Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides

[Display omitted] Seventeen silyl- and trityl-modified (5′-O- and 3′,5′-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentration of 100μM against a sma...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2016-06, Vol.24 (12), p.2716-2724
Hauptverfasser: Panayides, Jenny-Lee, Mathieu, Véronique, Banuls, Laetitia Moreno Y., Apostolellis, Helen, Dahan-Farkas, Nurit, Davids, Hajierah, Harmse, Leonie, Rey, M.E. Christine, Green, Ivan R., Pelly, Stephen C., Kiss, Robert, Kornienko, Alexander, van Otterlo, Willem A.L.
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Sprache:eng
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Zusammenfassung:[Display omitted] Seventeen silyl- and trityl-modified (5′-O- and 3′,5′-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentration of 100μM against a small panel of tumor cell lines (HL-60, K-562, Jurkat, Caco-2 and HT-29). The entire set was also tested at varying concentrations against two human glioma lines (U373 and Hs683) to obtain GI50 values, with the best results being values of ∼25μM.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2016.04.036