Lung cancer is one of the most diagnosed cancers worldwide and the development of anticancer agents for the treatment of lung cancer is an important task for researchers. For this purpose, herein pyrazoline-based compounds 1–18 were investigated for their cytotoxic effects on A549 human lung adenocarcinoma and CCD-19Lu human lung fibroblast cell lines using MTT assay. According to the results, 1-(4-methoxyphenyl)-3-(2-furanyl)-5-(4-methylphenyl)-2-pyrazoline (7) was identified as the most promising anticancer agent due to its selective inhibitory effect on A549 cell line with an IC50 value of 138.63 µg/mL when compared with cyclophosphamide (IC50 = 309.97 µg/mL).