Synthesis and evaluation of new pyrazoline derivatives as potential anticancer agents

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Karabacak M., ALTINTOP M. D., Çiftçi H. I., Koga R., Otsuka M., Fujita M., ...Daha Fazla

Molecules, cilt.20, sa.10, ss.19066-19084, 2015 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 20 Sayı: 10
  • Basım Tarihi: 2015
  • Doi Numarası: 10.3390/molecules201019066
  • Dergi Adı: Molecules
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.19066-19084
  • Anahtar Kelimeler: pyrazoline, oxadiazole, anticancer activity, apoptosis, DNA cleavage, BEARING BENZENE SULFONAMIDE, VITRO ANTITUMOR-ACTIVITY, BIOLOGICAL EVALUATION, ANTIFUNGAL ACTIVITIES, MOIETY, INHIBITORS, CARCINOMA, SCAFFOLD, HYBRIDS, DESIGN
  • Anadolu Üniversitesi Adresli: Evet

Özet

© 2015 by the authors; licensee MDPI, Basel, Switzerland.New 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.