Design, synthesis, and biological evaluation of a series of benzofuran[3,2-d]pyrimidine-4(3H)-one derivatives containing thiosemicarbazone analogs as novel PARP-1 inhibitors.
Anti-tumor
PARP-1 inhibitor
Poly ADP-ribose polymerase
Thiosemicarbazone
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
10 2023
10 2023
Historique:
received:
31
05
2023
revised:
20
07
2023
accepted:
29
07
2023
medline:
14
8
2023
pubmed:
7
8
2023
entrez:
6
8
2023
Statut:
ppublish
Résumé
Poly ADP ribose polymerase-1 (PARP-1), one of the most important members of the PARP protein family, plays a crucial role in DNA damage repair, gene transcription, and apoptosis of cancer cells. In this work, benzofuran[3,2-d]pyrimidine-4(3H)-one was used as a framework to design and synthesize a series of novel PARP-1 inhibitors by introducing thiosemicarbazone or its derivatives into the scafford. Among all the target compounds, 19b and 19c were found to exhibit more potent inhibitory activity and higher selectivity against PARP-1 than Olaparib, especially the latter had an IC
Identifiants
pubmed: 37544273
pii: S0045-2068(23)00420-0
doi: 10.1016/j.bioorg.2023.106759
pii:
doi:
Substances chimiques
Benzofurans
0
DNA
9007-49-2
Poly(ADP-ribose) Polymerase Inhibitors
0
Pyrimidines
0
Thiosemicarbazones
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
106759Informations de copyright
Copyright © 2023 Elsevier Inc. 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.