Unusual cytotoxicities of 5-(acylethynyl)-1-(2-hydroxyethoxy)methyluracils

5-(Acylethynyl)-1-(2-hydroxyethoxy)methyl uracils ( 2)-( 6) were synthesised in excellent yields from 1-(2-acetoxyethoxy)methyl-5-iodouracil ( 7) utilising palladium-copper catalysed reactions. Compounds ( 2)-( 5) were shown to be highly active against CCRF-CEM (IC 50 0.6–1.6 μM) and L1210/0 cells (...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-07, Vol.6 (13), p.1497-1502
Main Authors: Kundu, Nitya G., Mahanty, Jyan S., Spears, C.Paul
Format: Article
Language:English
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Summary:5-(Acylethynyl)-1-(2-hydroxyethoxy)methyl uracils ( 2)-( 6) were synthesised in excellent yields from 1-(2-acetoxyethoxy)methyl-5-iodouracil ( 7) utilising palladium-copper catalysed reactions. Compounds ( 2)-( 5) were shown to be highly active against CCRF-CEM (IC 50 0.6–1.6 μM) and L1210/0 cells (IC 50 0.7–2.2 μM) in culture, and thus exhibit greater activity than their parent bases. 5-(Acylethynyl)-1-(2-hydroxyethoxy)methyluracils, synthesized in excellent yields from 1-(2-acetoxyethoxy)methyl-5-iodouracil through palladium-copper catalyzed reactions, were found to be highly active against CCRF-CEM and L1210/0 cells in culture. They were more potent than their parent bases.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(96)00256-9