DHFR inhibitors: Reading the past for discovering novel anticancer agents

Mery La Franca, Giampaolo Barone, Maria Valeria Raimondi, Ornella Randazzo, Daniela Rossi, Elisa Vignoni, Simona Collina

Risultato della ricerca: Articlepeer review

21 Citazioni (Scopus)


Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, in order to thoroughly delineate the current landscape for medicinal chemists interested in furthering this study in the anticancer field.
Lingua originaleEnglish
pagine (da-a)1-19
Numero di pagine19
Stato di pubblicazionePublished - 2019

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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