5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells

Julia Senkiv, Nataliya Finiuk, Danylo Kaminskyy, Dmytro Havrylyuk, Magdalena Wojtyra, Iryna Kril, Andrzej Gzella, Rostyslav Stoika, Roman Lesyk

Research output: Contribution to journalArticlepeer-review

55 Scopus citations


The article presents the synthesis of 5-ene-4-thiazolidinone derivatives with pyrazole core linked by enamine group. The structure and purity of compounds were confirmed by analytical and spectral data including X-ray analysis. Target compounds were screened for their anticancer activity and selective antileukemic action was confirmed. 5-[5-(2-Hydroxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-3-(3-acetoxyphenyl)-2-thioxothiazolidin-4-one (compound 1) was selected as most active agent against HL-60 and HL-60/ADR cell lines; IC50 Combining double low line 118 nM/HL-60 with low toxicity towards pseudonormal cells. The mitochondria-depended apoptosis was identified as the main mode of 1 action. Moreover compound's effect induces G0/G1 arrest of the treated cells and causes inhibition of cell division and is related with activation of ROS production.

Original languageEnglish
Pages (from-to)33-46
Number of pages14
JournalEuropean Journal of Medicinal Chemistry
StatePublished - Jul 19 2016

Bibliographical note

Funding Information:
The authors support all people of good will currently struggling for the liberty and justice in Ukraine. The authors thank the Association for Regional Cooperation in the Fields of Health, Science and Technology (RECOOP HST Association) and Dr. Sandor Vari (president of the RECOOP HST Association) for their support. This work was partially supported by the West-Ukrainian Biomedical Research Center (for Julia Senkiv and Natalia Finiuk in 2015/2016).

Publisher Copyright:
© 2016 Elsevier Masson SAS All rights reserved.

Copyright 2020 Elsevier B.V., All rights reserved.


  • 5-Ene-4-thiazolidinones
  • Anticancer activity
  • Apoptosis
  • Leukemia
  • ROS

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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