Research output: Contribution to journal › Article › peer-review
Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1. / Kovaleva, Kseniya S.; Yarovaya, Olga I.; Chernyshova, Irina A. et al.
In: MolBank, Vol. 2023, No. 4, М1743, 12.2023.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1
AU - Kovaleva, Kseniya S.
AU - Yarovaya, Olga I.
AU - Chernyshova, Irina A.
AU - Zakharenko, Alexandra L.
AU - Cheresiz, Sergey V.
AU - Azimirad, Amirhossein
AU - Pokrovsky, Andrey G.
AU - Lavrik, Olga I.
AU - Salakhutdinov, Nariman F.
N1 - This research was funded by the Russian Science Foundation, grant number 23-23-10077, https://rscf.ru/project/23-23-10077/ accessed on 8 November 2023, and the Government of the Novosibirsk Region (No p-53).
PY - 2023/12
Y1 - 2023/12
N2 - 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.
AB - 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.
KW - DNA repair
KW - TDP1 inhibitors
KW - abietic acid
KW - adamantane
KW - dehydroabietic acid
KW - heterocyclic compounds
KW - parabanic acid
KW - resin acids
UR - https://www.scopus.com/record/display.uri?eid=2-s2.0-85180686638&origin=inward&txGid=5da881f8312a4579d70c704e314e1d27
UR - https://www.mendeley.com/catalogue/eb65e4d7-aa38-3374-a24e-6dc4da54c82c/
U2 - 10.3390/M1743
DO - 10.3390/M1743
M3 - Article
VL - 2023
JO - MolBank
JF - MolBank
SN - 1422-8599
IS - 4
M1 - М1743
ER -
ID: 59544355