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New derivatives of dehydroabiethylamine and adamantane: synthesis and activity as inhibitors of the repair enzyme TDP1

  • K. S. Kovaleva,
  • O. I. Yarovaya,
  • I. A. Chernyshova,
  • O. I. Lavrik,
  • N. F. Salakhutdinov

摘要

A number of new conjugates of dehydroabiethylamine and adamantane was obtained using a three-step synthetic scheme in order to study the effect of linker type and length on biological activity. The inhibitory activity of the synthesized compounds toward the DNA repair enzyme Tyrosyl-DNA phosphodiesterase 1 was studied. The compounds are potent inhibitors, exhibiting activity in micromolar concentrations.