Síntesis de fenil triazoles y estudio de su actividad inmunomoduladora

Treball final de Màster Universitari en Química Aplicada i Farmacològica. Codi: SIM138. Curs acadèmic: 2018/2019El objetivo principal de este trabajo se basa en sintetizar y estudiar la actividad biológica de una serie de derivados de tipo fenil triazol frente a las dos dianas descritas con anterioridad. Así, los objetivos se pueden enumerar como: I. Síntesis de una batería de feniltriazoles mediante el empleo de click chemistry. II. Evaluación biológica de los compuestos sintetizados con objeto de determinar su actividad antiproliferativa y su capacidad para inhibir PDL1 y c-My

Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents

Twenty-six triazole-based derivatives were designed for targeting both PD-L1 (programmed death receptor ligand 1) and VEGFR-2 (vascular endothelial growth factor receptor 2). These compounds were synthetized and biologically evaluated as multitarget inhibitors of VEGFR-2, PD-L1 and c-Myc proteins. The antiproliferative activity of these molecules on several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was determined. The effects on the abovementioned biological targets were evaluated for some selected compounds. Compound 23, bearing a p-chlorophenyl group, showed better results than sorafenib in regard to the downregulation of VEGFR-2 and a similar effect to BMS-8 on both PD-L1 and c-Myc proteins. The antiangiogenic and antivascular activities of chloro derivatives were also established by endothelial microtube formation assay on Matrigel®