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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Other documents of the author: Agut, Raúl; Falomir, Eva; Murga, Juan; Martín Beltrán, Celia; Gil Edo, Raquel; Pla, Alberto; Carda, Miguel; Marco, J. Alberto
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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Title
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 ExpressionAuthor (s)
Date
2020Publisher
MDPIISSN
1420-3049Bibliographic citation
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.Type
info:eu-repo/semantics/articlePublisher version
https://www.mdpi.com/1420-3049/25/3/660Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
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. [-]
Is part of
Molecules 2020, 25, 660Investigation project
project CTQ2014-52949-P, project RTI2018-097345-B-I00, project UJI-B2018-38Rights
info:eu-repo/semantics/openAccess
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