Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents
AbstractNew pyrazoline derivatives were synthesized and evaluated for their cytotoxic effects on AsPC-1 human pancreatic adenocarcinoma, U87 and U251 human glioblastoma cell lines. 1-[((5-(4-Methylphenyl)-1,3,4-oxadiazol-2-yl)thio)acetyl]-3-(2-thienyl)-5-(4-chlorophenyl)-2-pyrazoline (11) was found to be the most effective anticancer agent against AsPC-1 and U251 cell lines, with IC50 values of 16.8 µM and 11.9 µM, respectively. Tumor selectivity of compound 11 was clearly seen between Jurkat human leukemic T-cell line and human peripheral blood mononuclear cells (PBMC). Due to its promising anticancer activity, compound 11 was chosen for apoptosis/necrosis evaluation and DNA-cleavage analysis in U251 cells. Compound 11-treated U251 cells exhibited apoptotic phenotype at low concentration (1.5 µM). DNA-cleaving efficiency of this ligand was more significant than cisplatin and was clearly enhanced by Fe(II)-H2O2-ascorbic acid systems. This result pointed out the relationship between the DNA cleavage and the cell death. View Full-Text
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Karabacak, M.; Altıntop, M.D.; İbrahim Çiftçi, H.; Koga, R.; Otsuka, M.; Fujita, M.; Özdemir, A. Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents. Molecules 2015, 20, 19066-19084.
Karabacak M, Altıntop MD, İbrahim Çiftçi H, Koga R, Otsuka M, Fujita M, Özdemir A. Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents. Molecules. 2015; 20(10):19066-19084.Chicago/Turabian Style
Karabacak, Muhammed; Altıntop, Mehlika D.; İbrahim Çiftçi, Halil; Koga, Ryoko; Otsuka, Masami; Fujita, Mikako; Özdemir, Ahmet. 2015. "Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents." Molecules 20, no. 10: 19066-19084.