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Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity
dc.contributor.author | Blasco, Víctor | |
dc.contributor.author | Cuñat, Ana Carmen | |
dc.contributor.author | Sanz-Cervera, Juan F. | |
dc.contributor.author | Marco, J. Alberto | |
dc.contributor.author | Falomir, Eva | |
dc.contributor.author | Murga, Juan | |
dc.contributor.author | Carda, Miguel | |
dc.date.accessioned | 2018-06-14T09:36:57Z | |
dc.date.available | 2018-06-14T09:36:57Z | |
dc.date.issued | 2018-04-25 | |
dc.identifier.citation | BLASCO, Víctor; CUÑAT, Ana Carmen; SANZ-CERVERA, Juan F.; MARCO, J. Alberto; FALOMIR VENTURA, Eva; MURGA, Juan; CARDA, Miguel. (2018). Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. European Journal of Medicinal Chemistry, v. 150, p. 817-828 | ca_CA |
dc.identifier.uri | http://hdl.handle.net/10234/175146 | |
dc.description.abstract | Our efforts to get therapeutically useful colchicine derivatives for the treatment of cancer have led us to synthetize and biologically evaluate twenty-seven N,N′-disubstituted ureas containing a colchicine moiety and an aryl fragment. The cytotoxicity of the compounds, their ability to inhibit the expression of oncogenes related to telomerase activation and to the VEGF/VEGFR-2 autocrine process, such as c-MYC, hTERT and VEGF and their capability to downregulate c-MYC and VEGFR-2 proteins and the secretion of VEGF have been measured. In these biological evaluations, we have found that the change of the acetyl group in colchicines for an N-arylurea unit causes a great improvement in anticancer properties. The most promising derivatives were compounds 6 (o-Cl) and 14 (o,o-di-F) as they were able to downregulate all the tested targets at a concentration below their IC50 values. Thus, the arylurea unit enhances the potential of colchicine as an anticancer agent. | ca_CA |
dc.format.extent | 12 p. | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | Elsevier | ca_CA |
dc.relation.isPartOf | European Journal of Medicinal Chemistry (2018), v. 150 | ca_CA |
dc.rights.uri | http://rightsstatements.org/vocab/CNE/1.0/ | * |
dc.subject | Colchicine | ca_CA |
dc.subject | Urea derivatives | ca_CA |
dc.subject | Cytotoxicity | ca_CA |
dc.subject | Oncogenes downregulation | ca_CA |
dc.title | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | https://doi.org/10.1016/j.ejmech.2018.03.039 | |
dc.relation.projectID | This research has been funded by 1) the Ministerio de Economía y Competitividad (project CTQ2014-52949-P), 2) by the Universitat Jaume I (project PI-1B2015-75) and 3) by the Conselleria d’Educaciò, Investigaciò, Cultura i Sport de la Generalitat Valenciana (project PROMETEO 2013/027). | ca_CA |
dc.rights.accessRights | info:eu-repo/semantics/restrictedAccess | ca_CA |
dc.relation.publisherVersion | https://www.sciencedirect.com/science/article/pii/S0223523418302824?via%3Dihub | ca_CA |
dc.type.version | info:eu-repo/semantics/publishedVersion | ca_CA |
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