吡咯烷二酮-噻唑烷酮杂合体的合成及抗白血病活性研究

Q4 Biochemistry, Genetics and Molecular Biology

Ukrainian Biochemical Journal Pub Date : 2020-04-17 DOI:10.15407/ubj92.02.108

Anna Kryshchyshyn, D. Kaminskyy, O. Roman, R. Kralovics, O. Karpenko, R. Lesyk

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引用次数: 11

摘要

合成了一系列新的2-（5-亚基-4-氧代-2-硫代噻唑烷-3-基）-琥珀酰亚胺和5-亚基-3-（1-芳基吡咯烷-2,5-二酮）-噻唑烷-2,4-二酮。提出了一种有效、简单的罗丹妮吡咯烷二酮杂化物合成方案，该方案避免了酸酐形成的步骤。根据先前有关噻唑烷酮衍生物抗白血病特性的数据，研究了19种靶化合物对四种白血病细胞系的活性：Dami、hl-60、Jurkat和K562。在测试的化合物中，3-[5-（4-氯-亚苄基）-4-氧代-2-硫代噻唑烷-3-基]-1-苯基-吡咯烷-2,5-二酮（化合物1）对Dami和hl-60细胞系具有良好和选择性的抗增殖作用，并且具有令人满意的毒性水平（在小鼠体内评估的急性毒性）。

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Synthesis and anti-leukemic activity of pyrrolidinedione-thiazolidinone hybrids

A series of novel 2-(5-ylidene-4-oxo-2-thioxo-thiazolidin-3-yl)-succinimides and 5-ylidene-3-(1-arylpyrrolidine-2,5-dione)-thiazolidine-2,4-diones were synthesized. An efficient simple protocol for rhodaninepyrrolidinedione hybrids synthesis which allows avoiding the step of anhydride formation was proposed. Following the previous data on antileukemic properties of related thiazolidinone derivatives, the activity of 19 target compounds was investigated towards four leukemia cell lines: Dami, hl-60, Jurkat, and K562. Among the tested compounds, 3-[5-(4-chloro-benzylidene)-4-oxo-2-thioxo-thiazolidin-3-yl]-1-phenyl-pyrrolidine-2,5-dione (compound 1) possessed good and selective antiproliferative action against Dami and hl-60 cell lines and satisfactory toxicity level (acute toxicity evaluated in vivo in mice).

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来源期刊

Ukrainian Biochemical Journal Biochemistry, Genetics and Molecular Biology-Biochemistry

CiteScore

1.20

自引率

0.00%

发文量

审稿时长

16 weeks

期刊介绍： The Ukrainian Biochemical Journal publishes original research papers, reviews and brief notes; papers on research methods and techniques; articles on the history of biochemistry, its development and prominent figures; discussion articles; book reviews; chronicles; etc. The journal scope includes not only biochemistry but also related sciences, such as cellular and molecular biology, bioorganic chemistry, biophysics, pharmacology, genetics, and medicine (medical biochemistry et al.) – insofar as the studies use biochemical methods and discuss biochemical findings.