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

Anna Nikitjuka, Irina Shestakova, Nadezhda Romanchikova, Aigars Jirgensons
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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


Keywords


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

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