5-(Acylethynyl)-1-(2-hydroxyethoxy)methyl uracils (2)-(6) were synthes
ised in excellent yields from 1-(2-acetoxyethoxy)methyl-5-iodouracil (
7) utilising palladium-copper catalysed reactions. Compounds (2)-(5) w
ere shown to be highly active against CCRF-CEM (IC50 0.6-1.6 mu M) and
L1210/0 cells (IC50 0.7-2.2 mu M) in culture, and thus exhibit greate
r activity than their parent bases. Copyright (C) 1996 Elsevier Scienc
e Ltd