Aryl urea based scaffolds for multitarget drug discovery in anticancer immunotherapies
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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Title
Aryl urea based scaffolds for multitarget drug discovery in anticancer immunotherapiesAuthor (s)
Date
2021-04-06Publisher
MDPIBibliographic citation
Martín-Beltrán, C.; Gil-Edo, R.; Hernández-Ribelles, G.; Agut, R.; Marí-Mezquita, P.; Carda, M.; Falomir, E. Aryl Urea Based Scaffolds for Multitarget Drug Discovery in Anticancer Immunotherapies. Pharmaceuticals 2021, 14, 337. https:// doi.org/10.3390/ph14040337Type
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Abstract
Twenty-one styryl and phenethyl aryl ureas have been synthetized and biologically evaluated as multitarget inhibitors of Vascular endothelial growth factor receptor-2 VEGFR-2 and programmed death-ligand-1 (PD-L1) ... [+]
Twenty-one styryl and phenethyl aryl ureas have been synthetized and biologically evaluated as multitarget inhibitors of Vascular endothelial growth factor receptor-2 VEGFR-2 and programmed death-ligand-1 (PD-L1) proteins in order to overcome resistance phenomena offered by cancer. The antiproliferative activity of these molecules on several tumor cell lines (HT-29, MCF-7, HeLa and A549), on the endothelial cell line human microvascular endothelial cells (HMEC)-1 and on the non-tumor cell line human embryonic kidney cells (HEK)-293 has been determined. Some derivatives were evaluated for their antiangiogenic properties such as their ability to inhibit microvessel formation using HMEC-1 or their effect on VEGFR-2 in both cancer and endothelial cell lines. In addition, the immunomodulator action of a number of selected compounds was also studied on PD-L1 and c-Myc proteins. Compounds 16 and 23 (Z) and (E)-styryl p-bromophenyl urea, respectively, showed better results than sorafenib in down-regulation of VEGFR-2 and also improved the effect of the anti-PD-L1 compound BMS-8 on both targets, PD-L1 and c-Myc proteins. [-]
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Pharmaceuticals Vol. 14, Issue 4Related data
https://www.mdpi.com/1424-8247/14/4/337/s1Funder Name
Ministerio de Economía y Competitividad | Universitat Jaume I
Project code
RTI2018-097345-B-I00 | UJI-B2018-38
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info:eu-repo/semantics/openAccess
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