ABSTRACT
By the early 1950s, a number of nucleic acid analogues were under development for the treatment of cancer. Rat hepatomas were shown to demonstrate increased uptake and catabolism of [2-14C]uracil when compared with normal liver tissue.1
Furthermore, it was noted that fluorine could alter cellular metabolism when it was substituted for hydrogen in various biologic compounds. Based on these observations, Heidelberger et al2 synthesized the fluoropyrimidine 5-fluorouracil (5-FU) and injected it into the peritoneal cavities of tumor-bearing mice and rats. The drug showed significant antitumor activity and appeared to be well tolerated.
