Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating Agents
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Otros documentos de la autoría: Gil-Edo, Raquel; Royo, Santiago; Carda, Miguel; Falomir, Eva
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INVESTIGACIONMetadatos
Título
Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating AgentsFecha de publicación
2023Editor
MDPICita bibliográfica
Gil-Edo, R.; Royo, S.; Carda, M.; Falomir, E. Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating Agents. Pharmaceuticals 2023, 16, 808. https://doi.org/10.3390/ph16060808Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
https://www.mdpi.com/1424-8247/16/6/808Versión
info:eu-repo/semantics/publishedVersionPalabras clave / Materias
tumor microenvironment | aryl urea | angiogenesis | VEGFR-2 | PD-L1 | immune checkpoints | CD-11b | CD-80 | THP-1 | HT-29 | co-cultures | 3. Salud y bienestar
Resumen
This work focuses on the development of thirteen benzylethylenearyl ureas and one
carbamate. After the synthesis and purification of the compounds, we studied their antiproliferative action on cell lines, such as ... [+]
This work focuses on the development of thirteen benzylethylenearyl ureas and one
carbamate. After the synthesis and purification of the compounds, we studied their antiproliferative action on cell lines, such as HEK-293, and cancer ones, such as HT-29, MCF-7 or A-549, on the
immune Jurkat T-cells and endothelial cells HMEC-1. Compounds C.1, C.3, C.12 and C.14 were
selected for further biological studies to establish their potential as immunomodulating agents.
Some of the derivatives exhibited significant inhibitory effects on both targets: PD-L1 and VEGFR-2
in the HT-29 cell line, showing that urea C.12 is active against both targets. Some compounds could
inhibit more than 50% of cancer cell proliferation compared to non-treated ones when assessed in
co-cultures using HT-29 and THP-1 cells. In addition, they significantly reduced CD11b expression,
which is a promising target for immune modulation in anticancer immunotherapies. [-]
Publicado en
Pharmaceuticals, 2023Entidad financiadora
Ministerio de Economía y Competitividad | Universitat Jaume I
Código del proyecto o subvención
RTI2018-097345-B-I00 | PID2021-1267770B-100 | UJI-B2021-46
Derechos de acceso
info:eu-repo/semantics/openAccess
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