title: 5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells.
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.
authors.affiliation: Institute of Cell Biology of National Academy of Sciences of Ukraine, 14/16 Drahomanov Str., Lviv 79005, Ukraine.
authors.forename: Julia
authors.initials: J
authors.lastname: Senkiv
authors.affiliation: Institute of Cell Biology of National Academy of Sciences of Ukraine, 14/16 Drahomanov Str., Lviv 79005, Ukraine.
authors.forename: Nataliya
authors.initials: N
authors.lastname: Finiuk
authors.affiliation: Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
authors.forename: Danylo
authors.initials: D
authors.lastname: Kaminskyy
authors.affiliation: Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
authors.forename: Dmytro
authors.initials: D
authors.lastname: Havrylyuk
authors.affiliation: Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
authors.forename: Magdalena
authors.initials: M
authors.lastname: Wojtyra
authors.affiliation: Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
authors.forename: Iryna
authors.initials: I
authors.lastname: Kril
authors.affiliation: Poznan University of Medical Sciences, 6 Grunwaldzka Str., Poznan 60780, Poland.
authors.forename: Andrzej
authors.initials: A
authors.lastname: Gzella
authors.affiliation: Institute of Cell Biology of National Academy of Sciences of Ukraine, 14/16 Drahomanov Str., Lviv 79005, Ukraine.
authors.forename: Rostyslav
authors.initials: R
authors.lastname: Stoika
authors.affiliation: Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine. Electronic address: dr_r_lesyk@org.lviv.net.
authors.forename: Roman
authors.initials: R
authors.lastname: Lesyk
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000188:drug therapy* / Q000473:pathology; D015394:Molecular Structure; D017382:Reactive Oxygen Species; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D017382:Reactive Oxygen Species; D045162:Thiazolidinediones
keywords: 5-Ene-4-thiazolidinones; Anticancer activity; Apoptosis; Leukemia; ROS