• Garth Powis
Part of the Cancer Growth and Progression book series (CAGP, volume 10)


The nitrosoureas represent a large and extensively studied family of antitumor agents. They exhibit a broader spectrum of activity against experimental tumors than any other class of agents and are one of the few groups of compounds to cross the so-called blood-brain barrier at therapeutically effective concentrations. Clinically the nitrosoureas are used against a variety of human solid tumors. There continues to be of interest in the development of new nitrosourea analogs with greater activity and reduced toxicity. The basic nitrosourea structure and analogs discussed in this chapter are shown in Fig. 1. Observations in the late 1950’s that N-methyl-N′-nitro-N-nitrosoguanidine, a precursor of the methylating agent diazomethane, had activity against murine L1210 leukemia led to studies identifying the N-nitroso function as important for cytotoxicity. Nitrosoureas were the most active N-nitroso agents (81, 82 and references therein). Structure-activity studies led to the development of chloroethylnitrosoureas and observations that one analog, BCNU,* was curative against L1210 leukemia implanted intracranially or intraperitoneally (51, 105).


Antitumor Activity Human Tumor Xenograft Brain Tumor Model Cyclohexyl Ring Phenobarbital Pretreatment 
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© Kluwer Academic Publishers 1989

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  • Garth Powis

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