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- Title
Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1.
- Authors
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.
- 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.
- Subjects
DNA ligases; OXALYL chloride; ADAMANTANE; ABIETIC acid
- Publication
Molbank, 2023, Vol 2023, Issue 4, pM1743
- ISSN
1422-8599
- Publication type
Article
- DOI
10.3390/M1743