新型基于4-噻唑烷酮、吡啶和哌嗪的共轭物的合成及其对人白血病细胞的抗增殖作用。
Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells.
作者信息
Sharath Kumar Kothanahally S, Hanumappa Ananda, Hegde Mahesh, Narasimhamurthy Kereyagalahally H, Raghavan Sathees C, Rangappa Kanchugarakoppal S
机构信息
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
Department of Biochemistry, Indian Institute of Science, Bangalore 560012, India.
出版信息
Eur J Med Chem. 2014 Jun 23;81:341-9. doi: 10.1016/j.ejmech.2014.05.009. Epub 2014 May 4.
The present work reveals the synthesis and antiproliferative effect of a series of 2, 3 disubstituted 4-thiazolidinone analogues on human leukemic cells. The chemical structures of newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR and mass spectral analysis. Compound methyl 3-methoxy-4-(4-oxo-3-(5-(piperazin-1-yl)pyridin-2-yl)thiazolidin-2-yl)benzoate (5) displayed potent activity (IC509.71, 15.24 and 19.29 μM) against Nalm6, K562, Jurkat cells. Cell cycle analysis and mitochondrial membrane potential further confirmed that compound 5 is cytotoxic and able to induce cell death.
本研究揭示了一系列2,3-二取代4-噻唑烷酮类似物的合成及其对人白血病细胞的抗增殖作用。通过红外光谱、核磁共振氢谱、核磁共振碳谱和质谱分析确定了新合成化合物的化学结构。化合物3-甲氧基-4-(4-氧代-3-(5-(哌嗪-1-基)吡啶-2-基)噻唑烷-2-基)苯甲酸甲酯（5）对Nalm6、K562、Jurkat细胞显示出较强的活性（IC50分别为9.71、15.24和19.29 μM）。细胞周期分析和线粒体膜电位进一步证实化合物5具有细胞毒性并能够诱导细胞死亡。
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