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Folate antimetabolites inhibitory to de novo purine synthesis

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New Drugs, Concepts and Results in Cancer Chemotherapy

Part of the book series: Cancer Treatment and Research ((CTAR,volume 58))

Abstract

The discovery of the activity of methotrexate (figure 1) for the treatment of human cancers in the early 1950s prompted the search for other folate analogs that were more active than methotrexate or, at least, that had different properties than this important folate antimetabolite. After 40 years of preclinical and clinical investigation, methotrexate is still in clinical use and still represents the only folate analog in widespread therapeutic application for the treatment of cancers. This is the case, in spite of the fact that thousands of folate analogs have been made and studied in the interim and that the potential of folate antimetabolites as therapeutic agents is established.Of course, the pharmaceutical promise for a new class of folate antimetabolites also continues to be high, given the central nature of the folate-dependent enzymes in processes required for any proliferative cell population.

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  1. Richard G. Moran
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  1. University of Southern California Cancer Center, USA

    F. M. Muggia

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Moran, R.G. (1992). Folate antimetabolites inhibitory to de novo purine synthesis. In: Muggia, F.M. (eds) New Drugs, Concepts and Results in Cancer Chemotherapy. Cancer Treatment and Research, vol 58. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3876-9_4

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  • DOI: https://doi.org/10.1007/978-1-4615-3876-9_4

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