Purine Antimetabolites

  • Wolfgang Sadée
  • Binh Nguyen
Part of the Cancer Growth and Progression book series (CAGP, volume 10)


The ever increasing number of purine analogs with potent biological properties, either isolated from various microorganisms or obtained by chemical synthesis, can elicit an unusual fascination with this subject. What are the unique features of purine metabolism in different species and cell types that allow one organism to accumulate high concentrations of cytotoxic purines, presumably as a defense mechanism without harm to itself? And more relevant to the present review, can these natural antipurines or their synthetic counterparts be utilized to preferentially kill cancer cells without affecting normal tissues? The answer to the latter question must be a qualified because with the exception of the 6-thiopurines there are no purine antimetabolites in general clinical use in the treatment of neoplasms. However, among the new anticancer drugs undergoing clinical evaluation, the purine antimetabolites indeed play a very prominent role. Of 37 experimental anticancer drugs for which INDA’s were filed by the NCI during the period 1977–1983, no less than seven are purine antimetabolites (64). These experimental antipurines are:
  • L-alanosine (NSC 51143)

  • tiazofurin (NSC 286193)

  • fludarabine phosphate; 5-fluoro-ara-AMP (NSC 312887)

  • acivicin (NSC 163501)

  • DON; 6-diazo-5-oxo-L-norleucine (NSC 7365)

  • pentostatin; deoxycoformycin (NSC 218321) (potentiates araA activity)

  • 9-arabinosyl adenine; araA (NSC 404241) (in combination with pentoatatin).


Mycophenolic Acid Purine Nucleotide Purine Biosynthesis Purine Metabolite Adenylosuccinate Lyase 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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© Kluwer Academic Publishers 1989

Authors and Affiliations

  • Wolfgang Sadée
  • Binh Nguyen

There are no affiliations available

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