Mostrar el registro sencillo del ítem
Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3′-aminocombretastatin A-4
dc.contributor.author | Conesa Milián, Laura | |
dc.contributor.author | Falomir, Eva | |
dc.contributor.author | Murga, Juan | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Marco, J. Alberto | |
dc.date.accessioned | 2019-04-04T07:17:51Z | |
dc.date.available | 2019-04-04T07:17:51Z | |
dc.date.issued | 2019-01-15 | |
dc.identifier.citation | CONESA MILIÁN, Laura; FALOMIR, Eva; MURGA CLAUSELL, Juan; CARDA USÓ, Miguel; MARCO VENTURA, Juan Alberto (2019). Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3′-aminocombretastatin A-4. European Journal of Medicinal Chemistry, v. 162, p. 781-792 | ca_CA |
dc.identifier.uri | http://hdl.handle.net/10234/182192 | |
dc.description.abstract | Twenty-six compounds derived from 3′-aminocombretastatin A-4 (AmCA-4) containing a urea fragment mimicking the structure of Sorafenib, have been synthesized and evaluated as antiangiogenic compounds. Antiproliferative activity of all the synthetic ureas has been measured on tumor cell lines HT-29, MCF-7, HeLa, A-549 and HL-60 as well as on the endothelial cell line HMEC-1 and on the non-tumor cell line HEK-293. Preliminary docking studies were developed in order to predict which ureas show better interactions with the protein VEGFR-2. Then, the selected derivatives were evaluated in terms of their apoptotic effect and antiangiogenic properties. In this regard, VEGFR-2/ligand interactions were determined by flow cytometry and immunofluorescence techniques. Inhibition of VEGFR-2 tyrosine kinase activity in both the A-549 and HMEC-1 cell lines was also carried out. In addition, tube formation inhibition was studied in endothelial cells. Ortho-chloro substituted urea 5 and ortho-bromo substituted urea 8 were the most active ones in both down-regulation of VEGFR-2 and inhibition of the kinase activity of this receptor, with better results than those obtained with sunitinib and sorafenib. | ca_CA |
dc.format.extent | 12 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | Elsevier | ca_CA |
dc.relation.isPartOf | European Journal of Medicinal Chemistry (2019), v. 162 | ca_CA |
dc.rights.uri | http://rightsstatements.org/vocab/CNE/1.0/ | * |
dc.subject | Aminocombretastatin A-4 | ca_CA |
dc.subject | Ureas | ca_CA |
dc.subject | Apoptosis | ca_CA |
dc.subject | Angiogenesis | ca_CA |
dc.subject | VEGFR-2 | ca_CA |
dc.title | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3′-aminocombretastatin A-4 | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | https://doi.org/10.1016/j.ejmech.2018.11.023 | |
dc.relation.projectID | 1) Ministerio de Economía y Competitividad (project CTQ2014-52949-P); 2) Universitat Jaume I (project PI-1B2015-75); 3) Conselleria d’Educació, Investigació, Cultura i Sport de la Generalitat Valenciana (project PROMETEO 2013/027); 4) Spanish Ministry of Education, Culture and Sport for the FPU fellowship (FPU14/00878). | ca_CA |
dc.rights.accessRights | info:eu-repo/semantics/restrictedAccess | ca_CA |
dc.relation.publisherVersion | https://www.sciencedirect.com/science/article/pii/S0223523418309814?via%3Dihub | ca_CA |
dc.type.version | info:eu-repo/semantics/publishedVersion | ca_CA |
Ficheros en el ítem
Ficheros | Tamaño | Formato | Ver |
---|---|---|---|
No hay ficheros asociados a este ítem. |
Este ítem aparece en la(s) siguiente(s) colección(ones)
-
QUIO_Articles [701]
Articles de publicacions periòdiques