SYNTHESIS AND BIOLOGICAL EVALUATION OF AZIRIDIN-1-YL OXIME-BASED VORINOSTAT ANALOGS AS ANTICANCER AGENTS

Authors

  • Anna Nikitjuka Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009
  • Irina Shestakova Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009
  • Nadezhda Romanchikova Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009
  • Aigars Jirgensons Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009

DOI:

https://doi.org/10.1007/2467

Keywords:

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

Abstract

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.

How to Cite
Nikitjuka, A.; Shestakova, I.; Romanchikova, N.; Jirgensons, A. Chem. Heterocycl. Compd. 2015, 51, 647. [Khim. Geterotsikl. Soedin. 2015, 51, 647.]

For this article in the English edition see DOI 10.1007/s10593-015-1752-z

Author Biographies

Anna Nikitjuka, Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009

Anna Nikitjuka

OSM group, researcher

Irina Shestakova, Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009

Irina Shestakova

Nadezhda Romanchikova, Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009

Nadezhda Romanchikova

Aigars Jirgensons, Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1009

Aigars Jirgensons

Downloads

Published

2015-07-31

Issue

Vol. 51 No. 7 (2015)

Section

Original Papers