Molecules (Sep 2022)

Folic Acid Antimetabolites (Antifolates): A Brief Review on Synthetic Strategies and Application Opportunities

  • Igor S. Kovalev,
  • Grigory V. Zyryanov,
  • Sougata Santra,
  • Adinath Majee,
  • Mikhail V. Varaksin,
  • Valery N. Charushin

DOI
https://doi.org/10.3390/molecules27196229
Journal volume & issue
Vol. 27, no. 19
p. 6229

Abstract

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Antimetabolites of folic acid represent a large group of drugs and drug candidates, including those for cancer chemotherapy. In this current review, the most common methods and approaches are presented for the synthesis of therapeutically significant antimetabolites of folic acid, which are Methotrexate (MTX), Raltitrexed (Tomudex, ZD1694), Pralatrexate, Pemetrexed, TNP-351, and Lometrexol. In addition, the applications or uses of these folic acid antimetabolites are also discussed.

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