Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells.
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.
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
Kothanahally S
KS
Sharath Kumar
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
Ananda
A
Hanumappa
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
Mahesh
M
Hegde
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India.
Kereyagalahally H
KH
Narasimhamurthy
Department of Biochemistry, Indian Institute of Science, Bangalore 560012, India.
Sathees C
SC
Raghavan
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570006, India. Electronic address: rangappaks@gmail.com.
Kanchugarakoppal S
KS
Rangappa
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020014:K562 Cells; D007938:Leukemia / Q000473:pathology*; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D015394:Molecular Structure; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D010879:Piperazines; D011725:Pyridines; D053778:Thiazolidines; D000077489:Piperazine; C023666:pyridine
Apoptosis; Chemotherapeutics; Cytotoxicity; Leukemia; Propylphosphonic anhydride (T(3)P(®)); Thiazolidinones