Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity
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Other documents of the author: Blasco, Víctor; Cuñat, Ana Carmen; Sanz-Cervera, Juan F.; Marco, J. Alberto; Falomir, Eva; Murga, Juan; Carda, Miguel
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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https://doi.org/10.1016/j.ejmech.2018.03.039 |
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Title
Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activityAuthor (s)
Date
2018-04-25Publisher
ElsevierBibliographic 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. 817-828Type
info:eu-repo/semantics/articleVersion
info:eu-repo/semantics/publishedVersionSubject
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 ... [+]
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. [-]
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European Journal of Medicinal Chemistry (2018), v. 150Investigation project
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).Rights
http://rightsstatements.org/vocab/CNE/1.0/
info:eu-repo/semantics/restrictedAccess
info:eu-repo/semantics/restrictedAccess
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