Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity
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Other documents of the author: Torijano Gutiérrez, Sandra Adela; Diaz-Oltra, Santiago; Falomir, Eva; Murga, Juan; 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 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activityAuthor (s)
Date
2013-12xmlui.dri2xhtml.METS-1.0.item-edition
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ElsevierISSN
0968-0896Bibliographic citation
TORIJANO-GUTIÉRREZ, Sandra, et al. Synthesis of combretastatin A-4< i> O</i>-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity. Bioorganic & medicinal chemistry, 2013, vol. 21, no 23, p. 7267-7274Type
info:eu-repo/semantics/articlePublisher version
http://www.sciencedirect.com/science/article/pii/S0968089613008535Subject
Abstract
We here report the synthesis and biological evaluation of several combretastatin A-4 derivatives alkylated at the phenol hydroxyl group. Some of these derivatives contain an (E)-arylalkene fragment reminiscent of that ... [+]
We here report the synthesis and biological evaluation of several combretastatin A-4 derivatives alkylated at the phenol hydroxyl group. Some of these derivatives contain an (E)-arylalkene fragment reminiscent of that present in some natural stilbenes like resveratrol. The cytotoxicities towards one human healthy kidney embryonic and two tumoral cell lines were determined. In addition, the ability of these compounds to inhibit the production of the vascular endothelial growth factor (VEGF) was measured. Finally, the expression of genes controlling the production of telomerase was measured. Some of the compounds were found to have an activity comparable or higher than that of combretastatin A-4 in at least one of the aforementioned biological properties. The compounds with the (E)-arylalkene fragment were in general terms more active than the simple O-alkyl derivatives. However, no clear structure/activity correlations were perceived when comparing the observed compound activities across the three biological properties. This points out the existence of marked differences between the mechanisms responsible for their cytotoxicity. [-]
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Bioorganic and Medicinal Chemistry, 2013, Vol. 21, no. 23Rights
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