Synthesis and evaluation of new pyrazoline derivatives as potential anticancer agents
Molecules, vol.20, no.10, pp.19066-19084, 2015 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 20 Issue: 10
- Publication Date: 2015
- Doi Number: 10.3390/molecules201019066
- Journal Name: Molecules
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.19066-19084
- Keywords: pyrazoline, oxadiazole, anticancer activity, apoptosis, DNA cleavage, BEARING BENZENE SULFONAMIDE, VITRO ANTITUMOR-ACTIVITY, BIOLOGICAL EVALUATION, ANTIFUNGAL ACTIVITIES, MOIETY, INHIBITORS, CARCINOMA, SCAFFOLD, HYBRIDS, DESIGN
- Open Archive Collection: AVESIS Open Access Collection
- Anadolu University Affiliated: Yes
Abstract
© 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.