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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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Senkiv J,Finiuk N,Kaminskyy D,Havrylyuk D,Wojtyra M,Kril I,Gzella A,Stoika R,Lesyk R

doi

10.1016/j.ejmech.2016.03.089

subject

Has Abstract

pub_date

2016-07-19 00:00:00

pages

33-46

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30272-0

journal_volume

117

pub_type

杂志文章

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