Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells.
Anti-Cancer
Dual inhibitor
HDAC
PI3K
Rational drug design
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 Dec 2023
15 Dec 2023
Historique:
received:
01
08
2023
revised:
19
10
2023
accepted:
25
10
2023
medline:
27
11
2023
pubmed:
11
11
2023
entrez:
10
11
2023
Statut:
ppublish
Résumé
Inhibition of PI3K and histone deacetylase (HDAC) activity simultaneously using a single molecule appears to be a promising approach for cancer treatment. Current PI3K/HDAC dual inhibitors commonly use hydroxamate moiety as zinc binding group, which lack HDAC isoform selectivity and have potential genotoxicity. In this study, a novel series of benzamide-based PI3K/HDAC dual inhibitors were rationally designed and synthesized. Representative compound PH14 showed potent inhibitory activity toward PI3Kα and HDAC3, with IC
Identifiants
pubmed: 37948955
pii: S0223-5234(23)00882-6
doi: 10.1016/j.ejmech.2023.115915
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Histone Deacetylase Inhibitors
0
Phosphatidylinositol 3-Kinases
EC 2.7.1.-
Benzamides
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115915Informations de copyright
Copyright © 2023 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.