Synthesis of Combretastatin A-4 and 3 0 -Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression
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Otros documentos de la autoría: Agut, Raúl; Falomir, Eva; Murga, Juan; Martín Beltrán, Celia; Gil Edo, Raquel; Pla, Alberto; Carda, Miguel; Marco, J. Alberto
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INVESTIGACIONMetadatos
Título
Synthesis of Combretastatin A-4 and 3 0 -Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene ExpressionAutoría
Fecha de publicación
2020Editor
MDPIISSN
1420-3049Cita bibliográfica
Agut, R.; Falomir, E.; Murga, J.; Martín-Beltrán, C.; Gil-Edo, R.; Pla, A.; Carda, M.; Marco, J.A. Synthesis of Combretastatin A-4 and 3′-Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression. Molecules 2020, 25, 660.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
https://www.mdpi.com/1420-3049/25/3/660Versión
info:eu-repo/semantics/publishedVersionPalabras clave / Materias
Resumen
Natural product combretastatin A-4 (CA-4) and its nitrogenated analogue
3
0
-aminocombretastatin A-4 (AmCA-4) have shown promising antitumor activities. In this study,
a range of CA-4 and AmCA-4 derivatives ... [+]
Natural product combretastatin A-4 (CA-4) and its nitrogenated analogue
3
0
-aminocombretastatin A-4 (AmCA-4) have shown promising antitumor activities. In this study,
a range of CA-4 and AmCA-4 derivatives containing amino acid pendants have been synthesized in
order to compare their biological actions with those of their parent compounds. Thus, inhibition of
cell proliferation on tumor cell lines HT-29, MCF-7 and A-549, as well as on the nontumor cell line
HEK-273; in vitro tubulin polymerization; mitotic cell arrest; action on the microtubule cell network
and inhibition of VEGF, hTERT, and c-Myc genes have been evaluated. Some AmCA-4 derivatives
bearing L-amino acids exhibited inhibition of cell proliferation at low nanomolar levels exceeding
the values shown by AmCA-4. Furthermore, while CA-4 and AmCA-4 derivatives do not show
significant effects on the in vitro tubulin polymerization and cell cycle arrest, some selected CA-4 and
AmCA-4 derivatives are able to cause total depolymerization of the microtubule network on A-549
cells. The best results were obtained in the inhibition of gene expression, particularly on the VEGF
gene, in which some AmCA-4 derivatives greatly exceeded the inhibition values achieved by the
parent compound. [-]
Publicado en
Molecules 2020, 25, 660Proyecto de investigación
project CTQ2014-52949-P, project RTI2018-097345-B-I00, project UJI-B2018-38Derechos de acceso
info:eu-repo/semantics/openAccess
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