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Synthesis and Inhibitory Properties of Imines Containing Monoterpenoid and Adamantane Fragments Against DNA Repair Enzyme Tyrosyl-DNA Phosphodiesterase 1 (Tdp1)

Author:
Zakharenko, A. L., Mozhaitsev, E. S., Suslov, E. V., Korchagina, D. V., Volcho, K. P., Salakhutdinov, N. F., Lavrik, O. I.
Source:
Chemistry of natural compounds 2018 v.54 no.4 pp. 672-676
ISSN:
0009-3130
Subject:
DNA repair, aldehydes, chemistry, enzyme inhibition, enzyme inhibitors, humans, imines, inhibitory concentration 50, monoterpenoids, phosphodiesterase I, recombinant DNA
Abstract:
Six imines including four new ones were synthesized via the reaction of monoterpenoid aldehydes with aminoadamantanes. The inhibitory activities of the synthesized compounds against purified human recombinant DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) fell in the range IC₅₀ = 5.5–7.1 μM.
Agid:
6079246