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Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elements
dc.contributor.author | Blasco, Víctor | |
dc.contributor.author | Murga, Juan | |
dc.contributor.author | Falomir, Eva | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Royo, Santiago | |
dc.contributor.author | Cuñat, Ana Carmen | |
dc.contributor.author | Sanz-Cervera, Juan F. | |
dc.contributor.author | Marco, J. Alberto | |
dc.date.accessioned | 2018-10-11T10:01:25Z | |
dc.date.available | 2018-10-11T10:01:25Z | |
dc.date.issued | 2018 | |
dc.identifier.citation | BLASCO, Víctor, et al. Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elements. Organic & biomolecular chemistry, 2018, vol. 16, no 32, p. 5859-5870. | ca_CA |
dc.identifier.issn | 1477-0520 | |
dc.identifier.issn | 1477-0539 | |
dc.identifier.uri | http://hdl.handle.net/10234/176679 | |
dc.description.abstract | Several tricyclic compounds inspired by the structure of combretastatin A-4 and bearing group 14 elements have been synthesized by homocoupling lithiated aryl fragments followed by ring-closing metathesis. These tricyclic compounds and their diolefin precursors were evaluated for their antiproliferative action on the tumor cell lines HT-29, MCF-7, HeLa and A-549 and on the non-tumor cell line HEK-293. In addition, their effects on the cell cycle were also measured. The tricyclic compounds show antiproliferative activity similar to that of combretastatin A-4, even though they are not so active in arresting the cell cycle. However, some diolefin precursors are able to cause accumulation of cells in the G2/M phase in a higher percentage than combretastatin A-4 itself. Inhibition of endothelial tube formation and VEGFR-2 phosphorylation of some selected compounds is comparable to that of combretastatin A-4, particularly those of tin-containing compounds 23c and 26c, whose actions exceed those of sorafenib, a clinically used VEGFR-2 inhibitor. | ca_CA |
dc.format.extent | 12 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | Royal Society of Chemistry | ca_CA |
dc.relation.isPartOf | Org. Biomol. Chem., 2018, 16 | ca_CA |
dc.rights.uri | http://rightsstatements.org/vocab/CNE/1.0/ | * |
dc.title | Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elements | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | http://dx.doi.org/10.1039/C8OB01148F | |
dc.relation.projectID | CTQ2014-52949-P ; PI-1B-2015-75 | ca_CA |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | ca_CA |
dc.relation.publisherVersion | https://pubs.rsc.org/en/content/articlelanding/2018/ob/c8ob01148f#!divAbstract | ca_CA |
dc.date.embargoEndDate | 2019-08-01 | |
dc.type.version | info:eu-repo/semantics/acceptedVersion | ca_CA |
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