Experimental studies at Southern Research Institute with DTIC (NSC-45388).

Several years ago the diazotization of 5-aminoimidazole-4-carboxamide was found to give an internal diazonium salt, 5-diazoimidazole-4-carboxamide, which demonstrated marginal activity against some murine neoplasms. In an effort to improve this activity and develop a clinically useful agent, this compound was converted to a number of derivatives including DTIC, an agent that showed encouraging activity against a variety of rodent neoplasms. Studies carried out at Southern Research Institute on the chemistry, metabolism, and biologic activity of DTIC and its congeners are discussed briefly.