Aryl azoles based scaffolds for disrupting tumor microenvironment
Impacto
Scholar |
Otros documentos de la autoría: Pla López, Alberto; Martinez-Colomina, Paula; Cañada-García, Laura; Fuertes-Monge, Laura; Orellana-Palacios, Jose C.; Valderrama-Martínez, Alejandro; Pérez Sosa, Marikena; Carda, Miguel; Falomir, Eva
Metadatos
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comunitat-uji-handle3:10234/8639
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INVESTIGACIONMetadatos
Título
Aryl azoles based scaffolds for disrupting tumor microenvironmentAutoría
Fecha de publicación
2023-11-15Editor
ElsevierISSN
0968-0896Cita bibliográfica
A. Pla-López, P. Martínez-Colomina, L. Cañada-García, L. Fuertes-Monge, J. C. Orellana-Palacios, A. Valderrama-Martínez, M. Pérez-Sosa, M. Carda, E. Falomir E. Aryl azoles based scaffolds for disrupting tumor microenvironment. Bioorg Med Chem. 2023; 95:117490. https://doi.org/10.1016/j.bmc.2023.117490Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
https://www.sciencedirect.com/science/article/pii/S0968089623003383?casa_token=j ...Versión
info:eu-repo/semantics/publishedVersionPalabras clave / Materias
triazole | tetrazole | PD-L1 | VEGFR-2 | c-Myc | CD-47 | IL-6 | tumor microenvironment | antiproliferative activity | angiogenesis
Resumen
Thirty-nine aryl azoles, thirteen triazoles and twenty-seven tetrazoles, have been synthetized and biologically evaluated to determine their activity as tumor microenvironment disruptors. Antiproliferative studies ... [+]
Thirty-nine aryl azoles, thirteen triazoles and twenty-seven tetrazoles, have been synthetized and biologically evaluated to determine their activity as tumor microenvironment disruptors. Antiproliferative studies have been performed on tumor cell lines HT-29, A-549 and MCF-7 and on non-tumor cell line HEK-293. It has been studied in HT-29 the expression levels of biological targets which are involved in tumor microenvironment processes, such as PD-L1, CD-47, c-Myc and VEGFR-2. In addition, antiproliferative activity was evaluated when HT-29 were co-cultured with THP-1 monocytes and the secretion levels of IL-6 were also determined in these co-cultures. The angiogenesis effect of some selected compounds on HMEC-1 was also evaluated as well as their action against vasculogenic mimicry on HEK-293. Compounds bearing an amino group in the phenyl ring and a halogen atom in the benzyl ring showed promising results as tumor microenvironment disrupting agents. The most outstanding compound decrease dramatically the population of HT-29 cells when co-cultured with THP-1 monocytes and the levels of IL-6 secreted, as well as it showed moderate effects over PD-L1, CD-47 and c-Myc. [-]
Publicado en
Bioorganic & Medicinal Chemistry, 2023, vol. 95Entidad financiadora
Ministerio de Ciencia e Innovación | Universitat Jaume I | Generalitat Valenciana
Identificador de la entidad financiadora
https://doi.org/10.13039/501100011033
Código del proyecto o subvención
MCIN/PEICTI2021-2023/PID2021-126277OB-100 | UJI-B2021-46 | ACIF/2020/341
Derechos de acceso
info:eu-repo/semantics/openAccess
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