Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity

被引:15
|
作者
Ozdemir, Ahmet [1 ]
Altintop, Mehlika Dilek [1 ]
Kaplancikli, Zafer Asim [1 ]
Turan-Zitouni, Gulhan [1 ]
Ciftci, Gulsen Akalin [2 ]
Yildirim, Safak Ulusoylar [3 ]
机构
[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey
[2] Anadolu Univ, Fac Pharm, Dept Biochem, TR-26470 Eskisehir, Turkey
[3] Anadolu Univ, Fac Pharm, Dept Pharmacol, TR-26470 Eskisehir, Turkey
关键词
Pyrazoline; anticancer activity; MTT assay; caspase-3; activation; BEARING BENZENE SULFONAMIDE; VITRO ANTITUMOR-ACTIVITY; BIOISOSTERISM; CASPASE-3; DESIGN; MOIETY;
D O I
10.3109/14756366.2012.724682
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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, H-1-NMR, C-13-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.
引用
收藏
页码:1221 / 1227
页数:7
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