Carbohydrate Research 2011-10-18

Synthesis of various 5-alkoxymethyluracil analogues and structure-cytotoxic activity relationship study.

Lucie Brulíková, Petr Džubák, Marián Hajdúch, Jan Hlaváč

Index: Carbohydr. Res. 346(14) , 2136-44, (2011)

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Abstract

A number of 5-alkoxymethyluracil analogues were synthesized to evaluate their cytotoxic activity. 5-Alkoxymethyluracil derivatives 1 were prepared via known nucleophilic substitution of 5-chloromethyluracil 5 and subsequently transformed to their corresponding nucleosides 2. All prepared compounds were submitted to cytotoxic activity testing against drug sensitive and drug resistant leukaemia cells and solid tumour derived cell lines. In addition, the cytotoxic activity of 5-alkoxymethyluracil analogues 1 and 2 was compared with the previously published 5-[alkoxy(4-nitrophenyl)methyl]uracil analogues 3 and 4. Extensive structure-cytotoxic activity relationship studies are reported.Copyright © 2011 Elsevier Ltd. All rights reserved.