Synthesis and Biological Evaluation of Aziridin-1-Yl Oxime-Based Vorinostat Analogs as Anticancer Agents

Chemistry of Heterocyclic Compounds 2015
Anna Nikitjuka, Irina Shestakova, Nadezda 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, IC<inf>50</inf> 0.3–7.7 μM) comparable to vorinostat (HT1080, IC<inf>50</inf> 2.4 μM), they showed only weak histone deacetylase inhibition activity in HeLa cell line extracts.

Keywords
aldoxime | aziridin-1-yl oxime | cytotoxic activity | histone deacetylase | hydroximoyl chloride | suberoyl anilide hydroxamic acid
DOI
10.1007/s10593-015-1752-z
Hyperlink
http://link.springer.com/article/10.1007%2Fs10593-015-1752-z

Nikitjuka, A., Shestakova, I., Romanchikova, N., Jirgensons, A. Synthesis and Biological Evaluation of Aziridin-1-Yl Oxime-Based Vorinostat Analogs as Anticancer Agents. Chemistry of Heterocyclic Compounds, 2015, Vol.51, Iss.7, pp.647-657. ISSN 0009-3122. e-ISSN 1573-8353. Available from: doi:10.1007/s10593-015-1752-z

Publication language
English (en)