65068-86-2Relevant articles and documents
Design, synthesis, and molecular docking study of new tyrosyl-dna phosphodiesterase 1 (Tdp1) inhibitors combining resin acids and adamantane moieties
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
, (2021/05/22)
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.
Synthesis of Homologs of 1-Isothiocyanatoadamantane
Pitushkin,Burmistrov,Butov
, p. 1475 - 1479 (2019/01/04)
Amines of the adamantane series reacted with carbon disulfide and di-tert-butyl dicarbonate in the presence of triethylamine and a catalytic amount of 4-(dimethylamino)pyridine to give homologs of 1-isothiocyanatoadamantane in 80–86% yields. Adamantan-2-a
Nitrogen heterocyclic carboximidamide compounds
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, (2008/06/13)
5-, 6- or 7-Membered fully saturated 1-azacarbocyclic-2-ylidene derivatives of guanidine having anti-secretory and hypoglycemic activities, and further useful for treatment of cardiovascular disease states.