Computer-aided identification, synthesis, and biological evaluation of DNA polymerase η inhibitors for the treatment of cancer.
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Feb 2023
15 Feb 2023
Historique:
received:
22
08
2022
revised:
20
12
2022
accepted:
20
12
2022
pubmed:
10
1
2023
medline:
1
2
2023
entrez:
9
1
2023
Statut:
ppublish
Résumé
In cancer cells, Pol η allows DNA replication and cell proliferation even in the presence of chemotherapeutic drug-induced damages, like in the case of platinum-containing drugs. Inhibition of Pol η thus represents a promising strategy to overcome drug resistance and preserve the effectiveness of chemotherapeutic drugs. Here, we report the discovery of a novel class of Pol ƞ inhibitors, with 35 active close analogs. Compound 21 (ARN24964) stands out as the best inhibitor, with an IC
Identifiants
pubmed: 36621139
pii: S0223-5234(22)00946-1
doi: 10.1016/j.ejmech.2022.115044
pii:
doi:
Substances chimiques
Rad30 protein
EC 2.7.7.7
Platinum
49DFR088MY
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115044Informations de copyright
Copyright © 2023 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Marco De Vivo reports financial support was provided by Italian Association for Cancer Research. Marco De Vivo reports a relationship with Italian Institute of Technology that includes: funding grants. Marco De Vivo has patent #patent application IT 102022000007988. pending to Italian Institute of Technology. Nicoletta Brindani has patent #patent application IT 102022000007988. pending to Italian Institute of Technology. Federico Munafo’ has patent #patent application IT 102022000007988. pending to Italian Institute of Technology. Michela Nigro has patent #patent application IT 102022000007988. pending to Italian Institute of Technology. None.