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 |
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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 | ||||||
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Affiliations |
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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 РИНЦ
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 РИНЦ
Dates:
Submitted: | Oct 19, 2023 |
Accepted: | Nov 7, 2023 |
Published print: | Nov 9, 2023 |
Identifiers:
Web of science | WOS:001130831300001 |
Elibrary | 63938775 |
OpenAlex | W4388524215 |