New 5-Hydroxycoumarin-Based Tyrosyl-DNA Phosphodiesterase I Inhibitors Sensitize Tumor Cell Line to Topotecan.
DNA repair
coumarin
enzyme inhibition
monoterpene
synergy
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
23 May 2023
23 May 2023
Historique:
received:
29
03
2023
revised:
05
05
2023
accepted:
19
05
2023
medline:
12
6
2023
pubmed:
10
6
2023
entrez:
10
6
2023
Statut:
epublish
Résumé
Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is an important enzyme in the DNA repair system. The ability of the enzyme to repair DNA damage induced by a topoisomerase 1 poison such as the anticancer drug topotecan makes TDP1 a promising target for complex antitumor therapy. In this work, a set of new 5-hydroxycoumarin derivatives containing monoterpene moieties was synthesized. It was shown that most of the conjugates synthesized demonstrated high inhibitory properties against TDP1 with an IC
Identifiants
pubmed: 37298106
pii: ijms24119155
doi: 10.3390/ijms24119155
pmc: PMC10253161
pii:
doi:
Substances chimiques
tyrosyl-DNA phosphodiesterase
EC 3.1.4.-
Topotecan
7M7YKX2N15
Phosphodiesterase Inhibitors
0
Phosphoric Diester Hydrolases
EC 3.1.4.-
Antineoplastic Agents
0
TDP1 protein, human
EC 3.1.4.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Russian Science Foundation
ID : 19-13-00040
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