title: Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides.
abstract: 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.
authors.affiliation: Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa; Pioneering Health Sciences, CSIR Biosciences, PO Box 395, Pretoria 0001, South Africa.
authors.forename: Jenny-Lee
authors.initials: JL
authors.lastname: Panayides
authors.affiliation: Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Véronique
authors.initials: V
authors.lastname: Mathieu
authors.affiliation: Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Laetitia Moreno Y
authors.initials: LM
authors.lastname: Banuls
authors.affiliation: Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa.
authors.forename: Helen
authors.initials: H
authors.lastname: Apostolellis
authors.affiliation: Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa.
authors.forename: Nurit
authors.initials: N
authors.lastname: Dahan-Farkas
authors.affiliation: Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa; Department of Biochemistry and Microbiology, Nelson Mandela Metropolitan University, PO Box 77000, Port Elizabeth 6031, South Africa.
authors.forename: Hajierah
authors.initials: H
authors.lastname: Davids
authors.affiliation: Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa.
authors.forename: Leonie
authors.initials: L
authors.lastname: Harmse
authors.affiliation: School of Molecular and Cellular Biology, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa.
authors.forename: M E Christine
authors.initials: ME
authors.lastname: Rey
authors.affiliation: Department of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch, Matieland 7602, South Africa.
authors.forename: Ivan R
authors.initials: IR
authors.lastname: Green
authors.affiliation: Department of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch, Matieland 7602, South Africa.
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Pelly
authors.affiliation: Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Robert
authors.initials: R
authors.lastname: Kiss
authors.affiliation: Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, USA.
authors.forename: Alexander
authors.initials: A
authors.lastname: Kornienko
authors.affiliation: Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa; Department of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch, Matieland 7602, South Africa. Electronic address: wvo@sun.ac.za.
authors.forename: Willem A L
authors.initials: WA
authors.lastname: van Otterlo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009705:Nucleosides
keywords: 1,3-Dihydroxy-1,1,3,3-tetraisopropyldisiloxane; Antiproliferative activities; Dimethoxytrityl; Nucleosides; Silyl protecting groups; tert-Butyldimethylsilyl