Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives
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https://doi.org/10.1016/j.ejmech.2018.03.019 |
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Title
Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivativesDate
2018-04-25Publisher
ElsevierBibliographic citation
MARZO MAS, Ana; FALOMIR VENTURA, Eva; MURGA, Juan; CARDA, Miguel; MARCO, J. Alberto. (2018). Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. European Journal of Medicinal Chemistry, v. 150, p. 591-600Type
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Abstract
Several colchicine analogues in which the N-acetyl residue has been replaced by haloacetyl, cyclohexylacetyl, phenylacetyl and various aroyl moieties have been synthesized. The cytotoxic activities of the synthesized ... [+]
Several colchicine analogues in which the N-acetyl residue has been replaced by haloacetyl, cyclohexylacetyl, phenylacetyl and various aroyl moieties have been synthesized. The cytotoxic activities of the synthesized compounds have been measured on three tumor cell lines (HT-29, MCF-7 and A549) and on one non-tumor cell line (HEK-293). These compounds exhibit high antiproliferative activities at the nanomolar level, in many cases with a higher potency than colchicine itself. Some of the compounds, particularly the haloacetyl derivatives, inhibit the polymerization of tubulin in a similar manner as colchicine. As regards the cell cycle, the most active compounds are the chlorobenzoyl and bromobenzoyl derivatives, which cause cell cycle arrest at the G2/M phase when tested at 20 nM, and the bromoacetyl derivative, which arrests the cell cycle at 15 nM. In addition, these colchicine derivatives have shown fairly active downregulating the expression of the c-Myc, hTERT and VEGF genes, as well as VEGF protein secretion, at very low concentrations. [-]
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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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