A series of 7-arylindoline-1-benzenesulfonamides were prepared and evaluated for anticancer activity. 7-(4′-Cyanophenyl)indoline-1-benzenesulfonamide 15 exhibited substantial antiproliferative activity with IC50 values ranging from 17–32 nM against a variety of human cancer cell lines, including MDR resistant line. Compound 15 (IC50 = 1.5 μM) also showed more potent inhibition of tubulin polymerization than 4a (combretastatin A-4, IC50 = 2.0 μM) and displayed strong binding to the colchicine binding site of the tubulin.
