5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib.
Bortezomib
Combination therapy
Proteasome inhibitors
Selective class IIa HDAC inhibitors
Synergistic anti-cancer activity
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:
05 Jan 2024
05 Jan 2024
Historique:
received:
02
09
2023
revised:
18
10
2023
accepted:
21
10
2023
medline:
4
12
2023
pubmed:
19
11
2023
entrez:
18
11
2023
Statut:
ppublish
Résumé
Clinically used pan and class I HDACi cause severe side effects, whereas class IIa HDACi are less cytotoxic. Here, we present the synthesis and anticancer effects of a series of 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based amides and alkoxyamides derived from the previously reported class IIa HDACi YAK540. The most active class IIa inhibitor 1a showed nanomolar inhibition of the class IIa enzymes 4, 5, 7 (IC
Identifiants
pubmed: 37979441
pii: S0223-5234(23)00874-7
doi: 10.1016/j.ejmech.2023.115907
pii:
doi:
Substances chimiques
Histone Deacetylase Inhibitors
0
Bortezomib
69G8BD63PP
Oxadiazoles
0
Antineoplastic Agents
0
Hydroxamic Acids
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115907Informations de copyright
Copyright © 2023. Published by Elsevier Masson SAS.
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: Matthias U. Kassack, Thomas Kurz reports financial support was provided by Deutsche Forschungsgemeinschaft. Yodita Asfaha, Lukas M. Bollmann, Alexander J. Skerhut, Fabian Fischer reports financial support was provided by Deutsche Forschungsgemeinschaft (DFG).