Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents

被引：82

作者：

Karabacak, Muhammed ^{[1
]}

Altintop, Mehlika Dilek ^{[1
]}

Ciftci, Halil Ibrahim ^{[2
]}

Koga, Ryoko ^{[2
]}

Otsuka, Masami ^{[2
]}

Fujita, Mikako ^{[3
]}

Ozdemir, Ahmet ^{[1
]}

机构：

[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey

[2] Kumamoto Univ, Sch Pharm, Dept Bioorgan Med Chem, Kumamoto 8620973, Japan

[3] Kumamoto Univ, Sch Pharm, Res Inst Drug Discovery, Kumamoto 8620973, Japan

来源：

MOLECULES | 2015年 / 20卷 / 10期

关键词：

pyrazoline; oxadiazole; anticancer activity; apoptosis; DNA cleavage; BEARING BENZENE SULFONAMIDE; VITRO ANTITUMOR-ACTIVITY; BIOLOGICAL EVALUATION; ANTIFUNGAL ACTIVITIES; MOIETY; INHIBITORS; CARCINOMA; SCAFFOLD; HYBRIDS; DESIGN;

D O I：

10.3390/molecules201019066

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：

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 mu M and 11.9 mu M, 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 mu M). 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.

引用

页码：19066 / 19084

页数：19

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