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  2. Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells

Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells

  • Eur J Med Chem. 2014 Jun 23:81:341-9. doi: 10.1016/j.ejmech.2014.05.009.
Kothanahally S Sharath Kumar 1 Ananda Hanumappa 1 Mahesh Hegde 1 Kereyagalahally H Narasimhamurthy 1 Sathees C Raghavan 2 Kanchugarakoppal S Rangappa 3
Affiliations

Affiliations

  • 1 Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
  • 2 Department of Biochemistry, Indian Institute of Science, Bangalore 560012, India.
  • 3 Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India. Electronic address: rangappaks@gmail.com.
Abstract

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.

Keywords

Apoptosis; Chemotherapeutics; Cytotoxicity; Leukemia; Propylphosphonic anhydride (T(3)P(®)); Thiazolidinones.

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