Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics

Dobiecki-Davies, J

Abstract

DAOY Medullablastoma cells are highly invasive, mobile and can cause severe neurological and physical illness in patients affected by this cancer. Previous work by Wilkinson & Co-workers (2017) showed that some small-molecule non-sugar glycomimetic drugs were able to prevent wound healing in DAOY cells. Therefore establishing a SAR for these molecules was of interest.
A number of mono, di, tri, tetra & poly-sulfated drug molecules were synthesised from easily available starting materials and reagents and tested for potency against wound healing in DAOY cells in a scratch assay against human growth factor/scatter factor (HGF/SF) as a control. Compounds trialled in scratch assays did not show any reasonable biological activity. HGF/SF has been shown to activate downstream signalling of the oncogene product c-Met which is a biomarker for cancer(s) and can be associated with poorer outcomes for patients.

Citation

Dobiecki-Davies, J. Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics. (Dissertation). University of Salford

• Thesis Type: Dissertation
• Deposit Date: Oct 5, 2021
• Publicly Available Date: Oct 5, 2021
• Award Date: Mar 31, 2021