(E)-Styryl derivatives for the discovery of anticancer and antiviral agents

Abstract

The present doctoral thesis is situated within the field of medicinal chemistry and the main objective is to design and evaluate organic small molecules with potential anticancer activity and to assess their potential as antiviral agents. For this purpose, a total of 44 compounds have been synthesised, purified and characterised. Of these, 37 are final and share a common (E)-styryl motif. The anti-tumour biological evaluation includes the study of their cytotoxic effect, an analysis of their immunomodulatory action, and an examination of their anti-inflammatory ability. The findings indicate that 1,4-[p-(methoxystytyryl)]fluoro- and chlorophenylcarbamates drastically reduce the immunosuppressive environment in the TME. This is partly due to the effect on PD-1/PD-L1 membrane protein binding and favourable regulation of pro-inflammatory cytokine levels, which favours immune system activation and reduces inflammation in TME. Finally, the biological evaluation as antiviral agents has led to the conclusion that they do not show outstanding activity against viruses.