Abstract
The reaction of methyl 4-(2′-nitroimidazolyl)crotonate ( 1) with glutathione (GSH) in phosphate buffer solution was examined to form the corresponding 1,4-addition products which have been isolated and fully characterized by spectroscopy. The same reaction took place within EMT6/KU cells with intracellular GSH to give the drug-GSH conjugates. The enhance radiosensitizing activity of 1 on hypoxic EMT6/KU cells by alteration in both D 0 and n parameters of dose-survival curve was suggested as the result of the intracellular NPSH-depletion by the α,β-unsaturated carbonyl side chain of 1.
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