Synthesis and evaluation of some new pyrazoline substituted benzenesulfonylureas as potential antiproliferative agents.

Abstract Twenty six new pyrazoline substituted benzenesulfonylureas ( 2a – z ) were synthesized and tested for in vitro anticancer activity. Fourteen derivatives ( 2i , 2k – 2p , 2r , 2s – 2x ) were screened for their antiproliferative activity towards 60 human cancer cell lines by the National Cancer Institute (USA). Among them four compounds ( 2i , 2n , 2v and 2x ) exhibited significant growth inhibition and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compounds 2i , 2n , 2v and 2x showed effective growth inhibition (GI 50 MID) values of 2.62, 3.93, 3.33, 3.74 μM respectively beside cytostatic activity TGI (MG-MID) values of 8.42, 65.80, 24.00 and 36.06 μM respectively. The compound 2i displayed remarkable antiproliferative activity in 8 different cell lines with GI 50 less than 2 μM. Compounds 2n , 2v and 2x also displayed good antiproliferative activity against 11, 18 and 14 different cell lines respectively with GI 50 less than 3 μM.