Medicinal Chemistry Research

, Volume 28, Issue 1, pp 71–80 | Cite as

Synthesis, characterization, and in vitro anticancer evaluation of 2-substituted 5-arylsulfonyl-1,3-oxazole-4-carbonitriles

  • Maryna V. Kachaeva
  • Stepan G. Pilyo
  • Victor V. Zhirnov
  • Volodymyr S. Brovarets
Original Research


In this series, six new 2-substituted 5-arylsulfonyl-1,3-oxazole-4-carbonitriles were synthesized and characterized by IR, 1H NMR, 13C NMR spectroscopy, elemental analysis and chromato-mass-spectrometry. The anticancer activities of the compounds were evaluated via single high dose (10−5M) against 60 cancer cell lines by the National Cancer Institute according to its own screening protocol. In the next phase, the compounds have been selected for five-dose assay. All synthesized compounds displayed growth inhibitory (GI50) and cytostatic activities (TGI) against the most sensitive cell lines at submicromolar (0.2–0.6 μM) and micromolar concentrations (1–3 μM), respectively. Cytotoxic activity (LC50) of these compounds, with the exception of 4d, against the most sensitive cell lines was also high (5–6 μM). All compounds exhibit high selectivity towards leukemia cell lines, and among them, 4e and 4f showed the best antiproliferative and cytostatic selectivity. Compounds 4c and 4f displayed considerable cytotoxic selectivity towards the renal and breast cancer subpanels. Our results provided evidence for anticancer activities of novel 2-substituted 5-arylsulfonyl-1,3-oxazole-4-carbonitriles which could be useful for developing new anticancer drugs. These substances could also be used as an excellent framework in anticancer research that may lead to discovery of potent antitumor agents.


2-Substituted 5-arylsulfonyl-1,3-oxazole-4-carbonitriles Synthesis Anticancer activity Selectivity 



We would like to thank US Public Health Service and National Cancer Institute, Bethesda, MD, USA, for in vitro evaluation of anticancer activity (providing the NCI-60 cell testing) within the framework of Developmental Therapeutic Program (, and Enamine Ltd for the material and technical support.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.


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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • Maryna V. Kachaeva
    • 1
  • Stepan G. Pilyo
    • 1
  • Victor V. Zhirnov
    • 1
  • Volodymyr S. Brovarets
    • 1
  1. 1.Department of Chemistry of Bioactive Nitrogen-Containing Heterocyclic Bases, V.P. Kukhar Institute of Bioorganic Chemistry and PetrochemistryNAS of Ukraine, 1KyivUkraine

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