title: Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity.
abstract: In the present study, 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (1-6) were synthesized via the ring closure reaction of 1-(2-thienyl)-3-aryl-2-propen-1-ones with hydrazine hydrate in acetic acid. The chemical structures of the compounds were elucidated by IR, (1)H-NMR, (13)C-NMR and mass spectral data and elemental analyses. MTT assay, analysis of DNA synthesis and caspase-3 activation assay were carried out to determine anticancer effects of the compounds on A549 and C6 cancer cell lines. They exhibited dose-dependent anticancer activity against A549 and C6 cancer cell lines. Anticancer activity screening results revealed that compounds 1, 2 and 4 were the most potent derivatives among these compounds. But anticancer effects of these compounds may result from different death mechanisms in A549 and C6 cell lines.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University , Eskişehir , Turkey.
authors.forename: Ahmet
authors.initials: A
authors.lastname: Özdemir
authors.forename: Mehlika Dilek
authors.initials: MD
authors.lastname: Altıntop
authors.forename: Zafer Asım
authors.initials: ZA
authors.lastname: Kaplancıklı
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.forename: Gülşen Akalın
authors.initials: GA
authors.lastname: Ciftçi
authors.forename: Safak Ulusoylar
authors.initials: SU
authors.lastname: Yıldırım
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D011720:Pyrazoles