Tetrazole derivatives as potent immunomodulatory agents in tumor microenvironment
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Títol
Tetrazole derivatives as potent immunomodulatory agents in tumor microenvironmentData de publicació
2023-11-01Editor
ElsevierISSN
0753-3322Cita bibliogràfica
Alberto Pla-López, Miguel Carda, Eva Falomir, Tetrazole derivatives as potent immunomodulatory agents in tumor microenvironment, Biomedicine & Pharmacotherapy, Volume 169, 2023, 115668, ISSN 0753-3322, https://doi.org/10.1016/j.biopha.2023.115668.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
https://www.sciencedirect.com/science/article/pii/S075333222301466XVersió
info:eu-repo/semantics/publishedVersionParaules clau / Matèries
Resum
Twenty-seven compounds bearing a tetrazole ring as a central unit have been designed, synthetized and biologically evaluated. Studies have been performed in order to compare the effect of tetrazole derivatives bearing ... [+]
Twenty-seven compounds bearing a tetrazole ring as a central unit have been designed, synthetized and biologically evaluated. Studies have been performed in order to compare the effect of tetrazole derivatives bearing amine electron-donor or nitro electron-acceptor groups. The antiproliferative activity has been determined in monoculture studies on tumor cell lines HT-29, A-549, MCF-7 and on non-tumor cell line HEK-293 as well as in co-culture studies (HT-29/THP-1). All the compounds have been studied as PD-L1 (Programmed Death Ligand 1), VEGFR-2 (Vascular Endothelial Growth Factor 2), CD-47 (Cluster of Differentiation 47) and c-Myc inhibitors. The effect on TNF-α secretion has also been determined. Bromoderivatives 23, 24 and chloroderivatives 26, 27 have demonstrated an apoptotic effect on HT-29 cancer cells. Compounds bearing an amine group have shown very promising effects as TME immunomodulatory agents. [-]
Publicat a
Biomedicine & Pharmacotherapy Volume 169, 31 December 2023.Entitat finançadora
Generalitat Valenciana | Universitat Jaume I | Ministerio de Ciencia e Innovación | European Regional Development Fund | Agencia Estatal de Investigación
Codi del projecte o subvenció
ACIF/2020/341 | UJI-B2021–46 | MCIN/AEI/ 10.13039/501100011033
Drets d'accés
info:eu-repo/semantics/openAccess
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