Sciact
  • EN
  • RU

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

Journal MolBank
ISSN: 1422-8599
Output data Year: 2023, Volume: 2023, Number: 4, Pages: M1743 Pages count : DOI: 10.3390/m1743
Tags resin acids; TDP1 inhibitors; heterocyclic compounds; DNA repair; parabanic acid; adamantane; dehydroabietic acid; abietic acid
Authors Kovaleva Kseniya S. 1 , Yarovaya Olga I. 1 , Chernyshova Irina A. 2 , Zakharenko Alexandra L. 2 , Cheresiz Sergey V. 3 , Azimirad Amirhossein 3 , Pokrovsky Andrey G. 3 , Lavrik Olga I. 2 , Salakhutdinov Nariman F. 1
Affiliations
1 N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences
2 Institute of Chemical Biology and Fundamental Medicine SB RAS
3 Novosibirsk State University

Funding (1)

1 Российский Научный Фонд
Министерство науки и инновационной политики Новосибирской области
23-23-10077

Abstract: 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.
Cite: Kovaleva K.S. , Yarovaya O.I. , Chernyshova I.A. , Zakharenko A.L. , Cheresiz S.V. , Azimirad A. , Pokrovsky A.G. , Lavrik O.I. , Salakhutdinov N.F.
Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1
MolBank. 2023. V.2023. N4. P.M1743. DOI: 10.3390/m1743 WOS Scopus РИНЦ OpenAlex
Dates:
Submitted: Oct 19, 2023
Accepted: Nov 7, 2023
Published print: Nov 9, 2023
Identifiers:
Web of science: WOS:001130831300001
Scopus: 2-s2.0-85180686638
Elibrary: 63938775
OpenAlex: W4388524215
Citing:
DB Citing
OpenAlex 2
Web of science 2
Altmetrics: