2. Academic Validation
  3. 5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells

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

  • Eur J Med Chem. 2016 Jul 19:117:33-46. doi: 10.1016/j.ejmech.2016.03.089.
Julia Senkiv 1,  Nataliya Finiuk 1,  Danylo Kaminskyy 2,  Dmytro Havrylyuk 2,  Magdalena Wojtyra 2,  Iryna Kril 2,  Andrzej Gzella 3,  Rostyslav Stoika 1,  Roman Lesyk 4
Affiliations

Affiliations

  • 1 Institute of Cell Biology of National Academy of Sciences of Ukraine, 14/16 Drahomanov Str., Lviv 79005, Ukraine.
  • 2 Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
  • 3 Poznan University of Medical Sciences, 6 Grunwaldzka Str., Poznan 60780, Poland.
  • 4 Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine. Electronic address: dr_r_lesyk@org.lviv.net.
PMID: 27089210 DOI: 10.1016/j.ejmech.2016.03.089
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 = 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.

Keywords

5-Ene-4-thiazolidinones; Anticancer activity; Apoptosis; Leukemia; ROS.

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