4.1 Article

SYNTHESIS AND STRUCTURAL CHARACTERIZATION OF NOVEL 2-PYRAZOLINE DERIVATIVES: EVALUATION OF THEIR ANTIPROLIFERATIVE ACTIVITY AND FLUORESCENCE PROPERTIES

期刊

ACTA POLONIAE PHARMACEUTICA
卷 79, 期 5, 页码 643-659

出版社

POLSKIE TOWARZYSTWO FARMACEUTYCZNE
DOI: 10.32383/appdr/157503

关键词

synthesis; pyrazoline; structural characterization; cytotoxic; fluorescent imaging

资金

  1. Scientific and Technological Research Council of Turkey (TUEBITAK) [221S850]

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A series of novel 2-pyrazoline derivatives were synthesized and their antiproliferative activities against lung and breast cancer cells were investigated. The compounds showed higher inhibitory effects on lung cancer cells and induced apoptosis at high concentrations. In addition, some compounds exhibited fluorescence properties.
In this study, a series of novel 2-pyrazoline derivatives were synthesized and their structures were established by using spectral methods. The antiproliferative activities of compounds were investigated against human cell lines A-549 and MCF-7 by MTT assay and L-929 (mouse normal fibroblast) cell cytotoxicity was also examined. Apoptotic effects of the compounds in breast and lung cancer cells were assessed by Annexin V-FITC apoptosis assay using flow cytometry. The antiproliferative effect on lung carcinoma of the synthesized compounds was higher than breast carcinoma. Moreover, it was observed that none of the synthesized compounds have cytotoxic activity in healthy cells. Flow cytometry studies have shown that compounds induced apoptosis at high concentrations. Additionally, fluorescence cell imaging studies were performed for the first time in A-549 and MCF-7 cancer cell lines to determine the potential of the biosensor compounds by fluorescence microscopy. Compounds 4b, 4d, 4e, and 4f showed fluorescence properties by considering microscopic imaging.

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