DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.
DHFR drug discovery
DHFR inhibitors as anticancer agents
dihydrofolate reductase (DHFR) enzyme
heterocyclic compounds
hybrid compounds
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
22 Mar 2019
22 Mar 2019
Historique:
received:
25
02
2019
revised:
18
03
2019
accepted:
20
03
2019
entrez:
27
3
2019
pubmed:
27
3
2019
medline:
16
7
2019
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 30909399
pii: molecules24061140
doi: 10.3390/molecules24061140
pmc: PMC6471984
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Folic Acid Antagonists
0
Folic Acid
935E97BOY8
Tetrahydrofolate Dehydrogenase
EC 1.5.1.3
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Ministero dell'Istruzione, dell'Università e della Ricerca
ID : PJ_RIC_FFABR_2017_160599
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