Uracil Mustard, a New Alkylating Agent for Oral Administration in the Management of Patients with Leukemia and Lymphoma

Abstract

SINCE the introduction of nitrogen mustard, methyl-bis-β-(chloroethyl)-amine, or HN₂ (Fig. 1), as a therapeutic agent in human cancer a number of analogues and related alkylating agents have been synthesized and evaluated as potential antitumor drugs. The goal has been to obtain compounds exhibiting greater antitumor effect and less general toxicity to the host.Lyttle and Petering^{1 , 2} synthesized 5-bis-(2-chloroethyl)-aminouracil, uracil mustard, or NSC-34462 or U-8344 (Fig. 2), replacing the methyl group of nitrogen mustard with a physiologically active group, uracil. This agent, which does not appear to be a uracil antagonist, has been found to be a particularly active carcinostatic . . .