Styryl carbamate backbones for the discovery of TME-disrupting agents
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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INVESTIGACIONMetadata
Title
Styryl carbamate backbones for the discovery of TME-disrupting agentsDate
2024Publisher
ElsevierISSN
2211-7156/Bibliographic citation
BOU-PUERTO, Amelia; CARDA, Miguel; FALOMIR, Eva. Styryl Carbamates Backbones for the discovery of TME-disruptors Agents. Results in Chemistry, 2024, 101372Type
info:eu-repo/semantics/articlePublisher version
https://www.sciencedirect.com/science/article/pii/S2211715624000687Version
info:eu-repo/semantics/publishedVersionSubject
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Abstract
Twenty-one styryl carbamates have been designed, synthetized and characterized by their physical properties. Afterwards, their potential activity as tumor microenvironment disruptors has been evaluated. First, antip ... [+]
Twenty-one styryl carbamates have been designed, synthetized and characterized by their physical properties. Afterwards, their potential activity as tumor microenvironment disruptors has been evaluated. First, antiproliferative studies on tumor cell lines HT-29, A-549 and MCF-7 and on non-tumor cell line HEK-293 were carried out. Then, the antiproliferative activity of some selected compounds was evaluated on co-cultures of A-549 and immune cells, Jurkat T or monocytes THP-1. To determine their potential as oncoinflammation regulators, the secretion levels of IL-6, TNF-α and SAA-1 were, also, determined from these co-culture assays. Then, the effect on the expression levels of anticancer targets PD-L1 in both A-549 and monocytes THP-1 were established and, finally, the expression of CD80 and CD11b in THP-1. Compounds 9–13 bearing halophenyl carbamate units exhibited promising results as TME disruptors and inflammation regulators. [-]
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Results in Chemistry, 2024, 101372Funder Name
Ministerio de Ciencia, Innovación y Universidades | Fondo Europeo de Desarrollo Regional | Ministerio de Economía y Competitividad | Universitat Jaume I | Agencia Estatal de Investigación
Project code
PID2021-126277OB-100 | RTI2018-097345-B-I00 | UJI-B2021-46
Rights
info:eu-repo/semantics/openAccess
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- QUIO_Articles [701]