Chemistry of Heterocyclic Compounds

, Volume 51, Issue 7, pp 647–657 | Cite as

Synthesis and biological evaluation of aziridin-1-yl oxime-based vorinostat analogs as anticancer agents

  • Anna NikitjukaEmail author
  • Irina Shestakova
  • Nadezhda Romanchikova
  • Aigars Jirgensons
The suberoyl anilide hydroxamic acid (vorinostat) analogs with the aziridin-1-yl oxime moiety as a possible metal chelating functionality have been synthesized. Their biological activity and stability under physiological conditions have been evaluated. Although some of the synthesized compounds demonstrated high antiproliferative activity against human HT1080 fibrosarcoma (HT1080, IC50 0.3–7.7 μM) comparable to vorinostat (HT1080, IC50 2.4 μM), they showed only weak histone deacetylase inhibition activity in HeLa cell line extracts.


aldoxime aziridin-1-yl oxime histone deacetylase hydroximoyl chloride suberoyl anilide hydroxamic acid cytotoxic activity 


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Anna Nikitjuka
    • 1
    Email author
  • Irina Shestakova
    • 1
  • Nadezhda Romanchikova
    • 1
  • Aigars Jirgensons
    • 1
  1. 1.Latvian Institute of Organic SynthesisRigaLatvia

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