4.0 Article

Inhibitory properties of nitrogen-containing adamantane derivatives with monoterpenoid fragments against tyrosyl-DNA phosphodiesterase 1

Journal

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
Volume 41, Issue 6, Pages 657-662

Publisher

MAIK NAUKA/INTERPERIODICA/SPRINGER
DOI: 10.1134/S1068162015060199

Keywords

diazaadamantane; monoterpene; tyrosyl-DNA phosphodiesterase 1; inhibitor of DNA repair

Funding

  1. [14.604.21.0018]
  2. [RFMEFI60414X0018]

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The compounds containing diazaadamantane and monoterpene moieties have been found to inhibit human purified recombinant tyrosyl-DNA phosphodiesterase 1 (Tdp1), a DNA repair enzyme. Several compounds have been shown to be potent inhibitors of a new structural type. Improved inhibition efficiency has been observed for compounds with longer aliphatic chains and increased flexibility of substituent.

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