to generate great levels of molecular diversity and complexity at low synthetic costs for these complex macrocycles. Also, the design and evaluation of new p53-MDM2/X inhibitors are presented.
Promotores Prof.dr. A.S.S. Dömling
Co-supervisor: dr. M.R. (Matthew) Groves