Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elements
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Altres documents de l'autoria: Blasco, Víctor; Murga, Juan; Falomir, Eva; Carda, Miguel; Royo, Santiago; Cuñat, Ana Carmen; Sanz-Cervera, Juan F.; Marco, J. Alberto
Metadades
Mostra el registre complet de l'elementcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
comunitat-uji-handle4:
INVESTIGACIONMetadades
Títol
Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elementsAutoria
Data de publicació
2018Editor
Royal Society of ChemistryISSN
1477-0520; 1477-0539Cita bibliogràfica
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.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
https://pubs.rsc.org/en/content/articlelanding/2018/ob/c8ob01148f#!divAbstractVersió
info:eu-repo/semantics/acceptedVersionResum
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 ... [+]
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. [-]
Publicat a
Org. Biomol. Chem., 2018, 16Proyecto de investigación
CTQ2014-52949-P ; PI-1B-2015-75Drets d'accés
http://rightsstatements.org/vocab/CNE/1.0/
info:eu-repo/semantics/openAccess
info:eu-repo/semantics/openAccess
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