Montgomery J A
Cancer Treat Rep. 1976 Feb;60(2):125-34.
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.
几年前，人们发现5-氨基咪唑-4-甲酰胺重氮化可生成一种内重氮盐，即5-重氮咪唑-4-甲酰胺，它对某些小鼠肿瘤显示出微弱活性。为了提高这种活性并开发一种临床上有用的药物，该化合物被转化为多种衍生物，包括达卡巴嗪（DTIC），这是一种对多种啮齿动物肿瘤显示出令人鼓舞活性的药物。本文简要讨论了南方研究所对达卡巴嗪及其同类物的化学、代谢和生物活性所进行的研究。
