TY - JOUR
T1 - 5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells
AU - Senkiv, Julia
AU - Finiuk, Nataliya
AU - Kaminskyy, Danylo
AU - Havrylyuk, Dmytro
AU - Wojtyra, Magdalena
AU - Kril, Iryna
AU - Gzella, Andrzej
AU - Stoika, Rostyslav
AU - Lesyk, Roman
N1 - Publisher Copyright:
© 2016 Elsevier Masson SAS All rights reserved.
PY - 2016/7/19
Y1 - 2016/7/19
N2 - 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.
AB - 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.
KW - 5-Ene-4-thiazolidinones
KW - Anticancer activity
KW - Apoptosis
KW - Leukemia
KW - ROS
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U2 - 10.1016/j.ejmech.2016.03.089
DO - 10.1016/j.ejmech.2016.03.089
M3 - Article
C2 - 27089210
AN - SCOPUS:84964324607
SN - 0223-5234
VL - 117
SP - 33
EP - 46
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -