Molbank, Vol. 2023, Article M1743: Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1

Molbank, Vol. 2023, Article M1743: Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1

Molbank doi: 10.3390/M1743

Authors: Kseniya S. Kovaleva Olga I. Yarovaya Irina A. Chernyshova Alexandra L. Zakharenko Sergey V. Cheresiz Amirhossein Azimirad Andrey G. Pokrovsky Olga I. Lavrik Nariman F. Salakhutdinov

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.