Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating Agents
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Other documents of the author: 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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Title
Unveiling the Potential of BenzylethyleneAryl–Urea Scaffolds for the Design of New Onco Immunomodulating AgentsDate
2023Publisher
MDPIBibliographic citation
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/ph16060808Type
info:eu-repo/semantics/articlePublisher version
https://www.mdpi.com/1424-8247/16/6/808Version
info:eu-repo/semantics/publishedVersionSubject
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
Abstract
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. [-]
Is part of
Pharmaceuticals, 2023Funder Name
Ministerio de Economía y Competitividad | Universitat Jaume I
Project code
RTI2018-097345-B-I00 | PID2021-1267770B-100 | UJI-B2021-46
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