Pyrimidine and Purine Antimetabolites

Abstract

Overview The development of pyrimidine and purine antimetabolite drugs has been based on the rationale that nucleic acids are critical to cell replication and, therefore, the pyrimidine and purine bases (and their nucleosides) that are the “building blocks” necessary to synthesize nucleic acids are themselves potential sites for designing drugs that could be effective in inhibiting nucleic acid synthesis, whether that be in bacteria, viruses, or tumor cells. In this chapter, the various antimetabolites or analogs of uracil/thymine, cytidine/deoxycytidine, hypoxanthine/guanine, and adenosine that are currently used in the management of cancer are presented and reviewed with regard to metabolism, mechanism of action, clinical pharmacology, clinical activity, and toxicity.