Desing, synthesis and biological evaluation of choline kinase enzyme inhibitor diazufro derivatives – Marina Úbeda García

In this research, a total of 9 symmetrical diazuffered bis-cationic compounds with inhibitory activity against the human ChoKα1 enzyme were designed, synthesised and characterised. The aim was to find compounds with effective inhibitory and antiproliferative activity in tumour cells. In-vitro biological assays were performed to determine their capacity to inhibit human ChoKα1 and restrict its proliferation. We noted that slight changes in the structure of the molecules give rise to considerable variations in inhibitory activity and antiproliferative capacity and that compounds with a high capacity to inhibit the enzyme were unable to inhibit tumour cell development and vice versa. Further studies are therefore needed to investigate the mechanism of action, as well as to continue in-vitro synthesising and testing of new ChoKα1 inhibitor compounds, so as to find molecules that perform this function successfully.

Keywords: sulphur derivatives; inhibitory capacity; antiproliferative capacity; choline kinase.

Directed by: Luisa Carlota López Cara