Nitrogen heterocyclic compounds such as pyrazolines have been found to possess a broad spectrum of biological activities such as anticancer, antitubercular, anti-inflammatory, analgesic, and antidepressant activities. Pyrazoline derivatives IV, V (a-e) have been synthesized from the intermediate chalcones III (a-h) by cyclizing with phenyl hydrazine and hydrazine hydrate. The structures of these compounds were confirmed by IR, NMR, and mass spectroscopy. Biological studies of the synthesized compounds showed promising antitumor, analgesic, and anti-inflammatory activities. The compounds were tested for their in vitro antitumor activity against EAC tumor cell lines. Compounds IVa and IVb showed the highest cytotoxicity of 80% at a 200 μg mL concentration. Among the tested compounds, IVa and Vd seem to be more effective analgesic agents. Compounds IVc, IVd, and Ve are found to be the most effective anti-inflammatory agents. Thus the results show that synthesized compounds possess antitumor, analgesic, and anti-inflammatory activity. It was observed that the test compounds with electron withdrawing groups (halogens) on the aromatic ring favors antitumor, analgesic, and anti-inflammatory activity.