Many derivatives of quinoline-2-one have been considered to synthesize and evaluate their biological properties due to their various biological effects, including antibacterial, antioxidant, anti-inflammatory, and anticancer activities. The connection of 4-hydroxyquinoline-2-one with 2-pyrazoline rings could make its the new remarkable activities. In this work, some 2-pyrazoline compounds were synthesized from α,βunsaturated ketones containing quinoline ring. 2-Pyrazoline derivatives was synthesized by reaction of α,βunsaturated ketones with 4-nitrophenylhydrazine with yields of 48–62%. Their structure was confirmed by IR, NMR and MS spectroscopic methods. Their anticancer activities were scanned by the standard methods. These compounds exhibited low toxicity to two cancer cell lines KB and HepG2.