Pyrazolines are well known and important nitrogen containing 5‐membered heterocyclic compounds. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. The newly synthesized 2‐pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. All of the newly synthesized target compounds were selected by the NCI for in vitro biological evaluation. These active compounds exhibited broad spectrum of various biological activities. Most of the compounds showed potent activity.