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Aryl urea based scaffolds for multitarget drug discovery in anticancer immunotherapies
dc.contributor.author | Martín Beltrán, Celia | |
dc.contributor.author | Gil-Edo, Raquel | |
dc.contributor.author | Hernández Ribelles, Germán | |
dc.contributor.author | Agut, Raúl | |
dc.contributor.author | Marí Mezquita, Pilar | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Falomir, Eva | |
dc.date.accessioned | 2021-06-09T08:14:27Z | |
dc.date.available | 2021-06-09T08:14:27Z | |
dc.date.issued | 2021-04-06 | |
dc.identifier.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/ph14040337 | ca_CA |
dc.identifier.uri | http://hdl.handle.net/10234/193345 | |
dc.description.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) 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. | ca_CA |
dc.format.extent | 11 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | MDPI | ca_CA |
dc.relation.isPartOf | Pharmaceuticals Vol. 14, Issue 4 | ca_CA |
dc.relation.uri | https://www.mdpi.com/1424-8247/14/4/337/s1 | ca_CA |
dc.rights | Atribución 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-sa/4.0/ | * |
dc.subject | styryl aryl urea | ca_CA |
dc.subject | phenethyl aryl urea | ca_CA |
dc.subject | PD-L1 | ca_CA |
dc.subject | VEGFR-2 | ca_CA |
dc.subject | c-Myc | ca_CA |
dc.subject | multitarget inhibitors | ca_CA |
dc.subject | immunomodulation | ca_CA |
dc.subject | angiogenesis | ca_CA |
dc.title | Aryl urea based scaffolds for multitarget drug discovery in anticancer immunotherapies | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | ca_CA |
dc.type.version | info:eu-repo/semantics/publishedVersion | ca_CA |
project.funder.name | Ministerio de Economía y Competitividad | ca_CA |
project.funder.name | Universitat Jaume I | ca_CA |
oaire.awardNumber | RTI2018-097345-B-I00 | ca_CA |
oaire.awardNumber | UJI-B2018-38 | ca_CA |
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