Pharmaceuticals (2021)
Update date:2022-08-11
Topics:
Kovaleva, Kseniya
Yarovaya, Olga
Ponomarev, Konstantin
Cheresiz, Sergey
Azimirad, Amirhossein
Chernyshova, Irina
Zakharenko, Alexandra
Konev, Vasily
Khlebnikova, Tatiana
Mozhaytsev, Evgenii
Suslov, Evgenii
Nilov, Dmitry
?vedas, Vytas
Pokrovsky, Andrey
Lavrik, Olga
Salakhutdinov, Nariman
In this paper, a series of novel abietyl and dehydroabietyl ureas, thioureas, amides, and thioamides bearing adamantane moieties were designed, synthesized, and evaluated for their in-hibitory activities against tyrosil-DNA-phosphodiesterase 1 (TDP1). The synthesized compounds were able to inhibit TDP1 at micromolar concentrations (0.19–2.3 μM) and demonstrated low cytotox-icity in the T98G glioma cell line. The effect of the terpene fragment, the linker structure, and the adamantane residue on the biological properties of the new compounds was investigated. Based on molecular docking results, we suppose that adamantane derivatives of resin acids bind to the TDP1 covalent intermediate, forming a hydrogen bond with Ser463 and hydrophobic contacts with the Phe259 and Trp590 residues and the oligonucleotide fragment of the substrate.
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