DHFR inhibitors: Reading the past for discovering novel anticancer agents

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

Risultato della ricerca: Article

4 Citazioni (Scopus)

Abstract

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)1140-
Numero di pagine19
RivistaMolecules
Volume24
Stato di pubblicazionePublished - 2019

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Folic Acid Antagonists
Antineoplastic Agents
inhibitors
Reading
Pharmacologic Actions
Chemotherapy
Pharmaceutical Chemistry
Antifungal Agents
Antimalarials
Drug Discovery
drugs
Anti-Bacterial Agents
Drug Therapy
Enzymes
chemotherapy
Pharmaceutical Preparations
enzymes
Neoplasms
selectivity
cancer

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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DHFR inhibitors: Reading the past for discovering novel anticancer agents. / Raimondi, Maria Valeria; Randazzo, Ornella; La Franca, Mery; Barone, Giampaolo; Rossi, Daniela; Vignoni, Elisa; Collina, Simona.

In: Molecules, Vol. 24, 2019, pag. 1140-.

Risultato della ricerca: Article

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AU - Raimondi, Maria Valeria

AU - Randazzo, Ornella

AU - La Franca, Mery

AU - Barone, Giampaolo

AU - Rossi, Daniela

AU - Vignoni, Elisa

AU - Collina, Simona

PY - 2019

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AB - 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.

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JO - Molecules

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SN - 1420-3049

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