Abstract
Although the title of this chapter implies that there has been a successful rational approach to the design of folic acid antagonists, a review of the history of these agents suggests quite the opposite. In more recent years the light of rationalism has begun to gleam more strongly and there promises to be an “age of reason” in the design of antifolates. The objectives of this chapter are two-fold. First, by reviewing the properties of existing agents it is hoped to demonstrate that perhaps a retrospective approach to old agents might be extremely productive in light of our current knowledge of folate biochemistry, and second, by consideration of new areas of considerable promise, more truly rational approaches will be discussed which could greatly enhance the therapeutic utility of these agents.
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Mead, J.A.R. (1974). Rational Design of Folic Acid Antagonists. In: Sartorelli, A.C., Johns, D.G. (eds) Antineoplastic and Immunosuppressive Agents Part I. Handbuch der experimentellen Pharmakologie / Handbook of Experimental Pharmacology, vol 38 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-65678-1_4
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