Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating Agents
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Altres documents de l'autoria: Gil-Edo, Raquel; Royo, Santiago; Carda, Miguel; Falomir, Eva
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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INVESTIGACIONMetadades
Títol
Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating AgentsData de publicació
2023Editor
MDPICita bibliogràfica
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/ph16060808Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
https://www.mdpi.com/1424-8247/16/6/808Versió
info:eu-repo/semantics/publishedVersionParaules clau / Matèries
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
Resum
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. [-]
Publicat a
Pharmaceuticals, 2023Entitat finançadora
Ministerio de Economía y Competitividad | Universitat Jaume I
Codi del projecte o subvenció
RTI2018-097345-B-I00 | PID2021-1267770B-100 | UJI-B2021-46
Drets d'accés
info:eu-repo/semantics/openAccess
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