Biochemical Loci for Modulation of 5-Fluorouracil Activity

  • Peter V. Danenberg
Part of the Developments in Oncology book series (DION, volume 47)


The development of the fluoropyrimidines as anticancer drugs began in 1957 with the publication by Heidelberger of a method for the synthesis of 5-fluorouracil (FU) (1). This compound was soon found to possess significant antitumor activity in both mice (2) and men (3) and today FU and some of its derivatives, notably the deoxyribonucleoside 5-fluoro-2′-deoxyuridine (FdUrd), are extensively used in the treatment of metastatic cancers, singly or in combination with other drugs. In addition to anticancer drugs, the fluoropyrimidines have been used as biochemical tools to study a wide variety of problems in biochemistry and cell biology. As might be expected, a vast literature on fluoropyrimidines has been generated describing studies on their metabolism, mechanism of action, biochemical pharmacology, synthesis of new derivatives, and clinical antitumor activity.


Ternary Complex Thymidylate Synthetase Ternary Complex Formation Murine Colonic Adenocarcinoma L1210 Mouse Leukemia Cell 
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© Martinus Nijhoff Publishing, Boston 1986

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  • Peter V. Danenberg

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