Modified N,O-Nucleosides: Design, Synthesis, and Anti-tumour Activity
Loredana Maiuolo A D , Olga Bortolini B D , Antonio De Nino A , Beatrice Russo A , Riccardo Gavioli C and Fabio Sforza CA Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Via P. Bucci, 87036 Rende (CS), Italy.
B Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Borsari 46, 44121 Ferrara, Italy.
C Dipartimento di Biochimica e Biologia Molecolare, Università di Ferrara, Via Fossato di Mortara 74, 44121 Ferrara, Italy.
D Corresponding authors. Email: maiuolo@unical.it; brl@unife.it
Australian Journal of Chemistry 67(4) 670-674 https://doi.org/10.1071/CH13511
Submitted: 25 September 2013 Accepted: 4 December 2013 Published: 23 January 2014
Abstract
A preliminary library of modified N,O-nucleosides was prepared and tested on a selected number of human cancer lines that include SKOV3, SW480, and K562. Thymine, N-benzyl substituents, and aromatic rings contribute to an increase of the biological activity, up to 10–25 μM, that appeared also reliant on the calculated lipophilicity of the nucleosides, expressed as cLogP, where P represents the partition coefficient of a solute between n-octanol and water.
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