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Rational Design of Purine Nucleoside Analogs

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Antineoplastic and Immunosuppressive Agents Part I

Abstract

The rational design of cancer chemotherapeutic agents must ultimately be based on an exploitable biochemical difference between normal host cells and the invading cancer cells. Although much is known about the biologic activity of certain agents, such as 6-mercaptopurine and 6-thioguanine, the basis of their selective action on cancer cells is still not fully understood. This selectivity could result from greater catabolism of the drug by normal cells, since it is known that the xanthine oxidase level of cancer cells is generally lower than that of normal cells (Bergel et al., 1957). The metabolic state of treated cells must also be important, since established solid tumors with a low growth fraction do not normally respond well to antimetabolites, purines or otherwise (Laster et al., 1969). Because of our limited knowledge about the basis of selective toxicity of purine antagonists, we must base the design of new agents on what is known about the metabolism and the mechanisms of action of purine analogs and the effects of structural changes on both of these. Although some of these topics will be discussed in more detail later in this volume, our knowledge of the biologically active purine analogs will be summarized briefly here.

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  2. Laboratory of Chemical Pharmacology, National Cancer Institute, National Istitutes of Health, Bethesda, Maryland, 20014, USA

    David G. Johns M. D.

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Montgomery, J.A. (1974). Rational Design of Purine Nucleoside Analogs. 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_5

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  • DOI: https://doi.org/10.1007/978-3-642-65678-1_5

  • Publisher Name: Springer, Berlin, Heidelberg

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  • Online ISBN: 978-3-642-65678-1

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