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

62 Scopus citations

Abstract

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
Volume117
DOIs
StatePublished - Jul 19 2016

Bibliographical note

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

Keywords

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

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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