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Chloroethylnitro soureas have proven to be highly effective cancer chemotherapeutic agents that are in common clinical use. Although the most widely used analog in this class of agents, BCNU, was introduced in the mid 1960s, efforts to develop new compounds with selective sites of action and reduced toxicity have continued to the present day. Along with these developments, studies into the mechanisms of activation and action have been reported and attempts have been made to identify the active species responsible for the antitumor activity and toxicity of this class of drug. Biodistribution and metabolism studies have also been conducted in order to reveal the fate of these chemically reactive agents. Many recent reports have resolved questions concerning the activation of these agents and revealed that activity may be influenced by unusually complex structurally specific interactions. These aspects of the literature on Chloroethylnitro soureas have been reviewed in detail in this article.
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