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Antimetabolites in Cancer Chemotherapy

1991; Springer Nature; Linguagem: Inglês

10.1007/978-1-4899-2638-8_2

2214-8019

Stephen Clarke, Ann L. Jackman, Kenneth R. Harrap,

Cancer Treatment and Pharmacology

Some 43 years have elapsed since the first successful use of an anti-metabolite, methotrexate (MTX), in the treatment of malignant disease. In the intervening years much attention has been devoted to the discovery and development of other anticancer anti-metabolites: several, notably 5-fluorouracil (5FU), 6-mercaptopurine (6MP), 6-thioguanine (6-TG), cytosine arabinoside (ARA-C), together with MTX, now fulfill an established role in the chemotherapy of malignant diseases. Enthusiasm for the discovery and development of novel antimetabolites persists and there are several which are presently at various stages of development. In this discussion we will restrict our comments to those new antimetabolites listed in Table 1, which have reached the clinic. The structures of these agents are shown in Figure 1 and sites of action of some of the agents are shown in Figure 2.