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
  • 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: [email protected].
PMID: 24852281 DOI: 10.1016/j.ejmech.2014.05.009
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.