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Comparison of Mutagenicity, Antitumor Activity, and Chemical Properties of Selected Nitrosoureas and Nitrosoamides

Departments of Chemistry [E. H. W., J. M.] and Biology [P. E. H., D. L. B.], and the Oncology Center [R. B. B., M. C.], Johns Hopkins University, Baltimore, Maryland 21205

A number of nitrosoureas and nitrosoamides have been compared with respect to mutagenicity for Salmonella typhimurium, in vitro cytotoxicity, in vivo toxicity and antitumor activity against murine L1210 leukemia, and chemical properties. Despite chemical similarities between the nitrosoureas and nitrosoamides, they show important differences in biological activity. Some of the nitrosoureas are very active antitumor agents, and they are less mutagenic than are the corrsponding nitrosoamides, which lack antitumor activity.

¹ Recipient of National Cancer Institute Grants CA-16783 and CA-06973.

² To whom requests for reprints should be addressed, at the Pharmacology Laboratory, Johns Hopkins Oncology Center, Baltimore, Md. 21205.

³ Recipient of National Cancer Institute Grant CA-18387.

⁴ Recipient of National Institute of Allergy and Infectious Diseases Grant AI-01650.

Received 8/ 7/78. Accepted 12/27/78.