Abstract <p>A number of histone deacetylase inhibitors (HDACi) containing an adamantane backbone in the CAP group, as well as hydroxamate or mercaptoacetamide functions as zinc-binding fragments connected via a monoterpene linker, were synthesized. It was found that, being HDAC inhibitors, the synthesized compounds significantly enhance the cytotoxic activity of cisplatin against human cervical carcinoma cells HeLa.</p>

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Synthesis and Chemo-Sensitizing Properties of New Monoterpene-Containing Inhibitors of Histone Deacetylases: Hydroxamic Acids and Mercaptoacetamides

  • Yu. R. Aleksandrova,
  • A. A. Munkuev,
  • I. A. Shagina,
  • E. V. Suslov,
  • K. P. Volcho,
  • N. F. Salakhutdinov,
  • M. E. Neganova

摘要

Abstract

A number of histone deacetylase inhibitors (HDACi) containing an adamantane backbone in the CAP group, as well as hydroxamate or mercaptoacetamide functions as zinc-binding fragments connected via a monoterpene linker, were synthesized. It was found that, being HDAC inhibitors, the synthesized compounds significantly enhance the cytotoxic activity of cisplatin against human cervical carcinoma cells HeLa.