Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1

New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic acid fragment made it possible to increase th...

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Veröffentlicht in:	MolBank 2023-11, Vol.2023 (4), p.M1743
Hauptverfasser:	Kovaleva, Kseniya S, Yarovaya, Olga I, Chernyshova, Irina A, Zakharenko, Alexandra L, Cheresiz, Sergey V, Azimirad, Amirhossein, Pokrovsky, Andrey G, Lavrik, Olga I, Salakhutdinov, Nariman F
Format:	Artikel
Sprache:	eng
Schlagworte:	Acids adamantane Analysis Cancer Chemical synthesis Chemotherapy Chloride Chromatography Cytotoxicity DNA DNA damage DNA repair Drugs Enzymes Genetic aspects Genetic research Heterocyclic compounds Identification and classification Methods Organic acids parabanic acid Peptides Prevention Properties Radiation Radiotherapy resin acids TDP1 inhibitors Toxicity
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Zusammenfassung:	New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic acid fragment made it possible to increase the solubility of compounds and conduct biological studies. The compounds inhibit the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 in submicromolar concentrations. Cytotoxic concentrations were also studied on the glioblastoma cell line SNB19.
ISSN:	1422-8599 1422-8599
DOI:	10.3390/M1743