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6-Thiopurines

  • Chapter
Antineoplastic and Immunosuppressive Agents

Abstract

It was recognized through early studies with 2,6-diaminopurine, 8-azaguanine, and 6-mercaptopurine that chemotherapy with analogs of nucleic acid bases might afford control of some aspects of neoplastic disease (Elion and Hitchings, 1965). The inhibitory activity of thiopurines toward rodent tumors, and the value of 6-mercaptopurine in the treatment of human leukemias (the latter was first reported by Burchenal et al., 1953), focused a great deal of attention on the thiopurines; the immunosuppressive and anti-inflammatory properties of the thiopurines were subsequently recognized (thiopurine immunosuppressive effects have been reviewed by Schwartz and André, 1962; Hitchings and Elion, 1963, 1969; Berenbaum, 1967; Ashton et al., 1970; anti-inflammatory effects have been discussed by Page et al., 1962a,b; Hersh et al., 1966; Berenbaum, 1967; Furth, 1970). A great effort has been made to synthesize related analogs and to understand the metabolism and metabolic effects of thiopurines in a variety of cell systems. It has become apparent that 6-mercaptopurine and its homolog, 6-thioguanine, produce cytotoxic effects which are manifested in rapidly proliferating cell populations in vivo and in vitro. Despite an extensive research effort, the biochemical bases of the cytotoxic effects of 6-mercaptopurine and 6-thioguanine are only dimly perceived at present.

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Authors
  1. A. R. P. Paterson
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  2. D. M. Tidd
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Editors and Affiliations

  1. Department of Pharmacology, Yale University School of Medicine, 06510, New Haven, Connecticut, USA

    Alan C. Sartorelli (Professor) (Professor)

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

    David G. Johns M.D.

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Paterson, A.R.P., Tidd, D.M. (1975). 6-Thiopurines. In: Sartorelli, A.C., Johns, D.G. (eds) Antineoplastic and Immunosuppressive Agents. Handbuch der experimentellen Pharmakologie / Handbook of Experimental Pharmacology, vol 38 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-65806-8_18

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  • DOI: https://doi.org/10.1007/978-3-642-65806-8_18

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