Synthesis and biological evaluation of small molecules as potential anticancer multitarget agents

Pla López, A. ; Castillo, R. ; Cejudo Marín, R. ; García Pedrero, O. ; Bakir Laso, M. (Universidad de Zaragoza) ; Falomir, E. ; Carda, M.

Resumen: 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.

Idioma: Inglés

DOI: 10.3390/ijms23137049

Año: 2022

Publicado en: International Journal of Molecular Sciences 23, 13 (2022), 7049 [19 pp.]
ISSN: 1661-6596

Factor impacto JCR: 5.6 (2022)

Categ. JCR: BIOCHEMISTRY & MOLECULAR BIOLOGY rank: 66 / 285 = 0.232 (2022) - Q1 - T1
Categ. JCR: CHEMISTRY, MULTIDISCIPLINARY rank: 52 / 178 = 0.292 (2022) - Q2 - T1

Factor impacto CITESCORE: 7.8 - Biochemistry, Genetics and Molecular Biology (Q1) - Computer Science (Q1) - Chemistry (Q1) - Chemical Engineering (Q1) - Medicine (Q1)

Factor impacto SCIMAGO: 1.154 - Medicine (miscellaneous) (Q1) - Physical and Theoretical Chemistry (Q1) - Computer Science Applications (Q1) - Inorganic Chemistry (Q1) - Spectroscopy (Q1) - Organic Chemistry (Q1) - Molecular Biology (Q2) - Catalysis (Q2)

Tipo y forma: Article (Published version)

Área (Departamento): Área Química Analítica (Dpto. Química Analítica)